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.

Desfesoterodine (5-HMT) 是选择性毒蕈碱受体拮抗剂，Kb 和pA2分别为 0.84 nM 和 9.14。它可改善大鼠脑梗死诱导膀胱过度活动，是 Tolterodine 和 Fesoterodine 的主要药理活性代谢产物。

R715 TFA(185052-09-9 free base) 是强效和选择性缓激肽 B1 受体拮抗剂 (pA2 = 8.49)。它对B2 受体无活性。它减少神经性疼痛小鼠模型中的机械性过度伤害感受。它代谢稳定。

Adoprazine (SLV313) 是 5-HT 1A 受体的完全激动剂，其在 h5-HT1A 受体的 pEC50 为 9。Adoprazine 是 D2 和 D3 受体的完全拮抗剂，在 hD2 受体中的 pA2 值是 9.3，在 hD3 受体中的 pA2 值是 8.9。Adoprazine 具有非典型抗精神病的特征。

LE 300 是选择性多巴胺 D1 样受体拮抗剂，作用于人多巴胺 D1 和 D5 受体的Kis 分别为 1.9 nM 和 7.5 nM。在大鼠尾动脉实验中，它作用于5-HT2A 受体的pA2 为 8.32。

RS 17053 hydrochloride 是有效的、选择性的 α1A 肾上腺素受体 (α1A adrenoceptor) 拮抗剂。RS 17053 hydrochloride 在细胞膜中测得的 pKi 值为 9.1，功能分析的 pA2 值为 9.8。

PA22-2 (free acid) (Cys-Laminin A chain 2091-2108) 为促进神经突生长和神经元样过程形成的多肽。该化合物适用于人腺样囊性癌细胞培养和肽功能化磷脂双层制备^[3]。

PA22-2（IKVAV序列；层粘连蛋白A链片段）为一生物活性肽，源于小鼠层粘连蛋白a1氨基酸2110至2127残基。构成的细胞外基质能够促进神经突生长。

LPA2 antagonist 2 是一种具有选择性和高效性的 LPA2 拮抗剂（IC50：28.3 nM），具有潜在的抗癌活性，抑制 LPA3，可用于研究癌症。

gTPA2-OMe 是潜在的钙钛矿型太阳能电池（PSC）空穴传输层候选材料。

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

PPA24 (compound 19a) 作为一种PP2A激活剂，具有抑制诱导细胞凋亡和氧化应激的功能，同时能降低c-Myc的表达水平，因此被广泛用于抗癌研究领域。

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.

L-371,257 是催产素受体的竞争性拮抗剂，pA2 为 8.4，Ki 为 19 nM。 L-371,257 对加压素受体 1a 的 Ki 值为 3.7 nM。

JNJ-39758979是一种选择性的、高亲和力的、可口服的组胺 H4 受体拮抗剂，具有抗炎和止痒作用，对人、小鼠和猴子的组胺 H4 受体的 Ki 值分别为 12.5、5.3 和 25 nM。它对组胺诱导的 cAMP 抑制作用具有拮抗作用，pA2 为 7.9。

Aprocitentan (ACT-132577) 是一种 Macitentan 的主要活性代谢物。它是 ETA ETB 的双重拮抗剂，其 pA2值分别为 6.7 和 5.5，IC50分别为 3.4 nM 和 987 nM。

SNAP 94847 hydrochloride 是一种选择性黑色素浓缩激素受体1 拮抗剂，Ki 为 2.2 nM，具有抗抑郁样活性。它是 MCH 诱发的肌醇磷酸形成的高亲和力拮抗剂 ，pA2为 7.81。

[Nphe1]Nociceptin(1-13) NH2 TFA 是一种 Nociceptin/orphanin FQ (NC)内源性配体，是一种选择性和竞争性的 ociceptin receptor 拮抗剂，不具有激动剂活性。[Nphe1]nociceptin(1-13)NH2 选择性结合重组 nociceptin 受体(pKi=8.4)，拮抗 nociceptin 对 CHO 细胞中 cAMP 积累的抑制作用(pA2=6.0)。[Nphe1]Nociceptin(1-13)NH2 有可能作为一种止痛试剂。

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).

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).

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

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.

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).

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

Bryonolic acid (20-epi-Bryonolic acid) 是一种从 Sandoricum indicum 提取的三萜类化合物，具有免疫调节、抗炎，抗氧化和抗癌等活性，通过抑制Ca2+内流和调节Ca2+-CaMKII-CREB信号通路中的基因表达来避免PC12细胞免受NMDA诱导的细胞凋亡反应。

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).

Rp-Adenosine-5'-O-(1-thiotriphosphate)（Rp-ATP-α-S）是一种含硫核苷酸衍生物ATP-α-S的异构体，同时也是嘌呤P2Y1受体的激动剂。在表达人类P2Y1受体的HEK293细胞中，Rp-ATP-α-S能增加钙的动员（EC50 = 75 nM）。该化合物与洗涤的人类孤立血小板结合（Ki = 156 nM），抑制由ADP引发的人类富血小板血浆（PRP）的聚集（pA2 = 4.74），并且能够抑制前列腺素E1（PGE1）在人类孤立PRP中引发的cAMP产生（pA2 = 5.26）。同时，Rp-ATP-α-S还能引起用氨基甲酰胆碱预先缩紧的豚鼠结肠条带的松弛（EC50 = 56 nM）。此外，Rp-ATP-α-S已经被用于合成被细菌核糖开关识别的环状二核苷酸。

(D-Pro2,D-Trp6,8,Nle10)-Neurokinin B 是 Neurokinin B(Neurokinin Receptor) 的竞争性拮抗剂，pA2 为 5.5，对 Substance P 或 Neurokinin A 没有影响。

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

[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].

(d(CH2)51,Tyr(Me)2,Dab5,Arg8)-Vasopressin (d(CH2)5[Tyr(Me)2, Dab5]AVP)作为针对加压素受体V1a的特异性拮抗剂，具有pA2值为6.71。

JZP-361 是一种特异性 MAGL 抑制剂，对人重组 MAGL、人重组 FAAH 和人 hABHD6 的 IC50 分别为 46 nM、7.24 μM 和 1.79 μM。 JZP-361 具有抗组胺活性。 JZP-361可用于哮喘研究。

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).

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.

R 715是一种布拉迪肾上腺素B1受体拮抗剂。它抑制在表达布拉迪肾上腺素B1受体的孤立人类脐带中由布拉迪肾上腺素引发的收缩（pA2 = 8.49）。R 715（200、400及600 µg/kg）通过尾部闪烁测试减少了由链脲佐菌素（STZ）诱导的糖尿病神经病变小鼠模型中尾部撤回的潜伏期。它还在以髓磷脂少突胶质细胞糖蛋白（MOG）（35-55）（MOG35-55）抗原肽诱导的实验性自体免疫性脑炎（EAE）小鼠模型中，通过每天1 mg/kg的剂量减少了后肢无力和瘫痪的发病率，改善对称步态，并减少脊髓炎症灶点数、神经元脱髓鞘以及病灶单核细胞侵袭。R 715（0.01 nmol/动物，脑室内）能在自发性高血压大鼠中降低平均动脉血压并增加心率。

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

RXR antagonist 1 是类视黄醇 X 受体 (Retinoid X Receptor (RXR)) 调节剂，表现出较高的 RXR 拮抗作用 (pA2: 8.06)。RXR antagonist 1 能够用于研究 2 型糖尿病。

MRS2179 tetrasodium hydrate 是 P2Y1 受体的竞争性拮抗剂，能够作用于火鸡 P2Y1 受体 (Kb: 102 nM, pA2: 6.99)，对血小板聚集表现出抑制作用。MRS2179 tetrasodium hydrate 对 P2Y1 的选择性高于 P2X1 (IC50: 1.15 μM)、P2X3 (IC50: 12.9 μM)、P2X2、P2X4、P2Y2、P2Y4 和 P2Y6 受体。

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

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

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)

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

N-Despropyl Macitentan-d4 是 N-Despropyl Macitentan 的氘代化合物。N-Despropyl Macitentan 的 CAS 号为 1103522-45-7。Aprocitentan 是一种 Macitentan 的主要活性代谢物。它是ETA/ETB的双重拮抗剂，其pA2值分别为 6.7 和 5.5，IC50分别为 3.4 nM 和 987 nM。