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CAY10592 Exclusive

Cayman Chemical Item Number 10012536

(CAS 685139-10-0)

CAY10592 (CAS 685139-10-0)

See more	Nuclear Receptors (94) PPAR (59) Atherosclerosis (325) Metabolism (145)

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	Copy SMILES to clipboard OC(=O)COc1ccc(SCC=C(c2ccc(Br)cc2)c2ccc(Br)cc2)cc1Cl

Background Reading

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).

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).

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).

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

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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
Bulk	Contact
		Cart Total	$0.00

Pricing updated 2012-05-25. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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