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L-902688
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
L-902688图片
CAS NO:634193-54-7
包装:1mg (11.92 mM * 200 μL in Methanol)
市场价:9500元

产品介绍
L-902688 是一种有效的,选择性的,口服活性的EP4受体激动剂,Ki为 0.38 nM,EC50为 0.6 nM。L-902688 对EP4的选择性是其他 EP 和类前列腺素受体的 4,000 倍以上。
生物活性

L-902688 is a potent, selective and orally activeEP4 receptoragonist with aKiof 0.38 nM and anEC50of 0.6 nM. L-902688 shows >4,000-fold selective forEP4over otherEPand prostanoid receptors[1][2].

IC50& Target[2]

EP4

0.38 nM (Ki)

EP4

0.6 nM (EC50)

体外研究
(In Vitro)

L-902688 (1 μM; 24 hours; HUVE cells) treatment attenuates TGF-β-induced Twist and α-smooth muscle actin (α-SMA) expression[1].

Western Blot Analysis[1]

Cell Line:Human umbilical vein endothelial cells (HUVECs)
Concentration:1 μM
Incubation Time:24 hours
Result:Attenuated TGF-β-induced Twist and α-smooth muscle actin (α-SMA) expression.
体内研究
(In Vivo)

L-902688 (0.25-1 μg/kg/day; intraperitoneal injection; daily; for 3 weeks; adult male Sprague-Dawley rats) treatment reduces right ventricle fibrosis in the monocrotaline (MCT)-induced PAH rat model[1].

Animal Model:Adult male Sprague-Dawley rats injected with crotaline to induce pulmonary arterial hypertension (PAH) and right ventricular (RV) hypertrophy[1]
Dosage:0.25 μg/kg/day, 0.4 μg/kg/day or 1 μg/kg/day
Administration:Intraperitoneal injection; daily; for 3 weeks
Result:Reduced right ventricle fibrosis in the monocrotaline (MCT)-induced PAH rat model.
分子量

419.47

性状

Liquid

Formula

C21H27F2N5O2

CAS 号

634193-54-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Solution, -20°C, 2 years