tail

C13-112-tri-tail, a cationic lipid-like compound, features a polar amino alcohol head group, three hydrophobic 13-carbon tails, and a PEG2 linker, allowing for formulation into lipid nanoparticles (LNP).

C13-113-tetra tail, a cationic lipid-like compound, features a polar amino alcohol head group, a tertiary amine linker, and four hydrophobic carbon-13 tails. It can be formulated into a lipid nanoparticle (LNP).

Activated EG3 Tail facilitates the synthesis of exon-skipping oligomer conjugates that target specific sites within the human anti-muscular atrophy protein gene, promoting exon 51 skipping. This compound holds potential for research into muscular dystrophy treatments [1].

C13-112-tetra-tail, a cationic lipid-like compound, features a polar amino alcohol head group, four hydrophobic C13 tails, and a PEG2 linker, making it suitable for formulation into lipid nanoparticles (LNPs).

C13-113-tri tail, a cationic lipid-like compound, features a polar amino alcohol head group, three hydrophobic carbon-13 tails, and a tertiary amine linker. It is capable of being formulated into a lipid nanoparticle (LNP).

50-C2-C9-4tail is a chemical compound utilized in the creation of lipid nanoparticles (LNPs) for the efficient delivery of siRNA and mRNA, both in vitro and in vivo.

Amiodarone hydrochloride (Amiodarone HCl) is an antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. There is a resulting decrease in heart rate and in vascular resistance.

Antimicrobial Compound 1 is an alkyl pyridinium compound with Tail 12C, Head 4-carboxyl. Antimicrobial Compound 1 exhibits antimicrobial activities against B. subtilis and E. coli.

COH29 (RNR Inhibitor COH29) is an orally available, aromatically substituted thiazole and human ribonucleotide reductase (RNR) inhibitor with potential antineoplastic activity. COH29 binds to the ligand-binding pocket of the RNR M2 subunit (hRRM2) near the C-terminal tail, decreasing the pool of deoxyribonucleotide triphosphates needed for DNA synthesis, leading to cell cycle arrest and growth inhibition. It may also inhibit the nuclear enzyme poly (ADP-ribose) polymerase (PARP) 1, preventing DNA repair, causing accumulation of DNA breaks, and inducing apoptosis.

L-701324 is an NMDA receptor with high affinity and selectivity for the glycine site, used as an orally active and long-acting anticonvulsant.

Deltorphin II is a peptide agonist of δ2-opioid receptors.1,2It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (Kis = 0.0033, >1, and >1 μM, respectively) and induces [35S]GTPγS binding in mouse brain membrane preparations (EC50= 0.034 μM). Deltorphin II (0.12 mg/kg) decreases the infarction zone:risk zone ratio in a rat model of myocardial ischemia-reperfusion injury induced by coronary occlusion, an effect that can be reversed by the δ2-opioid receptor antagonist naltriben but not the δ1-opioid receptor antagonist BNTX.3Intrathecal administration of deltorphin II (15 μg/animal) increases latency to withdraw in the paw pressure and tail-flick tests in rats.4 1.Raynor, K., Kong, H., Chen, Y., et al.Pharmacological characterization of the cloned κ-, δ-, and μ-opioid receptorsMol. Pharm.45(2)330-334(1994) 2.Scherrer, G., Befort, K., Contet, C., et al.The delta agonists DPDPE and deltorphin II recruit predominantly mu receptors to produce thermal analgesia: A parallel study of mu, delta and combinatorial opioid receptor knockout miceEur. J. Neurosci.19(8)2239-2248(2004) 3.Maslov, L.N., Barzakh, E.I., Krylatov, A.V., et al.Opioid peptide deltorphin II simulates the cardioprotective effect of ischemic preconditioning: role of δ2-opioid receptors, protein kinase C, and KATP channelsBull. Exp. Biol. Med.149(5)591-593(2010) 4.Labuz, D., Toth, G., Machelska, H., et al.Antinociceptive effects of isoleucine derivatives of deltorphin I and deltorphin II in rat spinal cord: A search for selectivity of delta receptor subtypesNeuropeptides32(6)511-517(1998)

Rivanicline hemioxalate, also known as RJR-2403 hemioxalate or (E)-Metanicotine hemioxalate, is a chemical compound acting as a neuronal nicotinic receptor agonist with pronounced selectivity for the α4β2 receptor subtype, showing over 1,000-fold greater selectivity for this subtype (Ki=26 nM) compared to α7 receptors (Ki=3.6 μM). Its in vitro studies demonstrate no significant activation of nAChRs in PC12 cells, muscle type nAChRs, or muscarinic receptors at concentrations up to 1 mM. Furthermore, Rivanicline displayed less than one-tenth the potency of nicotine in inducing ileum contraction, with substantially lower efficacy, and failed to antagonize nicotine-induced stimulation of muscle or ganglionic nAChR functions, with an IC50 value greater than 1 mM. Chronic exposure to Rivanicline at 10 microM led to up-regulation of high-affinity nAChRs in M10 cells, mimicking effects observed with nicotine. In vivo studies revealed that Rivanicline significantly reversed scopolamine-induced amnesia and improved working and reference memory in a rat model, while being 15 to 30 times less potent than nicotine in affecting body temperature, respiration, and other physiological responses. Metanicitone’s potency was approximately five times lower than nicotine in tail-flick tests following subcutaneous administration, yet slightly more potent upon central administration.

Poly(A) polymerase enzymatically adds a polyadenosine tail of 20-200 adenine bases to the 3' end of RNA, a process that involves integrating ATP as AMP. This modification enhances RNA stability and augments mRNA translation efficiency in eukaryotic cells, evidencing the enzyme's high tailing efficiency [1] [2].

14-Pentadecenoic acid, a 15-carbon long-chain fatty acid with an alkene functional group on the terminal carbon of its aliphatic tail, has been observed to undergo oxidation due to the growth of M. cerificans at the expense of the parent alkene. This compound is utilized in the creation of fibrous scaffold biomaterials for tissue engineering purposes and in constructing metallomesogenic side-chain polymers for coating capillary columns in gas chromatography applications.

9A1P9, a multi-tail ionizable cationic phospholipid, facilitates membrane destabilization and is applicable for CRISPR-Cas9 gene editing in mice [1].

Hodgkinsine is a pyrrolidinoindoline alkaloid that has been found inP. colorataand has analgesic activity.1It increases latency to paw licking in the hot plate test and latency to tail withdrawal in the tail-flick test in mice when administered at a dose of 5 mg/kg. 1.Amador, T.A., Verotta, L., Nunes, D.S., et al.Antinociceptive profile of hodgkinsinePlanta Med.66(8)770-772(2000)

F9170, an antiviral peptide derived from the HIV-1 envelope glycoprotein (amino acids 789-803), targets the LLP1 domain in the virus's envelope protein cytoplasmic tail. This interaction inhibits HIV-1 IIIB infection in MT-2 cells, evidenced by an EC50 value of 0.19 µM. Additionally, at a dosage of 3 mg/kg, F9170 significantly lowers plasma viral load in rhesus macaques infected with simian HIV (SHIV).

Dihydropteroyl hexaglutamate is a link binding together sub-structures of the tail of Escherichia coli bacteriophage T4.

98N12-5, a novel multi-tail ionizable lipid, demonstrates efficient in vivo siRNA delivery to the liver.

Br-PBTC is a highly potent, 2/4 subtype-selective positive allosteric modulator of nicotinic acetylcholine receptors (nAChRs). It specifically targets α2β2, α2β4, α4β2, α4β4, (α4β2)2α4, and (α4β2)2β2 subtypes of nAChRs, with EC50 values ranging from 0.1 to 0.6 μM. Br-PBTC exerts its activity by binding to the c-tail region of an α subunit.

N(G)-Nitro-D-arginine methyl ester (D-NAME) is the less active enantiomer of the nitric oxide (NO) synthase inhibitor N(G)-nitro-L-arginine methyl ester . D-NAME was initially thought to be inactive and was often used as a negative control for L-NAME. Later studies showed that D-NAME (40 mg/kg/day in rats) can have similar but less pronounced effects as L-NAME (40 mg/kg/day in rats) in the cardiovascular system, particularly at long-term timepoints. D-NAME (3-10 µg/mouse) had no effect on nociception in mice assessed using the tail flick test.

Mambalgin 1 TFA, a selective inhibitor of ASIC1a (with IC50 values of 192 nM for human ASIC1a and 72 nM for the ASIC1a/1b dimer), preferentially binds to the channel in its closed/inactive state. It demonstrates selectivity for ASIC1a over a range of other channels, including ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2, and Kv1.2. In vivo, Mambalgin 1 TFA effectively prolongs the latency of the withdrawal response in mouse tail-flick and paw-flick tests.

SRA880 is a non-peptide antagonist of somatostatin sst1-receptor. SRA880 displayed significantly lower affinity for the other human recombinant somatostatin receptors ( pK(d) < or = 6.0). SRA880 shows a certain binding affinity to the human dopamine D4 re

Hodgkinsine B is an alkaloid and isomer of hodgkinsine that has analgesic activity.1It increases the latency to tail withdrawal in the tail-flick test in mice when administered at a dose of 10 mg/kg. 1.Kodanko, J.J., Hiebert, S., Peterson, E.A., et al.Synthesis of all low-energy stereoisomers of the tris(pyrrolidinoindoline) alkaloid hodgkinsine and preliminary assessment of their antinociceptive activityJ. Org. Chem.72(21)7909-7914(2007)

β-Endorphin (1-27) is an endogenous peptide that binds to μ-, δ-, and κ-opioid receptors (Kis = 5.31, 6.17, and 39.82 nM, respectively, in COS-1 cells expressing rat receptors). It binds to rat and mouse brain membrane preparations (IC50s = 1.1 and 5.7 nM, respectively) and induces chemotaxis of human monocytes in vitro when used at a concentration of 1 nM. Intracerebroventricular administration of β-endorphin (1-27) increases the latency to tail withdrawal in response to thermal stimulation in mice with a median antinociceptive dose (AD50) of 1,500 pmol per animal. It inhibits antinociception induced by β-endorphin in mice in response to thermal stimuli when administered at a dose of 65 pmol per animal. In rats, β-endorphin (1-27) does not affect drug-associated place preference when administered at doses up to 20 μg, i.c.v., but inhibits β-endorphin-induced place preference when administered at a dose of 10 μg per animal.

Z-VAE(OMe)-fmk is a cell-permeable and irreversible UCHL1 inhibitor. The inhibitor approaches the active-site cleft from the opposite side of the crossover loop as compared to the direction of approach of ubiquitin's C-terminal tail, thereby occupying the P1' (leaving group) site, a binding site perhaps used by the unknown C-terminal extension of ubiquitin in the actual in vivo substrate(s) of UCHL1.

Primordazine B is a selective inhibitor of primordial germ cell (PGC) development which targets poly(A)-tail-independent noncanonical translation (PAINT).

Mecamylamine hydrochloride (Mevasin) is a nicotinic antagonist, used as a ganglionic blocker in hypertension.

R 715, a bradykinin B1 receptor antagonist, inhibits contractions in isolated human umbilical cords that express bradykinin B1 receptors (pA2 = 8.49). When administered at doses of 200, 400, and 600 µg/kg, R 715 enhances latency to tail withdrawal in the tail-flick test for diabetic neuropathy mouse models induced by streptozotocin (STZ), signaling potential analgesic properties. Furthermore, at a 1 mg/kg per day dosage, it mitigates symptoms in a mouse model of experimental autoimmune encephalomyelitis (EAE) induced by MOG35-55 antigen peptide, such as reducing hind limb weakness and paralysis, improving gait symmetry, and decreasing spinal inflammation, neuron demyelination, and lesion monocyte invasion. Additionally, R 715 at 0.01 nmol/animal, administered intracerebroventricularly (i.c.v.), lowers mean arterial blood pressure and increases heart rate in spontaneously hypertensive rats, indicating cardiovascular effects.

Salvinorin A propionate is a selective partial agonist at κ1-opioid receptors (KOR) with a Ki value of 32.6 nM. It inhibits adenylate cyclase (EC50 = 4.7 nM) in HEK293 cells transfected with human KOR. It is selective for KORs over μ, δ, and ORL-1 opioid receptors and has no effect at serotonin, dopamine, muscarinic, or adrenergic receptors. In mice, salvinorin A propionate (13 μg, i.c.v.) reduces nociceptive responses in a radiant heat tail-flick assay, though not as potently as salvinorin A .

RAGE 229, N-(4-(7-cyano-4-(morpholin-4ylmethyl) quinolin-2-yl)phenyl)acetamide, is an orally active ctRAGE-DIAPH1 inhibitor. RAGE 229 can inhibit the intracellular RAGE signaling by inhibiting the interaction between the cytoplasmic tail of RAGE(ctRAGE) and Diaphanous-1(DIAPH1) [1].

SRA880 is a non-peptide somatostatin sst(1) receptor antagonist which displays a significantly lower affinity for the other human recombinant somatostatin receptors ( pK(d)= 6.0) or a wide range of neurotransmitter receptors, except for the human dopamine

UFP101 is a synthetic peptide that functions as an antagonist of the nociceptin receptor, demonstrating high affinity with a Ki of 0.06 nM in CHO cells expressing the human receptor. It exhibits selectivity for the nociceptin receptor over the κ-opioid receptor, with a Ki of 204 nM in CHO cells expressing the rat receptor. The compound effectively inhibits GTPγS release from the nociceptin receptor in CHO cell membranes, with an EC50 of 1.86 nM. When administered intracerebroventricularly at a dose of 10 nmol/animal, UFP101 prolongs the latency to tail withdrawal in the tail-flick test in mice, indicating its potential as an analgesic. Additionally, at doses of 0.003, 0.03, and 0.3 mg/kg, UFP101 enhances survival in a sepsis mouse model induced by cecal ligation and puncture, suggesting potential therapeutic applications in sepsis management.

Mitraciliatine, an alkaloid discovered in M. speciosa (Kratom in Thai), acts as a partial agonist for the μ-opioid receptor (MOR) and an agonist for the κ-opioid receptor (KOR), demonstrating selectivity for these receptors over the δ-opioid receptor (DOR) with EC50 values of 228, 218, and >1,000 nM respectively in mouse receptors through a GTPγS binding assay. When administered intracerebroventricularly (i.c.v.) at 100 nmol/animal, mitraciliatine increases latency to withdrawal in the warm water tail withdrawal assay in mice, an effect reversable by MOR knockout but unaffected by KOR knockout, distinguishing it from morphine by not causing hyperlocomotion or respiratory depression.

JWH 030 is a potent naphthoyl pyrrole cannabimimetic, exhibiting higher affinity for the CB1 receptor (EC50= 30.5 nM in rats, Ki= 87 nM in mice) compared to CB2 (EC50= 552 nM in human CB2 receptors). The compound demonstrates significant in vivo potency in mouse models, specifically in spontaneous activity and tail flick assays (antinociception) with an ED50 value of 26.8 μM/kg. Furthermore, JWH 030 dose-dependently reduces electrically-induced contractions in the mouse vas deferens, with an IC50 of 3.38 nM, highlighting its effective modulatory effects. This compound is designated for forensic or research applications.

DB293 is an inhibitor of PIT-1 and BRN-3 transcription factors. DB293 binds as head-to-tail stacked dimers in the minor groove of 5'-ATGA sequence, thereby leading to an increase in the size of minor groove.

τ-Fluvalinate is a pyrethroid acaricide.1It induces tail currents in Western honeybee (A. mellifera) voltage-gated sodium channels (AmNav1) expressed inXenopusoocytes (EC50= 60 nM). It also induces tail currents in honeybee parasitic Varroa mite (V. destructor) Nav1 channels (VdNav1) expressed inXenopusoocytes (EC50= 160 nM) with a faster tail current decay than that of AmNav1 channels. Topical application of τ-fluvalinate (2 μl) in combination with coumaphos , atrazine , 2,4-DMPF, chlorpyrifos , and chlorothalonil does not affect honeybee queen mass, egg-laying patterns, or the mass of daughter worker bees at emergence.2Formulations containing τ-fluvalinate have been used to control Varroa mites in beehives. 1.Gosselin-Badaroudine, P., and Chahine, M.Biophysical characterization of the Varroa destructor NaV1 sodium channel and its affinity for τ-fluvalinate insecticideFASEB J.31(7)3066-3071(2017) 2.McAfee, A.Honey bee queen health is unaffected by contact exposure to pesticides commonly found in beeswaxSci. Rep.11(1)15151(2021)

Selective ASIC1a inhibitor (IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Binds to closed/inactive channel. Selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Increases late