pa2

1-Palmitoyl-2-oleoyl-sn-glycero-3-PA (1,2-POPA) is a phospholipid featuring a palmitic acid (16:0) chain that is saturated and an oleic acid (18:1) chain that is monounsaturated, positioned at the sn-1 and sn-2 locations, respectively. This compound is utilized in creating micelles, liposomes, and various artificial membrane forms.

2-Pmp-PA is a taste modulator that inhibits sweetness.

1-Palmitoyl-d9-2-hydroxy-sn-glycero-3-PA (1-palmitoyl-d9LPA) serves as an internal standard for the quantification of 1-palmitoyl LPA using GC- or LC-MS. This compound, an analog of LPA with palmitic acid at the sn-1 position, activates reporter gene expression in PC12 cells fitted with human lysophosphatidic acid receptor 4 (LPA4) at 0.01 to 10 µM concentrations. Additionally, 1-palmitoyl LPA prompts aggregation in isolated human platelets within the 12-300 µM range, a process reversible by prostaglandin E1 (PGE1), theophylline, or EDTA. It also interacts with calcium and magnesium to boost the efficacy of ampicillin, piperacillin, and ceftazidime against P. aeruginosa strains from cystic fibrosis patients.

dopamine D1 receptor antagonist

RS 17053 hydrochloride is a potent and selective antagonist of α1A adrenoceptor. RS 17053 hydrochloride exhibits a pKi value of 9.1 in native cell membrane and a pA2 value of 9.8 in functional assays.

PA22-2 (free acid) (Cys-Laminin A chain 2091-2108), a peptide, promotes neurite outgrowth and facilitates the formation of neuron-like processes. It is utilized in the culturing of human adenoid cystic carcinoma cells and the development of peptide-functionalized supported phospholipid bilayers [1] [2] [3].

PA22-2, an active biological peptide featuring the IKVAV sequence from the laminin A-chain fragment, is derived from mouse laminin alpha1 amino acid residues 2110-2127. Substrates composed of PA22-2 have been shown to facilitate neurite outgrowth.

R715 TFA(185052-09-9 free base) is a potent and selective bradykinin B1 receptor antagonist (pA2 = 8.49). Displays no activity at B2 receptors. Reduces mechanical hypernociception in a mouse model of neuropathic pain. Metabolically stable.

Adoprazine (SLV313) is a potential atypical antipsychotic bearing potent D2 receptor antagonist and 5-HT1A receptor agonist properties.

LPA2 antagonist 2 is ＞480-fold more selective than LPA3 (IC50 of 13.85 μM).LPA2 antagonist 2 is a selective LPA2 antagonist with an IC50 of 28.3 nM and a Ki of 21.1 nM.

gTPA2-OMe is a potential hole transport layer candidate for perovskite solar cells (PSCs).

LPA2 antagonist 1 is an LPA2 antagonist (IC50: 17 nM).

Metipranolol (Betamann) is a type of β- Adrenergic receptors（ β- A potent antagonist of adrenergic receptor on guinea pig atria β 1- Adrenergic receptors and rat uterus β The 2-adrenergic receptor exhibited the beta blocking potentials (pA2) of 8.3 and 8.4, respectively. It is also a potent substituent in the 3H DHA binding assay, with a ligand concentration of 0.7 nM and a Ki of 39 ± 24 nM.

Potent neuropeptide Y (NPY) Y1 receptor antagonist (pA2 = 10 and 10.5 at rY1 and hY1, receptors respectively). Also a potent and selective NPY Y4 receptor agonist (pEC50 values are 6.0, 8.6 and 6.1 for rY2, hY4 and rY5 receptors respectively). Suppresses

Potent, selective and competitive corticotropin-releasing factor CRF2 receptor antagonist (Kd values are 1.4 and 153.6 nM for binding to mouse CRF2β and rat CRF1 receptors respectively). Inhibits sauvagine-stimulated cAMP accumulation in HEK-mCRF2β cells

l-Stephanine is a potent and highly selective alpha 1 adrenoceptor blocker, inhibits anococcygeus muscle contraction induced by phenylephrine with pA2 values of 6.76. Stephanine shows significant antiplasmodial activities with IC(50) ranged from 1.2 uM to 52.3 uM. Stephanine and crebanine have high inhibitory activity against gram-positive animal pathogenic bacteria, with MIC values of 0.078-0.312g/l, but low inhibitory activity against gram-negative animal pathogenic bacteria, they also inhibit hyphal growth of the plant pathogens Cercospora kaki.

Akuammigine has in vitro antimalarial activity. Akuammigine competitively antagonizes the effect of noradrenaline on postsynaptic alpha-adrenoceptors, yielding pA2 values of 4.68. Akuammidine also shows a preference for mu-opioid binding sites with Ki val

Tipelukast (KCA 757) is a novel orally available leukotriene receptor antagonist with anti-inflammatory activity that reduces fibrosis and down-regulates TIMP-1, type 1 collagen.Tipelukast is used in the study of asthma.

rac-7-hydroxy Propranolol (hydrochloride) is a ring-hydroxylated isomer and metabolite of propranolol that is an antagonist at β-adrenergic receptors (0.95 potency relative to propranolol). It also demonstrates potent vasodilator activity (0.20 potency relative to propranolol; pA2 = 7.58).

[Nphe1]Nociceptin(1-13)NH2 is a novel endogenous ligand for the nociceptin/orphanin FQ (NC) receptor, acting as a selective and competitive antagonist without any agonist effects. It binds specifically to recombinant nociceptin receptors with high affinity (pKi=8.4) and effectively blocks nociceptin's ability to inhibit cyclic AMP accumulation in CHO cells (pA2=6.0), showcasing potential as an analgesic agent.

Delequamine HCl is a potent and selective alpha 2-adrenoceptor antagonist. Delequamine HCl has a pKi of 9.45 for alpha 2-adrenoceptors in the rat cortex (pA2 in the guinea-pig ileum of 9.72).

Rp-Adenosine-5'-O-(1-thiotriphosphate) (Rp-ATP-α-S), a sulfur-containing nucleotide derivative isomer and a purinergic P2Y1 receptor agonist, promotes calcium mobilization in HEK293 cells expressing the human P2Y1 receptor (EC50 = 75 nM). This compound exhibits binding affinity to washed isolated human platelets (Ki = 156 nM) and attenuates ADP-induced aggregation in human platelet-rich plasma (PRP; pA2 = 4.74), as well as inhibits cAMP production triggered by prostaglandin E1 (PGE1) in human PRP (pA2 = 5.26). Furthermore, it triggers relaxation in carbamoylcholine-constricted guinea pig taenia coli strips (EC50 = 56 nM). Rp-ATP-α-S also contributes to the synthesis of cyclic dinucleotides, recognized by bacterial riboswitches.

ADL 08-0011 is an active metabolite of the μ-opioid receptor antagonist alvimopan. It is produced from alvimopan via amide hydrolysis by gut microbiota. ADL 08-0011 is a μ-opioid receptor antagonist (Ki = 0.25 nM). It is selective for μ-opioid receptors over κ- and δ-opioid receptors (Kis = 15.8 and 31.6 nM, respectively). ADL 08-0011 inhibits endomorphin 1-induced inhibition of electrically induced contraction of isolated guinea pig ileum (pA2 = 9.4). In vivo, ADL 08-0011 (0.03-1 mg/kg) reverses loperamide-induced delayed gastric emptying in a rat model of castor oil-induced diarrhea.

Rupatadine (UR-12592) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig cerebellum membranes).IC50 value:Target: PAF/H1 antagonistin vitro: Rupatadine competitively inhibited histamine-induced guinea pig ileum contraction (pA2 = 9.29 +/- 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). It also competitively inhibited PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2 = 6.68 +/- 0.08) and in human platelet-rich plasma (HPRP) (IC50 = 0.68 microM), while not affecting ADP- or arachidonic acid-induced platelet aggregation [1]. The IC50 for rupatadine in A23187, concanavalin A and anti-IgE induced histamine release was 0.7+/-0.4 microM, 3.2+/-0.7 microM and 1.5+/-0.4 microM, respectively whereas for loratadine the IC50 was 2.1+/-0.9 microM, 4.0+/-1.3 M and 1.7+/-0.5 microM. SR-27417A exhibited no inhibitory effect [2].in vivo: Rupatadine blocked histamine- and PAF-induced effects in vivo, such as hypotension in rats (ID50 = 1.4 and 0.44 mg/kg i.v., respectively) and bronchoconstriction in guinea pigs (ID50 = 113 and 9.6 micrograms/kg i.v.). Moreover, it potently inhibited PAF-induced mortality in mice (ID50 = 0.31 and 3.0 mg/kg i.v. and p.o., respectively) and endotoxin-induced mortality in mice and rats (ID50 = 1.6 and 0.66 mg/kg i.v.) [1]. rupatadine treatment improved the declined lung function and significantly decreased animal death. Moreover, rupatadine was able not only to attenuate silica-induced silicosis but also to produce a superior therapeutic efficacy compared to pirfenidone, histamine H1 antagonist loratadine, or PAF antagonist CV-3988 [3]. [1]. Merlos M, et al. Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF). J Pharmacol Exp Ther. 1997 Jan;280(1):114-21. [2]. Queralt M, et al. In vitro inhibitory effect of rupatadine on histamine and TNF-alpha release from dispersed canine skin mast cells and the human mast cell line HMC-1. Inflamm Res. 2000 Jul;49(7):355-60. [3]. Lv XX, et al. Rupatadine protects against pulmonary fibrosis by attenuating PAF-mediated senescence in rodents. PLoS One. 2013 Jul 15;8(7):e68631.

JNJ-39758979 is a selective and high-affinity histamine H4 receptor antagonist (Kis: 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively). JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2

MRS2179 is a competitive P2Y1 receptor antagonist (Kb = 100 nM) with no appreciable activity at P2Y2, P2Y4, or P2Y6 at concentrations up to 30 µM, or at P2Y12 and P2Y13. It inhibits ADP-induced platelet shape change and aggregation (pA2 = 6.55) in vitro a

DHP-218 is a calcium channel antagonist. DHP-218 inhibits Calcium-induced contraction of the rat aorta in high K+ solution with the pA2 value of 9.11. The IC50 value for the inhibitory effects of DHP-218 in high K+-induced and phenylephrine-induced contra

Tezosentan is an antagonist of the endothelin receptor (pA2s: 9.5, 7.7 for ETA and ETB receptors, respectively).

Aprocitentan D4 (ACT-132577 D4) is a deuterium-labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is a dual ETA/ETB antagonist (IC50s: 3.4 nM and 987 nM; pA2s: 6.7 and 5.5).

Bryonolic acid (20-epi-Bryonolic acid), a triterpenoid extracted from Sandoricum indicum, possesses immunomodulatory, anti-inflammatory, antioxidant and anticancer activities and protects PC12 cells from NMDA-induced apoptosis by inhibiting Ca2+ in-flux and modulating gene expression in the Ca2+-CaMKII-CREB signalling pathway.

Aprocitentan (ACT-132577) is ETA and ETB antagonist .

SUN-C5174 is a sleective 5-HT2 antagonist (pA2=8.98+/-0.06). SUN C5174 showed a marked inhibitory effect on the platelet aggregation induced by serotonin in combination with collagen and adenosine diphosphate (ADP) in canine or human platelet-rich plasma

L-371,257 is a competitive antagonist of oxytocin receptor with pA2 of 8.4 and Ki of 19 nM. L-371,257 shows a Ki of 3.7 nM for vasopressin receptor 1a.

(D-Pro2,D-Trp6,8,Nle10)-Neurokinin B functions as a competitive antagonist to the Neurokinin B receptor, exhibiting a pA2 value of 5.5. Notably, it does not affect Substance P or Neurokinin A [1].

(d(CH2)5[Tyr(Me)2, Dab5]AVP), a vasopressin V1a receptor-specific antagonist, demonstrates a pA2 value of 6.71 [1].

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.

[Des-His1,Glu9]-Glucagon amide TFA is a potent peptide antagonist targeting the glucagon receptor, featuring a pA2 value of 7.2. It holds potential utility in diabetes pathogenesis research[1].

JZP-361 is a specific MAGL inhibitor with IC50s of 46 nM, 7.24 μM, and 1.79 μM for human recombinant MAGL, human recombinant FAAH, and human hABHD6. JZP-361 displays anti-histaminergic activities. JZP-361 can be used in studies about asthma.

Chir 2279 is a N-(substituted)glycine peptoid trimer with high-affinity binding for alpha 1-adrenoceptors. CHIR 2279 antagonized the epinephrine-induced increase in intraurethal pressure (pseudo pA2, 6.86) in dogs.

Beperidium iodide is a competitive antagonist of the acetylcholine receptor (pA2: 7.93).

Desfesoterodine (5-HMT) is a new muscarinic receptor antagonist with Kb of 0.84 nM.

YM158 free base is a potent and selective antagonist of TXA2 and LTD4 receptor (pA2s: about 8.81 and 8.87).

Glucagon receptor antagonist (pA2 = 7.2 for inhibition of glucagon-induced adenylyl cyclase activation in rat liver membranes); displays no agonist activity. Enhances glucose-stimulated pancreatic insulin release in vitro. Blocks added glucagon-induced hy

RXR antagonist 1 is a Retinoid X Receptor (RXR) modulator that exhibits high RXR antagonism (pA2: 8.06). RXR antagonist 1 can be used to study type 2 diabetes.

Potent agonist of the nociceptin (ORL1) receptor, demonstrated both in vitro and in vivo. Selective, competitive antagonism at the nociceptin receptor has also been reported (pA2 = 7.02 and 6.75 in the guinea pig ileum and mouse vas deferens respectively)

Tiotidine is a selective histamine H2-receptor antagonist (pA2=7.3-7.8 for guinea-pig right atrium).

MRS2179 tetrasodium hydrate, a competitive antagonist of the P2Y1 receptor, acts on the turkey P2Y1 receptor (Kb: 102 nM, pA2: 6.99) and exhibits an inhibitory effect on platelet aggregation. IC50: 1.15 μM), P2X3 (IC50: 12.9 μM), P2X2, P2X4, P2Y2, P2Y4 and P2Y6 receptors.

SNAP 94847 hydrochloride is a melanin-concentrating hormonereceptor1 (MCHR1) antagonist(Ki= 2.2 nM)

N-Despropyl Macitentan-d4 is a deuterated compound of N-Despropyl Macitentan. N-Despropyl Macitentan has a CAS number of 1103522-45-7. Aprocitentan is ETA and ETB antagonist .