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抑制剂/激活剂

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凋亡与自噬

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URB597

URB597 (KDS-4103)是一种口服生物有效的FAAH抑制剂，IC50为4.6 nM，对其他大麻黄素相关靶点没有抑制活性。Phase 1。

货号：
TK0464
规格：

1mg

5mg

10mg

25mg
价格：
￥0.00

产品参数

CAS No.	546141-08-6
生物活性	URB-597 (KDS-4103) is an orally bioavailable and selective FAAH inhibitor. URB-597 inhibits FAAH activity with an IC50s of approximately 5 nM in rat brain membranes, 0.5 nM in intact rat neurons, 3 nM in human liver microsomes. Antidepressant-like effects. Analgesic activity.
分子式	C20H22N2O3
分子量	338.4
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder, -20°C ,3 years
溶解性数据	DMSO : ≥ 100 mg/mL (295.51 mM),H2O : 0.1 mg/mL (0.30 mM; ultrasonic and warming and heat to 50°C)
体内研究	URB-597 (KDS-4103) inhibits rat brain FAAH activity after intraperitoneal (i.p.) administration with a median inhibitory dose (ID50) of 0.15 mg/kg in wild-type mice (+/+) or FAAH-null mice (-/-).KDS-4103 (0.1-0.3 mg/kg, i.p.) elicits significant, anxiolytic-like, antidepressant-like and analgesic effects, which are prevented by treatment with CB1 receptor antagonists in rats and mice.URB-597 inhibits FAAH in the brain rapidly (1 h), sustains at >90% through 12 h and >60% through 24 h after an oral dose of 10 mg/kg.
体外研究	URB-597 (KDS-4103) prevents the FAAH-catalyzed hydrolysis of [H]anandamide by primary cultures of rat cortical neurons with an IC50 value of ~0.50 nM.
纯度及产品资料	98%

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