prostacyclin receptor

Girinimbine (Girinimbin) 是一种来自植物九里香、 M. koenigii和Murraya koenigii中分离出的咔唑类生物碱。Girinimbine 具有多种生物学作用，可诱导细胞凋亡 (apoptosis)，具有抗锥虫、抗血小板活性、抗菌活性、抗炎、抗氧化和抗肿瘤活性。

BAY 73-1449 是前列环素受体选择性拮抗剂，在人 HEL 细胞和大鼠 DRG 的 cAMP 分析中具有很高的效价，IC50小于 0.1 nM。BAY 73-1449在降血压方面有研究的价值。

Selexipag (ACT-293987) 是前列环素受体激动剂，可引起肺血管舒张，用于治疗肺动脉高压。

RO1138452 (CAY10441) 是一种选择性和可口服的前列环素受体拮抗剂，pKi 为8.3。它拮抗卡前列环素诱导的人神经母细胞瘤腺苷酸环化酶的激活，以剂量依赖性方式阻断环 AMP 积累，具有镇痛活性。

Ralinepag (APD811) 是一种可口服的非前列腺素前列环素 (IP) 受体激动剂，对人和大鼠 IP 受体以及人 DP1 受体的 EC50 分别为 8.5、530 和 850 nM。

BMY 45778 是一种有效的非前列腺素样前列腺素部分激动剂，对人、兔、鼠血小板聚集有抑制作用，IC50 分别为 35 nM、136 nM和1.3μm。BMY 45778 通过刺激前列环素受体起作用。

Prednicarbate (Hoe 777) 是一种外用皮质类固醇。Prednicarbate 可用于炎症性皮肤病的研究，如特应性皮炎。

RO3244794是一种具有选择性的前列环素 （IP）受体拮抗剂，可用于研究肝脏损伤。

Carbacyclin, a PGI2 analog, is a prostacyclin (PGI2) receptor agonist and vasodilator with potent inhibitory platelet aggregation.

Taprostene sodium 是一种部分激动prostacyclin (IP)受体的前列腺素类化合物。它能够与Prostaglandin E2 (PGE2)、ONO-AE1-259 (选择性 EP2 激动剂)及乙酰胆碱相互作用，并显示出显著的心脏保护作用。

Carbaprostacyclin-biotin (cPGI-biotin;Carbacyclin-biotin) 是Carbacyclin (Carbaprostacyclin) 与生物素结合的化合物。Carbacyclin 是 PGI2 的类似物，作为前列环素 (PGI2) 受体激动剂和血管扩张剂，能够有效抑制血小板聚集。

AFP-07 is a highly selective and potent agonist. It was used for the prostacyclin receptor.

TEI-9063 is a stable and highly specific prostacyclin analogue of prostacyclin receptor in mast cell tumor p-815 cells.

Palmitic acid-1-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid (T2908) is a 16-carbon saturated fatty acid. It comprises approximately 25% of human total plasma lipids.1 It increases protein levels of COX-2 in RAW 264.7 cells when used at a concentration of 75 μM.2 Palmitic acid (T2908) is involved in the acylation of proteins to anchor membrane-bound proteins to the lipid bilayer.2,3,4,5,6

Prostaglandin F1α(PGF1α)是一种脂质介质和prostacyclin的内源性代谢物，主要由DGLA经过COX途径代谢生成，能够剂量依赖性地调节平滑肌收缩。

Selective prostacyclin IP receptor antagonist (pKi = 8.3). Exhibits no affinity at other prostanoid receptors (EP1-4, FP and TP) in a radioligand binding assay. Demonstrates analgesic activity in rats. Orally bioavailable. Clark et al (2004) Discovery and SAR development of 2-(phenylamino) imidazolines as prostacyclin receptor antagonists. Bioorg.Med.Chem.Lett. 14 1053 PMID:15013022 |Jones et al (2006) Investigation of the prostacyclin (IP) receptor antagonist RO1138452 on isolated blood vessel and platelet preparations. Br.J.Pharmacol. 149 110 PMID:16880763 |Bley et al (2006) RO1138452 and RO3244794: characterization of structurally distinct, potent and selective IP (prostacyclin) receptor antagonists. Br.J.Pharmacol. 147 335 PMID:16331286

MRE-269 (ACT-333679) 是一种口服的长效前列环素受体激动剂前药，是 Selexipag 的活性代谢物，用于治疗肺动脉高压。

Cicaprost (ZK 96480) is a prostacyclin receptor (IP) agonist, which induces relaxation of the artery via concentration-dependent mechanisms. Its EC50 value, determined to be 5.8 nM [1], further highlights its potency.

Cefminox (Sodium) is a new cephamycin antibiotic possessing a D-amino acid moiety derived from D-cysteine at the C-7B side chain. Cefminox is active against a wide range of bacteria, especially Gram-negative and anaerobic bacteria. Cefminox shows excellent in vivo efficacy (ED50) which is higher than would be expected from its in vitro activity (MIC). Moreover, cefminox possesses more potent activity in suppression of bacterial regrowth than other cephems[1]. Cefminox (Sodium) was the most active beta-lactam, with an MIC at which 50% of isolates are inhibited (MIC50) of 1.0 microg/ml and an MIC90 of 16.0 microg/ml. Cefminox was especially active against Bacteroides fragilis (MIC90, 2.0 microg/ml), Bacteroides thetaiotaomicron (MIC90, 4.0 microg/ml), fusobacteria (MIC90, 1.0 microg/ml), peptostreptococci (MIC90, 2.0 microg/ml), and clostridia, including Clostridium difficile (MIC90, 2.0 microg/ml)[2]. The use of a single preoperative dose of cefminox was similar in efficacy to 3 doses of cefoxitin administered every 4 hours, and that the serum and tissue concentrations attained provide adequate antibiotic coverage[3]. Moreover, cefminox as a dual agonist of IP (Prostacyclin receptor) and PPARγ (peroxisome proliferator-activated receptor-gamma) that significantly inhibits PASMC proliferation by up-regulation of PTEN (phosphatase and tensin homolog) and cAMP ( cyclic adenosine monophosphate), suggesting that it has potential for treatment of PAH(pulmonary arterial hypertension)[4].

Selexipag Active Metabolite-D7是Selexipag Active Metabolite (T3S2007)的氘代化合物。Selexipag Active Metabolite的CAS号为475085-57-5。MRE269是一种口服的长效前列环素受体激动剂前药，是Selexipag 的活性代谢物，用于治疗肺动脉高压。

Selexipag-D7是Selexipag (T3216)的氘代化合物。Selexipag的CAS号为475086-01-2。Selexipag是前列环素受体激动剂，可引起肺血管舒张，用于治疗肺动脉高压。

Prednicarbate (Standard) 是 Prednicarbate 的标准品，适用于定量分析、质量控制及生化实验等相关研究。Prednicarbate (Hoe 777) 是一种外用皮质类固醇。Prednicarbate 可用于炎症性皮肤病的研究，如特应性皮炎。