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GW-803430

SKU: orb1707231

Description

GW-803430 (GW-3430) is a selective, orally bioavailable antagonist of the melanin-concentrating hormone receptor 1 (MCHR1). It is a valuable research tool for investigating energy homeostasis and obesity mechanisms in both in vitro binding assays and in vivo animal models.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number515141-51-2
MW481.99
Purity98.97% (May vary between batches)
FormulaC25H24ClN3O3S
SMILESO=C1C=2SC(=CC2N=CN1C3=CC=C(OCCN4CCCC4)C(OC)=C3)C=5C=CC(Cl)=CC5
TargetGPCR,Melanin-concentrating Hormone Receptor (MCHR)
SolubilityDMSO:<1 mg/mL (insoluble)

Bioactivity

Target IC50
MCH1R:13 nM
In Vivo
GW-803430 administered orally once daily at doses of 0.3, 3, and 15 mg/kg induced significant and sustained dose-dependent body weight loss compared to controls. GW-803430 has a favorable pharmacokinetic profile with a bioavailability of 31%, a half-life of 11 hours, and has been shown to exhibit excellent brain penetration in mice with a brain to plasma concentration ratio of 6:1, and is therefore considered an ideal compound.
In Vitro
GW-803430 exhibits significant antagonistic activity against the action of MCH on the MCHR1 receptor with an IC50 value of approximately 13 nM.

Storage & Handling

Storagekeep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

MelaninconcentratingHormoneReceptor, MelaninconcentratingHormoneReceptor(MCHR), Melaninconcentrating Hormone Receptor (MCHR), Melanin-concentrating Hormone Receptor, MCH R1, MCH1-R, MCHR, GW 803430, GW 803430A, GW 3430, GW3430, GW-3430, GW803430, GW-803430, GW803430A

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Quality Guarantee

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Key Properties

No computed properties available.

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Protocol Information

GW-803430 (orb1707231)

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Step 1: Enter information below

(Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
$ 100.00
2 mg
$ 130.00
5 mg
$ 190.00
10 mg
$ 310.00
25 mg
$ 530.00
50 mg
$ 820.00
100 mg
$ 1,090.00
DispatchUsually dispatched within 5-10 working days
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