prostacyclin receptor

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。

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。

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。

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。

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。

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-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid 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 is involved in the acylation of proteins to anchor membrane-bound proteins to the lipid bilayer.2,3,4,5,6 |1. Santos, M.J., López-Jurado, M., Llopis, J., et al. Influence of dietary supplementation with fish oil on plasma fatty acid composition in coronary heart disease patients. Ann. Nutr. Metab. 39(1), 52-62 (1995).|2. Lee, J.Y., Sohn, K.H., Rhee, S.H., et al. Saturated fatty acids, but not unsaturated fatty acids, induced the expression of cyclooxygenase-2 mediated through toll-like receptor 4. J. Biol. Chem. 276(20), 16683-16689 (2001).|3. Dietzen, D.J., Hastings, W.R., and Lublin, D.M. Caveolin is palmitoylated on multiple cysteine residues. Palmitoylation is not necessary for localization of caveolin to caveolae. J. Biol. Chem. 270(12), 6838-6842 (1995).|4. Robinson, L.J., and Michel, T. Mutagenesis of palmitoylation sites in endothelial nitric oxide synthase identifies a novel motif for dual acylation and subcellular targeting. Proc. Nat. Acad. Sci. USA 92(25), 11776-11780 (1995).|5. Topinka, J.R., and Bredt, D.S. N-terminal palmitoylation of PSD-95 regulates association with cell membranes and interaction with K+ channel Kv1.4. Neuron 20(1), 125-134 (1998).|6. Miggin, S.M., Lawler, O.A., and Kinsella, B.T. Palmitoylation of the human prostacyclin receptor. Functional implications of palmitoylation and isoprenylation. J. Biol. Chem. 278(9), 6947-6958 (2003).

Palmitic acid-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid-13C contains 13C at the C2 position and has been used in the study of free fatty acid incorporation into phospholipid fatty acids in soil microbes.1 Palmitic acid is a 16-carbon saturated fatty acid. It comprises approximately 25% of human total plasma lipids.2 It increases protein levels of COX-2 in RAW 264.7 cells when used at a concentration of 75 μM.3 Palmitic acid is involved in the acylation of proteins to anchor membrane-bound proteins to the lipid bilayer.3,4,5,6,7

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].

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。

Selexipag Active Metabolite-d7 是 Selexipag Active Metabolite 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 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。