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MedKoo Cat#: 406255 | Name: GSK-3787
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Description:

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

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

GSK-3787
GSK-3787
CAS#188591-46-0

Theoretical Analysis

MedKoo Cat#: 406255

Name: GSK-3787

CAS#: 188591-46-0

Chemical Formula: C15H12ClF3N2O3S

Exact Mass: 392.0209

Molecular Weight: 392.78

Elemental Analysis: C, 45.87; H, 3.08; Cl, 9.03; F, 14.51; N, 7.13; O, 12.22; S, 8.16

Price and Availability

Size Price Availability Quantity
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
200mg USD 1,250.00 2 Weeks
500mg USD 2,650.00 2 Weeks
1g USD 3,950.00 2 Weeks
2g USD 6,450.00 2 Weeks
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Related CAS #
No Data
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
More Info
        
Product Data
Product Data
Instruction
View handling instruction
Biological target:
GSK3787 is a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist with pIC50 of 6.6.
In vitro activity:
After that, GSK3787 was added to the IVC media, and during the first 84 h of in vitro culture, the two-cell and 3.5-day embryo rates were significantly affected by inhibitor treatment (Figure 5D and Table 1). Furthermore, this study analyzed the blastocyst hatching rate, which showed a marked reduction in the GSK3787 group (19.4%) compared to GW501516- (47.0%) and control-treated (35.9%) blastocysts (Figure 5E). Reference: Int J Mol Sci. 2019 Dec 2;20(23):6066. https://pubmed.ncbi.nlm.nih.gov/31810173/
In vivo activity:
Rats were treated with GSK3787, TXNIP CRISPR activation plasmid and LNA antimiR‐17‐5p to investigate the mechanism of GW0742‐induced suppressing effects on neuroinflammation. GSK3787 significantly increased NLRP3 expression (Figure 5A,B, P < 0.01), therefore reversing the effect of GW0742 and leading to significant increase of expression of TNF‐α, compared to respective DMSO + corn oil control group (Figure 5E, P < 0.05). Reference: J Cell Mol Med. 2020 Nov;24(21):12318-12330. https://pubmed.ncbi.nlm.nih.gov/33034416/
Solvent mg/mL mM
Solubility
DMF 3.0 7.64
DMSO 43.3 110.29
DMSO:PBS (pH 7.2) (1:2) 0.3 0.76
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 392.78 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. Idrees M, Xu L, El Sheikh M, Sidrat T, Song SH, Joo MD, Lee KL, Kong IK. The PPARδ Agonist GW501516 Improves Lipolytic/Lipogenic Balance through CPT1 and PEPCK during the Development of Pre-Implantation Bovine Embryos. Int J Mol Sci. 2019 Dec 2;20(23):6066. doi: 10.3390/ijms20236066. PMID: 31810173; PMCID: PMC6928732. 2. 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. PMID: 20516370; PMCID: PMC2939490. 3. Gamdzyk M, Doycheva DM, Kang R, Tang H, Travis ZD, Tang J, Zhang JH. GW0742 activates miR-17-5p and inhibits TXNIP/NLRP3-mediated inflammation after hypoxic-ischaemic injury in rats and in PC12 cells. J Cell Mol Med. 2020 Nov;24(21):12318-12330. doi: 10.1111/jcmm.15698. Epub 2020 Oct 9. PMID: 33034416; PMCID: PMC7686982. 4. Sidrat T, Khan AA, Idrees M, Joo MD, Xu L, Lee KL, Kong IK. Role of Wnt Signaling During In-Vitro Bovine Blastocyst Development and Maturation in Synergism with PPARδ Signaling. Cells. 2020 Apr 9;9(4):923. doi: 10.3390/cells9040923. PMID: 32283810; PMCID: PMC7226827.
In vitro protocol:
1. Idrees M, Xu L, El Sheikh M, Sidrat T, Song SH, Joo MD, Lee KL, Kong IK. The PPARδ Agonist GW501516 Improves Lipolytic/Lipogenic Balance through CPT1 and PEPCK during the Development of Pre-Implantation Bovine Embryos. Int J Mol Sci. 2019 Dec 2;20(23):6066. doi: 10.3390/ijms20236066. PMID: 31810173; PMCID: PMC6928732. 2. 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. PMID: 20516370; PMCID: PMC2939490.
In vivo protocol:
1. Gamdzyk M, Doycheva DM, Kang R, Tang H, Travis ZD, Tang J, Zhang JH. GW0742 activates miR-17-5p and inhibits TXNIP/NLRP3-mediated inflammation after hypoxic-ischaemic injury in rats and in PC12 cells. J Cell Mol Med. 2020 Nov;24(21):12318-12330. doi: 10.1111/jcmm.15698. Epub 2020 Oct 9. PMID: 33034416; PMCID: PMC7686982. 2. Sidrat T, Khan AA, Idrees M, Joo MD, Xu L, Lee KL, Kong IK. Role of Wnt Signaling During In-Vitro Bovine Blastocyst Development and Maturation in Synergism with PPARδ Signaling. Cells. 2020 Apr 9;9(4):923. doi: 10.3390/cells9040923. PMID: 32283810; PMCID: PMC7226827.
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.