L-902688

立即咨询

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。

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，K_i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 aK_iof 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