Bimatoprost,155206-00-1

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YZ剂描述：

产品名称：Bimatoprost

产品别名：比马前列素

英文别名：AGN 192024

靶点：Prostaglandin Receptor

CAS：155206-00-1

纯度：＞98%

外观：白色或类白色粉末

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Bimatoprost is a prostaglandin analog used topically (as eye drops) to control the progression of glaucoma and in the management of ocular hypertension.

溶解性：DMSO : 34 mg/mL (81.8 mM)
Ethanol : 77 mg/mL (185.3 mM)

体外研究：

Bimatoprost mildly stimulates the rate of aqueous humor flow during the day (13%) and at night (14%), its ocular hypotensive action is due primarily to a 26% reduction in the tonographic resistance to outflow. Bimatoprost enhances the pressure-sensitive outflow pathway. Bimatoprost displaces prostaglandin F(2alpha) from FP receptors with K(i) of 6.31 μM. Bimatoprost rapidly mobilizes intracellular Ca(2+) via cloned human FP receptors expressed in human embryonic kidney cells and via native FP receptors in 3T3 mouse fibroblasts with EC(50) of 2.94 μM and 2.2 μM. Bimatoprost up-regulates Cyr61 mRNA expression in the cat iris. Bimatoprost-induced up-regulation of Cyr61 mRNA expression is not because of the activation of the prostaglandin FP receptor but a different receptor. Bimatoprost consistently evokes responses in different cells within the same tissue preparation, whereas prostaglandin F(2 alpha) and 17-phenyl prostaglandin F(2 alpha) elicites signaling responses in the same cells. Bimatoprost selectively stimulates intracellular calcium signaling in different cat iris sphincter cells.

体内研究：Bimatoprost is the ethyl amide derivative of 17-phenyl trinor PGF2α, a potent prostaglandin FP receptor agonist. Bimatoprost elicits an immediate, robust spike in that rapidly decayes back to baseline levels. Bimatoprost possess direct agonist activities at the rat, mouse, and human FP prostanoid receptor.

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