URB-597

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性 FAAH 抑制剂，IC50 为 4.6 nM；增加大鼠和野生型小鼠大脑中的大麻素水平（0.3 mg/kg ip）；通过抑制 CCH 模型中 mTOR 依赖性自噬来改善认知障碍。

A potent and selective FAAH inhibitor with IC50 of 4.6 nM; increases anandamide levels in the brain of rats and wild-type mice (0.3 mg/kg i.p.); improves cognitive impairment by inhibiting mTOR-dependent autophagy in a CCH model.Anxiety Preclinical(In Vivo):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.KDS-4103 is orally available in rats and cynomolgus monkeys.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.

URB-597 (KDS-4103) prevents the FAAH-catalyzed hydrolysis of [3H]anandamide by primary cultures of rat cortical neurons with an IC50 value of ~0.50 nM.

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. KDS-4103 is orally available in rats and cynomolgus monkeys.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. Animal Model:Wistar rats Dosage:250, 500, 750, 1000, 1250 mg/kg (Pharmacokinetic Analysis)Administration:Oral administration Result:Absorbed at a moderate rate with peak plasma concentrations (Cmax) achieved at 1.2 h after treatment. The oral elimination half-life was approximately 2 h.

URB597 | KDS-4103 | URB 597 | KDS 4103 | KDS4103

Metabolic Enzyme/Protease

FAAH

FAAH

Neurological Disease

Anxiety

546141-08-6

338.4003

C20H22N2O3

>98% (HPLC)

10 mM in DMSO

O=C(OC1=CC=CC(C2=CC=CC(C(N)=O)=C2)=C1)NC3CCCCC3

Carbamic acid, N-cyclohexyl-, 3'-(aminocarbonyl)[1,1'-biphenyl]-3-yl ester

(-20℃)

With Ice Pack

≥ 2 years