GW-803430
featured

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

MedKoo CAT#: 526860

CAS#: 515141-51-2

Description: 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

img
GW-803430
CAS# 515141-51-2

Theoretical Analysis

MedKoo Cat#: 526860
Name: GW-803430
CAS#: 515141-51-2
Chemical Formula: C25H24ClN3O3S
Exact Mass: 481.12
Molecular Weight: 481.995
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 Quantity
5mg USD 250
25mg USD 670
Bulk inquiry

Synonym: GW-803430; GW 803430; GW803430.

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:
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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 2.0 4.15
DMSO 2.0 4.15
Ethanol 2.0 4.15

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.

Recalculate based on batch purity %
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. 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.

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

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.