GSK-3787
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MedKoo CAT#: 406255

CAS#: 188591-46-0

Description: GSK-3787 is a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist with good pharmacokinetic properties. GSK3787 can antagonize PPARbeta/delta in vivo, thus providing a new strategy to delineate the functional role of a receptor with great potential as a therapeutic target for the treatment and prevention of disease.


Chemical Structure

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GSK-3787
CAS# 188591-46-0

Theoretical Analysis

MedKoo Cat#: 406255
Name: GSK-3787
CAS#: 188591-46-0
Chemical Formula: C15H12ClF3N2O3S
Exact Mass: 392.02093
Molecular Weight: 392.78059
Elemental Analysis: C, 45.87; H, 3.08; Cl, 9.03; F, 14.51; N, 7.13; O, 12.22; S, 8.16

Size Price Shipping out time Quantity
50mg USD 250 2 Weeks
100mg USD 450 2 Weeks
200mg USD 750 2 Weeks
500mg USD 1450 2 Weeks
1g USD 2850 2 Weeks
2g USD 4650 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-03-07. Prices are subject to change without notice.

GSK-3787, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Synonym: GSK3787; GSK-3787; GSK 3787.

IUPAC/Chemical Name: 4-chloro-N-(2-((5-(trifluoromethyl)pyridin-2-yl)sulfonyl)ethyl)benzamide

InChi Key: JFUIMTGOQCQTPF-UHFFFAOYSA-N

InChi Code: InChI=1S/C15H12ClF3N2O3S/c16-12-4-1-10(2-5-12)14(22)20-7-8-25(23,24)13-6-3-11(9-21-13)15(17,18)19/h1-6,9H,7-8H2,(H,20,22)

SMILES Code: O=C(NCCS(=O)(C1=NC=C(C(F)(F)F)C=C1)=O)C2=CC=C(Cl)C=C2

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, not soluble in water.

Shelf Life:
>5 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

Handling Instructions:

Preparing Stock Solutions

The following data is based on the product molecular weight 392.78059 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.

Select a batch to recalculate based on the batch molecular weight:
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

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1: Gu Y, Li X, He T, Jiang Z, Hao P, Tang X. The Antifibrosis Effects of Peroxisome Proliferator-Activated Receptor δ on Rat Corneal Wound Healing after Excimer Laser Keratectomy. PPAR Res. 2014;2014:464935. doi: 10.1155/2014/464935. Epub 2014 Nov 13. PubMed PMID: 25477952; PubMed Central PMCID: PMC4248330.

2: Zhou X, Ringseis R, Wen G, Eder K. Carnitine transporter OCTN2 and carnitine uptake in bovine kidney cells is regulated by peroxisome proliferator-activated receptor β/δ. Acta Vet Scand. 2014 Apr 9;56:21. doi: 10.1186/1751-0147-56-21. PubMed PMID: 24716857; PubMed Central PMCID: PMC3998222.

3: Luo G, Shi Y, Zhang J, Mu Q, Qin L, Zheng L, Feng Y, Berggren-Söderlund M, Nilsson-Ehle P, Zhang X, Xu N. Palmitic acid suppresses apolipoprotein M gene expression via the pathway of PPARβ/δ in HepG2 cells. Biochem Biophys Res Commun. 2014 Feb 28;445(1):203-7. doi: 10.1016/j.bbrc.2014.01.170. Epub 2014 Feb 4. PubMed PMID: 24508264.

4: Chen YC, Chu LY, Yang SF, Chen HL, Yet SF, Wu KK. Prostacyclin and PPARα agonists control vascular smooth muscle cell apoptosis and phenotypic switch through distinct 14-3-3 isoforms. PLoS One. 2013 Jul 3;8(7):e69702. doi: 10.1371/journal.pone.0069702. Print 2013. PubMed PMID: 23844263; PubMed Central PMCID: PMC3701049.

5: Hack K, Reilly L, Palmer C, Read KD, Norval S, Kime R, Booth K, Foerster J. Skin-targeted inhibition of PPAR β/δ by selective antagonists to treat PPAR β/δ-mediated psoriasis-like skin disease in vivo. PLoS One. 2012;7(5):e37097. doi: 10.1371/journal.pone.0037097. Epub 2012 May 14. PubMed PMID: 22606335; PubMed Central PMCID: PMC3351437.

6: Palkar PS, Borland MG, Naruhn S, Ferry CH, Lee C, Sk UH, Sharma AK, Amin S, Murray IA, Anderson CR, Perdew GH, Gonzalez FJ, Müller R, Peters JM. Cellular and pharmacological selectivity of the peroxisome proliferator-activated receptor-beta/delta antagonist GSK3787. Mol Pharmacol. 2010 Sep;78(3):419-30. doi: 10.1124/mol.110.065508. Epub 2010 Jun 1. PubMed PMID: 20516370; PubMed Central PMCID: PMC2939490.

7: Shearer BG, Wiethe RW, Ashe A, Billin AN, Way JM, Stanley TB, Wagner CD, Xu RX, Leesnitzer LM, Merrihew RV, Shearer TW, Jeune MR, Ulrich JC, Willson TM. Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist. J Med Chem. 2010 Feb 25;53(4):1857-61. doi: 10.1021/jm900464j. PubMed PMID: 20128594.



Additional Information