GW-803430 | CAS#515141-51-2 | MCH1 inhibitor

MedKoo Cat#: 526860 | Name: GW-803430

Description:

WARNING: This product is for research use only, not for human or veterinary use.

GW-803430 is a potent, orally active and selective melanin-concentrating hormone receptor 1 (MCH1) antagonist (IC50 = 9.3 nM). GW-803430 displays antiobesity and antidepressant-like effects in rats and mice.

Chemical Structure

GW-803430

CAS#515141-51-2

Theoretical Analysis

MedKoo Cat#: 526860

Name: GW-803430

CAS#: 515141-51-2

Chemical Formula: C25H24ClN3O3S

Exact Mass: 481.1227

Molecular Weight: 482.00

Elemental Analysis: C, 62.30; H, 5.02; Cl, 7.35; N, 8.72; O, 9.96; S, 6.65

Price and Availability

Size	Price	Availability
25mg	USD 550.00	2 Weeks
50mg	USD 850.00	2 Weeks
100mg	USD 1,350.00	2 Weeks
200mg	USD 2,150.00	2 Weeks
1g	USD 4,850.00	2 Weeks

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Related CAS #

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Synonym

GW-803430; GW 803430; GW803430; GW-803430A; GW803430A; GW 803430A; GW3430; GW 3430; GW-3430

IUPAC/Chemical Name

6-(4-Chlorophenyl)-3-[3-methoxy-4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-thieno[3,2-d]pyrimidin-4(3H)-one

InChi Key

MWULMTACIBZPGN-UHFFFAOYSA-N

InChi Code

InChI=1S/C25H24ClN3O3S/c1-31-22-14-19(8-9-21(22)32-13-12-28-10-2-3-11-28)29-16-27-20-15-23(33-24(20)25(29)30)17-4-6-18(26)7-5-17/h4-9,14-16H,2-3,10-13H2,1H3

SMILES Code

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

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

GW-803430 (GW-3430) is a potent and selective melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pIC50 of 9.3.

In vitro activity:

TBD

In vivo activity:

Pretreatment with 3 mg/kg dose of GW803430, significantly reversed the MCH, OT, and MCH+OT mediated reduction in marble burying (Fig. 6A) in mice. Reference: Neuropharmacology. 2018 Jan;128:22-32. https://pubmed.ncbi.nlm.nih.gov/28888943/

	Solvent	mg/mL	mM
Solubility
	DMF	2.0	4.15
	DMSO	2.0	4.15
	Ethanol	2.0	4.15

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 482.00 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Sanathara NM, Garau C, Alachkar A, Wang L, Wang Z, Nishimori K, Xu X, Civelli O. Melanin concentrating hormone modulates oxytocin-mediated marble burying. Neuropharmacology. 2018 Jan;128:22-32. doi: 10.1016/j.neuropharm.2017.09.008. Epub 2017 Sep 6. PMID: 28888943; PMCID: PMC5830107. 2. Alachkar A, Alhassen L, Wang Z, Wang L, Onouye K, Sanathara N, Civelli O. Inactivation of the melanin concentrating hormone system impairs maternal behavior. Eur Neuropsychopharmacol. 2016 Nov;26(11):1826-1835. doi: 10.1016/j.euroneuro.2016.08.014. Epub 2016 Sep 9. PMID: 27617778; PMCID: PMC5929110.

In vitro protocol:

TBD

In vivo protocol:

1: Rabal O, Amr FI, Oyarzabal J. Novel Scaffold FingerPrint (SFP): applications in scaffold hopping and scaffold-based selection of diverse compounds. J Chem Inf Model. 2015 Jan 26;55(1):1-18. doi: 10.1021/ci500542e. Epub 2015 Jan 13. PubMed PMID: 25558803. 2: Zhang LN, Sinclair R, Selman C, Mitchell S, Morgan D, Clapham JC, Speakman JR. Effects of a specific MCHR1 antagonist (GW803430) on energy budget and glucose metabolism in diet-induced obese mice. Obesity (Silver Spring). 2014 Mar;22(3):681-90. doi: 10.1002/oby.20418. Epub 2013 Dec 2. PubMed PMID: 23512845. 3: Karlsson C, Zook M, Ciccocioppo R, Gehlert DR, Thorsell A, Heilig M, Cippitelli A. Melanin-concentrating hormone receptor 1 (MCH1-R) antagonism: reduced appetite for calories and suppression of addictive-like behaviors. Pharmacol Biochem Behav. 2012 Sep;102(3):400-6. doi: 10.1016/j.pbb.2012.06.010. Epub 2012 Jun 15. PubMed PMID: 22705492. 4: Cippitelli A, Karlsson C, Shaw JL, Thorsell A, Gehlert DR, Heilig M. Suppression of alcohol self-administration and reinstatement of alcohol seeking by melanin-concentrating hormone receptor 1 (MCH1-R) antagonism in Wistar rats. Psychopharmacology (Berl). 2010 Sep;211(4):367-75. doi: 10.1007/s00213-010-1891-y. Epub 2010 Jul 14. PubMed PMID: 20628734. 5: Gehlert DR, Rasmussen K, Shaw J, Li X, Ardayfio P, Craft L, Coskun T, Zhang HY, Chen Y, Witkin JM. Preclinical evaluation of melanin-concentrating hormone receptor 1 antagonism for the treatment of obesity and depression. J Pharmacol Exp Ther. 2009 May;329(2):429-38. doi: 10.1124/jpet.108.143362. Epub 2009 Jan 30. PubMed PMID: 19182070.