基本信息

产品描述

GSK3787是一种选择性的，不可逆PPARδ拮抗剂，pIC50为6.6，对hPPARα和hPPARγ没有亲和力。

靶点（IC50 & Targe）

PPARδ,6.6(pIC50)

参考文献

[1] Shearer BG, et al. J Med Chem, 2010, 53(4), 1857-1861.

[2] Palkar PS, et al. Mol Pharmacol, 2010, 78(3) 419-430.

[3] Brown PJ, et al. Chem Biol, 1997, 4(12), 909-918.

安全信息

图形或危害标志
提示语	Warning
危险说明	H302 H410
防范说明	P264 P270 P273 P301+P312 P330 P391 P501
UN号码	3077
危险分类	9
包装等级	III

产品说明

应用

GSK3787 has been used to inhibit the role of peroxisome proliferator-activated receptor-delta (PPARδ), during the pre-implantation period of bovine embryonic development. It has also been used as a PPARδ-specific inhibitor in in vitro maturation (IVM) media to inhibit PPARδ.

包装

5, 25 mg in glass bottle

生化/生理作用

GSK3787 is an orally available selective irreversible Peroxisome Proliferator-Activated Receptor δ (PPARδ) antagonist (pIC50=6.6) with no measurable affinity for hPPARR or hPPARγ (pIC50<5). It acts by covalently modifying Cys249 within the ligand binding pocket, and has been shown to antagonize the induction of PPARδ-regulated target genes in skeletal muscle cells.
GSK3787 is known to exhibit pharmacokinetic properties.

特点和优势

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

基本信息

产品性质

安全信息

产品说明

一般描述

A cell-permeable and orally available pyridylsulfone compound that acts as a selective, high affinity PPARβ (PPARδ) ligand (IC₅₀ in PPAR ligand displacement assays = 200 nM against human PPARβ and >10 µM against PPARα or PPARγ) and effectively antagonizes agonist-induced, but not basal, PPARβ transcription activity both in cultures in vitro (IC₅₀ = 126 nM against 2 nM GW501516-induced reporter transcription in CV-1 cells) and in mice in vivo (82% and 71% inhibition of 10 mg/kg GW0742-induced Adrp and Angptl4 mRNA upregulation, respectively, in colon epithelium by 10 mg/kg GSK3787; p.o.) by covalently modifying PPARβ at Cys²⁴⁹. GSK3787 is also shown to exhibit weak agonistic activity toward PPARγ (1.2-fold increase above basal level by 1 µM GSK3787), and effectively block the more potent agonist GW1929 (Cat. Nos. 370695) from further stimulation (1.5 and 3.5-fold above basal by 0.3 µM GW1929 in the presence or absence of 1 µM GSK3787, respectively).
A cell-permeable pyridylsulfone that acts as a selective, high affinity PPARβ (PPARδ) ligand (IC₅₀ in PPAR ligand displacement assays = 200 nM against human PPARβ and >10 µM against PPARα or PPARγ) and effectively antagonizes agonist-induced, but not basal, PPARβ transcription activity both in cultures in vitro (IC₅₀ = 126 nM in CV-1 cells) and in mice in vivo (82% and 71% inhibition of 10 mg/kg GW0742-induced Adrp and Angptl4 mRNA upregulation, respectively, in colon epithelium; 10 mg/kg GSK3787; p.o.) by covalently modifying PPARβ at Cys²⁴⁹. GSK3787 is also shown to exhibit weak agonistic activity toward PPARγ (1.2-fold increase above basal level by 1 µM GSK3787), and effectively block the more potent agonist GW1929 (Cat. Nos. 370695) from further stimulation (1.5 and 3.5-fold above basal by 0.3 µM GW1929 in the presence or absence of 1 µM GSK3787, respectively).

包装

10 mg in Glass bottle
Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Palkar, P.S., et al. 2010. Mol. Pharmacol.78, 419.
Shearer, B,G., et al. 2010. J. Med. Chem.53, 1857.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

产品性质

安全信息

基本信息

安全信息

图形或危害标志
危险性说明	H315: Causes skin irritation. H319: Causes serious eye irritation. H335: May cause respiratory irritation.
防范说明	P233: Keep container tightly closed. P260: Do not breathe . P261: Avoid breathing . P264: Wash hands thoroughly after handling. P271: Use only outdoors or in a well-ventilated area. P280: Wear . P302 + P352: IF ON SKIN: Wash with plenty of soap and water. P304: IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing.. P304 + P340: IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P305 + P351 + P338: IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. P312: Call a POISON CENTER or doctor/physician if you feel unwell. P321: Specific treatment (see relevant procedures. on this label). P332 + P313: If skin irritation occurs: Get medical advice/ attention. P337 + P313: If eye irritation persists: Get medical advice/attention. P340: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P362: Take off contaminated clothing and wash before reuse. P403: Store in a well-ventilated place. P403 + P233: Store in a well-ventilated place. Keep container tightly closed. P405: Store locked up. P501: Dispose of contents/container to in accordance with local regulation .