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  • Inhibitors & Agonists
    75
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Balsalazide sodium hydrate
Balsalazide disodium dihydrate,Balsalazide disodium salt dihydrate,Balsalazide disodium
T4615150399-21-6
Balsalazide sodium hydrate (Balsalazide disodium) is an anti-inflammatory compound used in the treatment of Inflammatory Bowel Disease.Balsalazide sodium hydrate is a new 5-aminosalicylic acid (5-ASA) containing prodrug. High dose Balsalazide sodium hydrate(3.0 g twice daily) was superior in maintaining remission in patients with ulcerative colitis compared with a low dose (1.5 g twice daily) or a standard dose of mesalazine (0.5 g three times daily). All three treatments were safe and well tolerated [1]. Balsalazide sodium hydrate is approved for the treatment of mild-to-moderate active UC. It is efficacious for the induction of remission in mild to moderate UC and has a favorable safety profile, with the added advantages of greater efficacy of remission induction and rapidity of onset [2].
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Etripamil
MSP-2017,(-)-MSP-2017
T152571593673-23-4In house
Etripamil (MSP-2017) displays atrioventricular nodal conduction and prolongs atrioventricular nodal refractory periods by inhibiting calcium ion influx through the calcium slow channels in the atrioventricular node cells. Etripamil is an antagonist of short-acting L-type calcium-channel. It has a rapid onset of action designed for intranasal administration. It is also used to treat Paroxysmal Supraventricular Tachycardia.
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Fosdevirine
GSK-2248761A,IDX 899,GSK 2248761A,GSK 2248761,GSK-2248761,IDX-12899,GSK2248761,FDV,GSK2248761A
T318601018450-26-4In house
Fosdevirine (GSK2248761) is a selective and potent non-nucleoside reverse transcriptase (NNRTI) inhibitor with anti-HIV activity for the study of neurological related disorders such as late-onset epilepsy.
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6-8weeks
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Tranylcypromine hemisulfate
Tranylcypromine Sulfate,Tranylcypromine (hemisulfate)
T794213492-01-8
Tranylcypromine hemisulfate (Tranylcypromine Sulfate) is an inhibitor of monoamine oxidase (MAO) and lysine-specific demethylase 1 (LSD1) with a rapid onset of activity.
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TargetMol | Citations Cited
D-Leucine
(R)-Leucine
T9299328-38-1
D-Leucine ((R)-Leucine) potently terminates seizures even after the onset of seizure activity. D-leucine reduces long-term potentiation but had no effect on basal synaptic transmission in vitro.
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Procaine
Duracaine,Spinocaine,Novocaine,Vitamin H3
T002959-46-1
Procaine (Vitamin H3) is a local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block.
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Zonisamide
AD 810,CI 912
T026768291-97-4
Zonisamide (AD 810), a sulfonamide anticonvulsant, is approved for use as an adjunctive treatment in adults with partial-onset seizures. It may inhibit a carbonic anhydrase although this is not one of the main mechanisms of action. Zonisamide may act by blocking repetitive firing of voltage-gated sodium channels results in a reduction of T-type calcium channel currents, or by binding allosterically to GABA receptors. This latter action may lower the uptake of the inhibitory neurotransmitter GABA while increasing the uptake of the excitatory neurotransmitter glutamate.
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Lacidipine
SN-305,GX-1048,GR-43659X
T1439103890-78-4
Lacidipine (SN-305) is a lipophilic dihydropyridine calcium antagonist with an intrinsically slow onset of activity. Due to its long duration of action, lacidipine does not lead to reflex tachycardia. It displays specificity in the vascular smooth muscle, where it acts as an antihypertensive agent to dilate peripheral arterioles and reduce blood pressure.
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Uridine triacetate
RG 2133 triacetate,PN-401,Tri-O-acetyluridine,PN401,RG 2133,RG-2133,PN 401,RG2133,RG2133 triacetate
T213274105-38-8
Uridine triacetate (RG 2133 triacetate) (Tri-O-acetyl uridine), an orally active prodrug of uridine, is efficiently absorbed in the gut and swiftly deacetylated in the circulation to release free uridine. It is utilized in the research of 5-fluorouracil (5-FU) and capecitabine toxicity, particularly targeting early-onset cardiac or central nervous system (CNS) complications.
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Levetiracetam
UCB L059,SIB-S1
T0192102767-28-2
Levetiracetam (SIB-S1) is a relatively unique anticonvulsant that is typically used in combination with other antiepileptic medications for partial onset seizures. Levetiracetam has been linked to rare instances of serum aminotransferase and alkaline phosphatase elevations during treatment and to rare cases of clinically apparent drug induced liver disease.
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Bilastine
Bilaxten
T4250202189-78-4
Bilastine (Bilaxten) is a novel new-generation antihistamine that is highly selective for the H1 histamine receptor, has a rapid onset and prolonged duration of action.
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Procaine hydrochloride
Novocaine HCl,Procaine HCl
T080251-05-8
Procaine hydrochloride (Novocaine HCl) is the hydrochloride salt form of procaine, a benzoic acid derivative with local anesthetic and antiarrhythmic properties. Procaine binds to and inhibits voltage-gated sodiumchannels, thereby inhibiting the ionic flux required for the initiation and conduction of impulses. In addition, this agent increases electrical excitation threshold, reduces rate of rise of action potential and slows nerve impulse propagation thereby causing loss of sensation.
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Menbutone
Naftobil,Genabilic acid,Genabilin
T11483562-99-0
Menbutone (Genabilin) is a derivative of oxobutyric acid, and is a choleretic. Menbutone shows a rapid onset of action, reaching its maximum plasma level within 1 hour and lasting for roughly 10 hours.
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Eslicarbazepine Acetate
Zebinix,Aptiom,BIA 2-093,Exalief,Stedesa
T3285236395-14-5
Eslicarbazepine Acetate (Zebinix) is an anticonvulsant medication approved for use in Europe, the United States and Canada as an adjunctive therapy for partial-onset seizures that are not adequately controlled with conventional therapy.
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Tribromoethyl alcohol
2,2,2-Tribromoethanol,Avertin,Basibrol,Tribromoethanol,TBE
T080775-80-9
Tribromoethyl alcohol (Avertin) is an organic compound used to anesthetize mice.
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Dexketoprofen trometamol
T9284156604-79-4
Dexketoprofen trometamol is a modified non-selective COX inhibitor with a rapid onset of action that is available as both oral and parenteral formulations.
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Etidocaine
T31716L36637-18-0In house
Etidocaine is an amino acidamide that acts as a local anesthetic with fast onset and long-acting properties.
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(Iso)-Fosdevirine
(Iso)-Fosdevirine(Iso-1018450-26-4),(Iso)-GSK2248761
T31860L2869918-45-4In house
(Iso)-Fosdevirine ( (Iso)-GSK2248761) is a selective and potent non-nucleoside reverse transcriptase (NNRTI) inhibitor with anti-HIV activity for the study of neurological disorders such as late-onset epilepsy.
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Vatanidipine
AE-0047,AE 0047,AE0047
T24932116308-55-5In house
Vatanidipine (AE0047) is a novel dihydropyridine (DHP)-type calcium channel blocker with slow-onset pharmacological actions.A slow-onset and long-lasting hypotensive action was observed in various experimental hypertensive models.
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6-8 weeks
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Litoxetine
T6795686811-09-8In house
Litoxetine is a selective 5-HT uptake inhibitor and is a 5-HT3 receptor antagonist. Litoxetine acts as an antidepressant and has shown antiemetic properties in ferrets. Litoxetine (1 and 10 mg kg i.v.) dose-dependently reduced the number of regurgitations and vomiting and delayed the onset of vomiting. Litoxetine has an affinity for brain 5HT3 receptors (Ki = 85 nM).
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6-8weeks
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Nemifitide acetate(173240-15-8 free base)
INN 00835 acetate
TP1127L1
Nemifitide acetate(173240-15-8 free base) (INN 00835 acetate) is a synthetic pentapeptide antidepressant with a potential for rapid onset of action. It is a peptide analog of melanocyte-inhibiting factor (MIF).
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AMG-369
AMG-247,AMG369,AMG 369,AMG 247,AMG247
T299711202073-26-4In house
AMG-369 (AMG 247) is an S1P1 S1P5 dual agonist that delays the onset of experimental autoimmune encephalomyelitis in rats. encephalomyelitis in rats.
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10-14 weeks
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Vonsetamig
T808552408319-33-3
Vonsetamig, a humanized immunoglobulin G4-kappa monoclonal antibody, targets both TNFRSF17 and CD3E. It serves as an antineoplastic agent.
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BMS-P5 free base
T22277L1550371-22-6
BMS-P5 free base is a specific and orally active peptidylarginine deiminase 4 (PAD4) inhibitor that blocks the formation of Neutrophil Extracellular Traps and delays the progression of multiple myeloma. Administration of BMS-P5 to multiple myeloma-bearing mice delays symptom onset and disease progression. Targeting PAD4 may be beneficial for treating multiple myeloma.
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Atosiban acetate
RW22164,Atosiban acetate (90779-69-4 free base),RWJ22164
T5148914453-95-5
Atosiban acetate (RW22164) is an inhibitor of the hormones oxytocin and vasopressin. It is used as an intravenous medication as a labour repressant (tocolytic) to halt premature labor. Atosiban acetate (RW22164) inhibits the oxytocin-mediated release of inositol trisphosphate from the myometrial cell membrane. As a result, there is reduced release of intracellular, stored calcium from the sarcoplasmic reticulum of myometrial cells, and reduced influx of Ca2+ from the extracellular space through voltage gated channels. In addition, Atosiban acetate (RW22164) suppresses oxytocin-mediated release of PGE and PGF from the decidua. In human pre-term labor, atosiban, at the recommended dosage, antagonizes uterine contractions and induces uterine quiescence. The onset of uterus relaxation following atosiban is rapid, uterine contractions being significantly reduced within 10 minutes to achieve stable uterine quiescence.
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ZZL-7
T6431799141-91-0
ZZL-7 is a fast-onset antidepressant agent that disrupts the interaction between neuronal nitric oxide synthase (nNOS) and the serotonin transporter (SERT) in the dorsal raphe nucleus (DRN). It easily crosses the blood-brain barrier and has research value in major depressive disorder (MDD).
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Tiotropium Bromide hydrate
BA-679 BR hydrate,BA 679BR
T6707411207-31-3
Tiotropium Bromide hydrate (BA-679 BR hydrate) is a potent anticholinergic and bronchodilator, serving as a muscarinic receptor antagonist, specifically targeting mAChR. It is developed for treating chronic obstructive airways disease (COPD), demonstrating novel and long-lasting effects. Binding studies with [3H]tiotropium bromide in human lung reveal its high potency and equivalent affinity for M1-, M2-, and M3-receptors, making it roughly 10 times more effective than ipratropium bromide. It notably inhibits cholinergic nerve-induced contraction of both guinea-pig and human airways more potently than atropine or ipratropium bromide, albeit with a slower onset. Tiotropium bromide uniquely presents slow dissociation from M3-receptors on airway smooth muscle and rapid dissociation from M2 autoreceptors on cholinergic nerve terminals. As a quaternary ammonium derivative, it shows high affinity and special kinetic selectivity towards muscarinic receptors across M1-, M2-, and M3-subtypes, due to its slower dissociation from M1- and M3-receptors compared to M2-receptors.
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6-8 weeks
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Masavibart
T744242640223-84-1
Masavibart (ZRC3308-A7), an IgG1 type anti-SARS-CoV-2 monoclonal antibody, demonstrates strong binding affinity for a distinct non-competing epitope located on the receptor-binding domain (RBD) of the SARS-CoV-2 spike protein. When paired in a 1:1 ratio with ZRC3308-B10, Masavibart is efficacious in preventing COVID-19, particularly in its early stages before the onset of severe symptoms [1].
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5β-Dihydroprogesterone
T37319128-23-4
5β-Dihydroprogesterone (5β-DHP) is a progesterone receptor agonist and metabolite of progesterone .1,2It is formed from progesterone by 5β-reductase.25β-DHP inhibits spontaneous contractions in isolated rat uterus when used at a concentration of 10 μg/ml, an effect that can be blocked by the progesterone receptor antagonist RU486 but not the GABAAreceptor antagonist picrotoxin .1It is a negative modulator of homooligomeric Ρ1 subunit-containing GABAAreceptors, inhibiting GABA-induced currents inX. laevisoocytes expressing these receptors (IC50= 5.02 μM).3Plasma levels of 5β-DHP decrease at the onset of spontaneous human labor.4
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7-10 days
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PLP (178-191)
T81439172228-98-7
PLP (178-191), an immunodominant encephalitogenic epitope from the proteolipid protein (PLP) fragment spanning amino acids 178 to 191, plays a pivotal role in SJL mice. It initiates disease onset earlier compared to the other major encephalitogenic epitope, PLP (139-151), though both epitopes result in similar incidence, severity, and histologic characteristics.
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Noberastine citrate
T70773139751-07-8
Noberastine citrate, a histamine H1 antagonist, has potent and specific peripheral antihistaminic activity. Noberastine, a furan derivative of nor-astemizole (an astemizole metabolite), has been shown to have a more rapid onset, and shorter duration of action than astemizole with peak antihistaminic activity at 4h following ingestion. Noberastine is rapidly absorbed and the peak plasma levels are obtained within 2 h of oral dosing. In preclinical studies Noberastine has been shown to lack central nervous system effects. After subacute (steady-state) administration of noberastine, there was increasing inhibition of weal and flare formation with higher doses of the drug. The 30 mg daily dose showed maximum antihistaminic effects.
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1-2 weeks
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Evogliptin HCl
Evogliptin hydrochloride,DA 1229,DA1229,Evogliptin,DA-1229
T317321246960-27-9
Evogliptin(DA-1229) is a potent and selective DPP4 inhibitor (dipeptidyl peptidase 4 inhibitor) that can improve insulin resistance and delays the onset of diabetes. Evogliptin delays the onset of diabetes in young db/db mice and improves insulin sensitiv
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6-8 weeks
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CBR-5884
T14884681159-27-3
CBR-5884 is an selective, active of phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity. CBR-5884 selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis. Biochemical characterization of the inhibitor revealed that it was a noncompetitive inhibitor that showed a time-dependent onset of inhibition and disrupted the oligomerization state of PHGDH
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C12 Galactosylceramide (d18:1/12:0)
T3685841613-14-3
C12 Galactosylceramide is a bioactive sphingolipid. It inhibits IL-4 production by 53.84% in EL4 T cells when used at a concentration of 10 μM. C12 Galactosylceramide reduces the growth of human papillomavirus type 16-associated tumors in mice and reduces tumor recurrence following surgical removal or chemotherapy. It also reduces natural killer T cell activity, delays the onset of proteinuria, and improves survival in a mouse model of systemic lupus.
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Bilastine-d4
TMIJ-02602747918-37-0
Bilastine-d4 is a deuterated compound of Bilastine. Bilastine has a CAS number of 202189-78-4. Bilastine is a novel new-generation antihistamine that is highly selective for the H1 histamine receptor, has a rapid onset and prolonged duration of action.
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20 days
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Bilastine-d6
TMIJ-02592470116-56-2
Bilastine-d6 is a deuterated compound of Bilastine. Bilastine has a CAS number of 202189-78-4. Bilastine is a novel new-generation antihistamine that is highly selective for the H1 histamine receptor, has a rapid onset and prolonged duration of action.
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20 days
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Camoteskimab
T769382492472-82-7
Camoteskimab (AVTX-007), a fully human, high-affinity anti-IL-18 monoclonal antibody, holds promise for research into autoinflammatory diseases, such as adult-onset Still’s disease (AOSD) [1].
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Asfotase alfa
ENB-0040
T782411174277-80-5
Asfotase alfa (ENB-0040), a bone-targeted genetically engineered glycoprotein, enhances survival, bone mineralization, and growth while preventing mineralization defects in the feet, rib cage, lower limbs, and jaws of Akp2 − − knockout mice. It has applications in researching perinatal, infantile, and juvenile-onset hypophosphatasia (HPP) [1].
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Stearoylcarnitine
Stearoyl-L-carnitine
T1956425597-09-5
Stearoylcarnitine (Stearoyl-L-carnitine) is a fatty ester lipid molecule, a human endogenous metabolite that serves as a biomarker for early-onset preeclampsia and late-onset preeclampsia.
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7-10 days
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Tauro-ω-muricholic acid sodium
T63793
Tauro-ω-muricholic acid sodium (TωMCA sodium) is an analogue of tauro-α-muricholic acid, a bile acid derived from the liver. TωMCA sodium can serve as a serum marker for early onset neonatal sepsis (EOS) and biliary stasis.
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10-14 weeks
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EGTA-AM
EGTA Acetoxymethyl ester
T1367399590-86-0
EGTA-AM (EGTA Acetoxymethyl ester) is a calcium chelator, a metabolic biomarker of early-onset preeclampsia and late-onset preeclampsia.
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7-10 days
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Noberastine maleate
T71425111922-05-5
Noberastine maleate, a histamine H1 antagonist, has potent and specific peripheral antihistaminic activity. Noberastine, a furan derivative of nor-astemizole (an astemizole metabolite), has been shown to have a more rapid onset, and shorter duration of action than astemizole with peak antihistaminic activity at 4h following ingestion. Noberastine is rapidly absorbed and the peak plasma levels are obtained within 2 h of oral dosing. In preclinical studies Noberastine has been shown to lack central nervous system effects. After subacute (steady-state) administration of noberastine, there was increasing inhibition of weal and flare formation with higher doses of the drug. The 30 mg daily dose showed maximum antihistaminic effects.
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6-8 weeks
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Bucindolol hydrochloride
MJ 131051,Bucindolol HCl,MJ131051,MJ-13105-1,MJ-131051
T2692070369-47-0
Bucindolol is a beta-adrenergic receptor antagonist. Bucindolol is a fourth-generation β-blocker. Bucindolol prevented new-onset AF; β₁ and α(2c) polymorphisms predicted therapeutic response; and the 47% of patients who were β₁389 Arg homozygotes had an e
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1-2 weeks
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AS 1892802
T22037928320-12-1
AS 1892802 is a potent and selective inhibitor of ROCK. AS 1892802 exibits IC50 values of 52nM, 57nM and 122 nM for human ROCK2, rat ROCK2 and human ROCK1, respectively. The onset of antinociceptive effect of AS 1892802 is as fast as those of Tramadol and Diclofenac.
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6-8 weeks
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PF 05089771
PF-05089771,PF05089771
T7502L1235403-62-9
PF 05089771 is a Selective inhibitor of Nav1.7 (IC50 = 11 nM) that interacts with the voltage-sensor domain of domain IV. It shows a slow onset of the block that is depolarization and concentration-dependent.
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Clervonafusp alfa
T771312145123-44-8
Clervonafusp alfa (VAL-1221) is a fusion protein targeting both cytosolic and lysosomal glycogen, addressing the mechanisms of Pompe disease. It combines the Fab segment of a cell-penetrating antibody with recombinant human acid alpha-glucosidase (rhGAA). The Fab portion utilizes the nucleoside transporter ENT-2 for cytosolic entry, while rhGAA accesses lysosomes via mannose-6-phosphate receptors (M6PRs). This dual-targeting approach suggests Clervonafusp alfa as a potential therapeutic research candidate for late-onset Pompe disease [1].
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Neuromedin U-25 (human) (trifluoroacetate salt)
T35598
Neuromedin U (NMU) is a neuropeptide first demonstrated to drive smooth muscle contraction.1Translated as a 174 amino acid propeptide, NMU is cleaved to different lengths in different animals. It has diverse receptor-mediated rolesin vivo, as it regulates feeding, vasoconstriction, nociception, and bone remodeling and contributes to obesity, cancer and septic shock.2,2NMU-25 is the active form of NMU in humans. It binds with high affinity to receptors on human left ventricle and coronary artery (KDs = 0.26 and 0.11 nM, respectively), eliciting endothelium-independent vasoconstriction.3NMU-25 also suppresses glucose-stimulated insulin secretion in human islets, and this effect is lost in NMU R165W mutants, resulting in early-onset obesity.4 1.Mitchell, J.D., Maguire, J.J., and Davenport, A.P.Emerging pharmacology and physiology of neuromedin U and the structurally related peptide neuromedin SBritish Journal of Pharmacology15887-103(2009) 2.Greenwood, H.C., Bloom, S.R., and Murphy, K.G.Peptides and their potential role in the treatment of diabetes and obesityRev.Diabet.Stud.8(3)355-368(2011) 3.Mitchell, J.D., Maguire, J.J., Kuc, R.E., et al.Expression and vasoconstrictor function of anorexigenic peptides neuromedin U-25 and S in the human cardiovascular systemCardiovascular Research81353-361(2009) 4.Alfa, R.W., Park, S., Skelly, K.R., et al.Suppression of insulin production and secretion by a decretin hormoneCell Metabolism21(2)323-333(2015)
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Cannabidiolic acid
CBDA
T848371244-58-2
Cannabidiolic acid (CBDA), the predominant phytocannabinoid in fiber and seed-oil hemp (Cannabis sativa L.), exhibits a range of biological activities, including the inhibition of vomiting induced by toxins or motion sickness and the enhancement of 5-HT1A receptor activation in the rat brain stem membrane. It offers a more potent effect than cannabidiol in reducing emetic responses and delaying the onset of emesis in rats exposed to movement. Additionally, CBDA holds potential as an anti-inflammatory, anxiolytic, and antidepressant agent.
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