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RP 70676

Names

[ CAS No. ]:
136609-26-2

[ Name ]:
RP 70676

[Synonym ]:
1H-Pyrazole, 1-[5-[(4,5-diphenyl-1H-imidazol-2-yl)thio]pentyl]-3,5-dimethyl-
1-{5-[(4,5-Diphenyl-1H-imidazol-2-yl)sulfanyl]pentyl}-3,5-dimethyl-1H-pyrazole

Biological Activity

[Description]:

RP 70676 is a potent inhibitor of ACAT, with IC50 of 25 and 44 nM for rat and rabbit ACAT.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Acyltransferase
Research Areas >> Metabolic Disease

[Target]

IC50: 25 nM (Rat ACAT), 44 nM (Rabbit ACAT)[1]


[In Vitro]

RP 70676 is a potent inhibitor of rabbit arterial ACAT (IC50 = 40 nM) and has been shown to be an effective inhibitor of ACAT derived from a number of tissues and species including man. The IC50 values range from 21 nM for hamster liver ACAT to 108 nM for enzyme from the intestine of cholesterol fed rabbits; in human hepatic tissues the mean IC50 is 44 nM. In whole cell P388D, murine macrophages the compound has an IC50 of 540 nM.

[In Vivo]

RP 70676 (10 mg/kg, p.o.) is well absorbed with plasma levels in NZW rabbits[1].

[References]

[1]. M.J. Ashton, et al. RP 70676: A potent systematically available inhibitor of acyl-CoA:cholesterol O-acyl transferase (ACAT). Bioorganic & Medicinal Chemistry Letters Volume 2, Issue 5, 1992, Pages 375-380.


[Related Small Molecules]

Avasimibe | LCQ-908 | DGAT-3 | A922500 | Xanthohumol | PF-04620110 | AZD7687 | MGAT2-IN-1 | DGAT-1 inhibitor 2 | DGAT1-IN-1 | K-604 dihydrochloride | PF-06471553 | YM17E | ABT-046 | Furan-2-carboxylic acid

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
605.9±57.0 °C at 760 mmHg

[ Molecular Formula ]:
C25H28N4S

[ Molecular Weight ]:
416.582

[ Flash Point ]:
320.2±32.1 °C

[ Exact Mass ]:
416.203461

[ LogP ]:
5.94

[ Vapour Pressure ]:
0.0±1.7 mmHg at 25°C

[ Index of Refraction ]:
1.634

[ Storage condition ]:
2-8℃


Related Compounds