1. GPCR/G Protein
    Neuronal Signaling
  2. MCHR1 (GPR24)
  3. GW-803430

GW-803430 (Synonyms: GW-3430)

Cat. No.: HY-11083 Purity: 98.06%
Handling Instructions

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.

For research use only. We do not sell to patients.

GW-803430 Chemical Structure

GW-803430 Chemical Structure

CAS No. : 515141-51-2

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10 mM * 1  mL in DMSO USD 371 Ask For Quote & Lead Time
5 mg USD 350 Ask For Quote & Lead Time
10 mg USD 591 Ask For Quote & Lead Time

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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[1].

IC50 & Target

pIC50: 9.3 (MCH R1)[1]

In Vitro

GW-803430 demonstrates a potent antagonist activity towards MCH induced MCHR1 receptor with an IC50 value of ~13 nM[2].

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[1].
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[1].

Animal Model: High fat diet-induced obese AKR/J mice[1]
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.
Molecular Weight

481.99

Formula

C₂₅H₂₄ClN₃O₃S

CAS No.

515141-51-2

SMILES

O=C1C2=C(C=C(C3=CC=C(Cl)C=C3)S2)N=CN1C4=CC=C(OCCN5CCCC5)C(OC)=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
References
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Keywords:

GW-803430GW-3430GW803430GW 803430GW3430GW 3430MCHR1 (GPR24)Melanin concentrating hormone receptor 1melaninobesityInhibitorinhibitorinhibit

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GW-803430
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