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GSK3787

Item № 15219
CAS № 188591-46-0
Purity ≥95%
product image
                (CAS 188591-46-0)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     5 mg $57.00 0.00
     10 mg $103.00 0.00
     25 mg $228.00 0.00
     50 mg $399.00 0.00

Pricing updated 2019-07-23. Prices are subject to change without notice.

Description

PPARβ/δ is thought to play a role in lipid homeostasis and glucose disposal by regulating genes involved in fatty acid oxidation, reverse cholesterol transport, and carbon substrate utilization in skeletal muscle. It has also been implicated in the progression of certain cancers.1,2,3,4 GSK3787 is an irreversible antagonist of PPARβ/δ (pIC50 = 6.6) with no measurable affinity for PPARα or PPARγ (pIC50 >5).5 At 1μM, it inhibits the expression of PPARβ/δ-regulated target genes, pyruvate dehydrogenase kinase 4 and carnitine palmitoyl transferase 1a, which are important for energy homeostasis in human skeletal muscle cells.5 GSK3787 (at 1 μM) also antagonizes agonist-induced expression of angiopoietin-like protein 4 in mouse fibroblasts, mouse keratinocytes, and human MCF-7, Huh7, and HepG2 cancer cell lines.6

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Technical Information
Formal Name
4-chloro-N-[2-[[5-(trifluoromethyl)-2-pyridinyl]sulfonyl]ethyl]-benzamide
CAS Number
188591-46-0
Molecular Formula
C15H12ClF3N2O3S
Formula Weight
392.8
Purity
≥95%
Formulation
A crystalline solid
λmax
238 nm
SMILES
O=S(C1=NC=C(C(F)(F)F)C=C1)(CCNC(C2=CC=C(Cl)C=C2)=O)=O
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)
InChI Key
JFUIMTGOQCQTPF-UHFFFAOYSA-N

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 2 years
Downloads & Resources
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Additional Information

View the Cayman Structure Database for chemical structure definitions for many Cayman products

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References & Product Citations
Product Description References

1. Michalik, L., Desvergne, B., and Wahli, W. Peroxisome-proliferator-activated receptors and cancers: Complex stories Nature Reviews.Cancer 4, 61-70 (2004).

2. Girroir, E.E., Hollingshead, H.E., Billin, A.N., et al. Peroxisome proliferator-activated receptor-ß/δ (PPAR ß/δ) ligands inhibit growth of UACC903 and MCF7 human cancer cell lines Toxicology 243, 236-243 (2008).

3. Peters, J.M., Foreman, J.E., and Gonzalez, F.J. Dissecting the role of peroxisome proliferator-activated receptor-ß/δ (PPARß/δ) in colon, breast, and lung carcinogenesis Cancer Metastasis Rev. 30(3-4), 619-640 (2011).

4. Elikkottil, J., Kohli, D.R., and Gupta, K. Antitumor activity of a PPARδ antagonist Cancer Biol. Ther. 8(13), 1262-1264 (2009).

5. Shearer, B.G., Wiethe, R.W., Ashe, A., et al. Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist J. Med. Chem. 53(4), 1857-1861 (2010).

6. Palkar, P.S., Borland, M.G., Naruhn, S., et al. Cellular and pharmacological selectivity of the peroxisome proliferator-activated receptor-β/δ antagonist GSK3787 Molecular Pharmacology 78(3), 419-430 (2010).

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