CAY10592 Exclusive

Cayman Chemical Item Number 10012536

(CAS 685139-10-0)

CAY10592 (CAS 685139-10-0)

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Description

Peroxisome proliferator-activated receptors (PPARs) α, δ, γ are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism.1,2 Pharmacologies of PPARδ receptor agonists, though relatively obscure, have recently been reported to elevate high-density lipoprotein (HDL) cholesterol and lower plasma triglyceride (TG) levels in obese insulin resistant rhesus monkeys.3 CAY10592 is a full PPARδ agonist (EC50 = 30 nM) in a fatty acid oxidation assay of rat L6 muscle cells with desirable oral pharmacokinetic properties.4 In a transactivation assay using human PPAR receptors, CAY10592 acts as a selective partial PPARδ agonist (EC50 = 53 nM) with no effect on PPARα or PPARγ activity up to 30 µM.4 Chronic treatment of high fat fed ApoB100/CETP-transgenic mice with CAY10592 at a dose of 20 mg/kg increases HDL levels, decreases low-density lipoprotein and TG levels, and improves insulin sensitivity.4

1 Michalik, L., Auwerx, J., Berger, J.P., et al. International union of pharmacology. LXI. Peroxisome proliferator-activated receptors. Pharmacol Rev 58 726-741 (2006).

2 Bratton, L.D., Filzen, G.F., Geyer, A., et al. Discovery of highly potent and selective benzyloxybenzyl-based peroxisome proliferator-activator receptor (PPAR) d agonists. Bioorg Med Chem Lett 17 3624-3629 (2007).

3 Oliver, W.R., Shenk, J.L., Snaith, M.R., et al. A selective peroxisome proliferator-activated receptor δ agonist promotes reverse cholesterol transport. Proc Natl Acad Sci USA 98(9) 5306-5311 (2001).

4 Sauerberg, P., Olsen, G.S., Jeppesen, L., et al. Identification and synthesis of a novel selective partial PPARδ agonist with full efficacy on lipid metabolism in vitro and in vivo. J Med Chem 50 1495-1503 (2007).

Formal Name 2-​[4-​[[3,​3-​bis(4-​bromophenyl)-​2-​propen-​1-​yl]thio]-​2-​chlorophenoxy]-​acetic acid
CAS Number 685139-10-0
Molecular Formula C23H17Br2ClO3S
Formula Weight 568.7
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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OC(=O)​COc1ccc(SCC=C(c2ccc(Br)​cc2)​c2ccc(Br)​cc2)​cc1Cl
InCHI Code
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​1S/C23H17Br2ClO3S/c24-17-5-1-15(2-6-17)​20(16-3-7-18(25)​8-4-16)​11-12-30-19-9-10-22(21(26)​13-19)​29-14-23(27)​28/h1-11,13H,12,14H2,(H,27,28)​
InCHI Key
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NQIYGYDPRBEUAZ-UHFFFAOYSA-N

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Size Price Quantity Subtotal
1 mg $26.00 $0.00
5 mg $117.00 $0.00
10 mg $208.00 $0.00
50 mg $910.00 $0.00
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Cart Total $0.00

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Pricing updated 2014-04-20. Prices are subject to change without notice.

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