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

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.

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GW-803430 Chemical Structure

GW-803430 Chemical Structure

CAS No. : 515141-51-2

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Based on 1 publication(s) in Google Scholar

GW-803430 Related Antibodies

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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]
Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
16 nM
Compound: 43
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
[PMID: 26022839]
In Vitro

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GW-803430 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Appearance

Solid

Color

Off-white to yellow

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
Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (25.93 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0747 mL 10.3737 mL 20.7473 mL
5 mM 0.4149 mL 2.0747 mL 4.1495 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.10%

SDS (393 KB)

COA (245 KB) HNMR (138 KB) RP-HPLC (168 KB) LCMS (107 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0747 mL 10.3737 mL 20.7473 mL 51.8683 mL
5 mM 0.4149 mL 2.0747 mL 4.1495 mL 10.3737 mL
10 mM 0.2075 mL 1.0374 mL 2.0747 mL 5.1868 mL
15 mM 0.1383 mL 0.6916 mL 1.3832 mL 3.4579 mL
20 mM 0.1037 mL 0.5187 mL 1.0374 mL 2.5934 mL
25 mM 0.0830 mL 0.4149 mL 0.8299 mL 2.0747 mL
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GW-803430 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GW-803430515141-51-2GW-3430GW803430GW 803430GW3430GW 3430MCHR1 (GPR24)Melanin concentrating hormone receptor 1melaninobesityInhibitorinhibitorinhibit

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