prostacyclin

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。

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。

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。

5-cis Carbaprostacyclin is a stable analog of PGI2 and an isomer of carbaprostacyclin. It is a weak inhibitor of human platelet aggregation with an IC50 of 2.8 μM compared to 0.3 μM for carbaprostacyclin. 5-cis Carbaprostacyclin is a much weaker effector of rabbit mesenteric artery relaxation with an EC50 of 104 μM compared to 5.9 μM for carbaprostacyclin. It even antagonizes the adenylate cyclase activation induced by carbaprostacyclin.

13,14-dehydro-15-cyclohexyl Carbaprostacyclin is a chemically stable analog of PGI2. It inhibits the ADP-induced aggregation of human platelets with an ED50 of about 40 nM in PRP and 77 nM in washed platelets, which is comparable to the potency of carbaprostacyclin.

2-Acetylbenzoic acid 在抑制血小板功能和血小板前列腺素 (PG) 合成方面比 2-丙酰氧基苯甲酸更有效，尽管这些药物在抑制前列环素 (PGI2) 合成方面的效力相当。

Bradykinin 是由激肽释放酶-激肽系统产生的活性肽。 它是炎症调节因子和神经调节因子，对几种血管和肾功能也有调节作用。

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。

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

Epoprostenol sodium (Prostaglandin I2 sodium salt) 是短效血管稀释剂，是一种合成前列环素，可用于研究肺动脉高压和充血性心力衰竭。

Tilsuprost为稳定的前列环素类似物，属于亚氨基前列环素衍生物，具有有效的细胞保护作用。

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.

OP-2507, a prostacyclin agonist, is used potentially for the treatment of hepatic insufficiency and hypertension.

Beraprost is a stable prostacyclin analog.

Nafazatrom is a pyrazolinone derivative and lipoxygenase inhibitor that increases endogenous prostacyclin (PGI2) and has experimental anticancer activity. Nafazatrom is also an antithrombotic drug that increases prostacyclin levels and reduces the inciden

RS-93427-007 is an orally active stable mimetic agent of prostacyclin for the study of mechanisms of atherogenesis.

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

Iloprost is a second generation structural analog of prostacyclin (PGI2) with about ten-fold greater potency than the first generation stable analogs, typified by carbaprostacyclin. Iloprost binds with equal affinity to the recombinant human IP and EP1 receptors with a Ki value of 11 nM. Most preparations of iloprost contain 16(S) and 16(R) stereoisomers. 16(R)-Iloprost inhibits platelet aggregation with an IC50 value of 65 nM.

Iloprost is a second generation structural analog of prostacyclin (PGI2) with about ten-fold greater potency than the first generation stable analogs, typified by carbaprostacyclin. Iloprost binds with equal affinity to the recombinant human IP and EP1 receptors with a Ki value of 11 nM. Most preparations of iloprost contain 16(S) and 16(R) stereoisomers. 16(S)-Iloprost potently inhibits platelet aggregation with an IC50 value of 3.5 nM.