GW-803430

SKU: orb2901605

Description

GW-803430 (GW-3430) is a potent and selective melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pIC50 of 9.3. GW-803430 is orally active in an animal model of obesity.

Key Properties

• CAS Number: 515141-51-2
• MW: 481.99
• Purity: >98% (HPLC)
• Formula: C₂₅H₂₄ClN₃O₃S
• SMILES: O=C1C=2SC(=CC2N=CN1C3=CC=C(OCCN4CCCC4)C(OC)=C3)C=5C=CC(Cl)=CC5
• Target: MCHR

Bioactivity

• In Vivo:
  GW-803430 (0.3, 3, and 15 mg/kg; oral administration; once daily) causes a sustained dose-dependent weight loss relative to vehicle controls. GW-803430 is a suitable compound for its good pharmacokinetic properties (bioavailability = 31%, t1/2 = 11 h) and brain penetration (6: 1 brain: plasma concentration) in mice. Animal model: High fat diet-induced obese AKR/J mice. Dosage: 0.3, 3, and 15 mg/kg. Administration: Orally, qd, 12 days. Result: Caused a sustained dose-dependent weight loss of-6.2%,-12.1%, and-13.1%, respectively, relative to vehicle controls.
• In Vitro:
  GW-803430 demonstrates a potent antagonist activity towards MCH induced MCHR1 receptor with an IC50 value of ~13 nM.

Storage & Handling

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

Quick Database Links

Gene Symbol

MCHR