URB-597

SKU: orb1224725

Description

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.

Key Properties

• CAS Number: 546141-08-6
• MW: 338.4003
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₂N₂O₃
• SMILES: O=C(OC1=CC=CC(C2=CC=CC(C(N)=O)=C2)=C1)NC3CCCCC3
• Target: FAAH
• Solubility: 10 mM in DMSO

Bioactivity

• 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. 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.
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• In Vitro:
  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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

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

Quick Database Links

Gene Symbol

FAAH