JTT705 Inhibitor CAS No. 211513-37-0

Cat. No.	Name	Size	Price
KI1146	JTT705	10 mg	$445.5
	JTT705	50 mg	$742.5
	JTT705	50 mg	$1100
	JTT705	100 mg	$2376

Chemical Characteristic

Product Name	JTT705
Synonyms	Dalcetrapib,RO4607381
CAS No.	211513-37-0
Molecular Weight	389.59
Formula	C₂₃H₃₅NO₂S
Chemical Name	S-[2-[[1-(2-ethylbutyl)cyclohexanecarbonyl]amino]phenyl] 2-methylpropanethioate
Smiles	C(=O)(C(C)C)Sc1c(cccc1)NC(=O)C1(CCCCC1)CC(CC)CC
Chemical Structure

Biological activities

JTT-705 is a novel inhibitor of cholesteryl ester transfer protein (CETP). JTT-705 induces the phosphorylation of p38 mitogen-activated protein kinase (MAPK) and extracellular-signal-regulated kinases (ERK) in SMCs. JTT-705 blocks the proliferation of SMCs through the activation of p38 kinase/p27^kip1 and Ras/p21^waf1 pathways. And simultaneously, JTT-705 also blocks EC tube formation associated with a decrease in VEGF production from SMCs.^[1] JTT-705 significantly inhibits CETP activities. JTT-705 increases HDL cholesterol (HDL-C) levels and the ratio of HDL2-C/HDL3-C. JTT-705 decreases the fractional esterification rate of cholesterol in HDL. JTT-705 treatment increases serum paraoxonase activity and HDL-associated platelet-activating factor acetylhydrolase activity. ^[2] JTT-705 increases plasma HDL cholesterol and inhibits the progression of atherosclerosis in cholesterol-fed rabbits. JTT-705 increases plasma HDL-C, decreases non-HDL-C and, importantly, results in a 70% decrease of aortic arch lesions. ^[3]

References

[1] Miura S, et al. JTT-705 blocks cell proliferation and angiogenesis through p38 kinase/p27 (kip1) and Ras/p21 (waf1) pathways. Atherosclerosis. 2005, 182(2): 267-275 [2] Zhang B, et al. Inhibition of cholesteryl ester transfer protein activity by JTT-705 increases apolipoprotein E-containing high-density lipoprotein and favorably affects the function and enzyme composition of high-density lipoprotein in rabbits. Arterioscler Thromb Vasc Biol. 2004, 24(10): 1910-1915 [3] de Grooth GJ, et al. Efficacy and safety of a novel cholesteryl ester transfer protein inhibitor, JTT-705, in humans: a randomized phase II dose-response study. Circulation. 2002, 105(18): 2159-2165.

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