917910-45-3 Usage
Biological Activity
mk-6892 is a highly potential gpr109a agonists.
in vitro
despite the increased serum shift of these compounds, the representative 1e was highly potent. furthermore, these compounds had no activity on gpr109b and gpr81, the two most closely related gpcrs with 96% and 50% sequence identity to gpr109a,respectively [1].
in vivo
na or mk-6892 was orally administered to wt or na receptor null mice on the same c57bl/6 genetic background. after 15 min of 100 mpk dosing of na or mk-6892 to fed wt or na receptor null mice, the blood levels of mk-6892 at 15 min were 229 μm (950-fold greater than the in vitro ec50 determined in mouse na receptor gtpγs assay, which is 240 nm) in wt mice and 148 μm (620-fold greater than the in vitro ec50) in na receptor null mice [1].
IC 50
ic50 value: 4.0 nm (ki for human gpr109a) [1]
Check Digit Verification of cas no
The CAS Registry Mumber 917910-45-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,1,7,9,1 and 0 respectively; the second part has 2 digits, 4 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 917910-45:
(8*9)+(7*1)+(6*7)+(5*9)+(4*1)+(3*0)+(2*4)+(1*5)=183
183 % 10 = 3
So 917910-45-3 is a valid CAS Registry Number.
917910-45-3Relevant articles and documents
Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): A potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate
Shen, Hong C.,Ding, Fa-Xiang,Raghavan, Subharekha,Deng, Qiaolin,Luell, Silvi,Forrest, Michael J.,Carballo-Jane, Ester,Wilsie, Larissa C.,Krsmanovic, Mihajlo L.,Taggart, Andrew K.,Wu, Kenneth K.,Wu, Tsuei-Ju,Cheng, Kang,Ren, Nina,Cai, Tian-Quan,Chen, Qing,Wang, Junying,Wolff, Michael S.,Tong, Xinchun,Holt, Tom G.,Waters, M.Gerard,Hammond, Milton L.,Tata, James R.,Colletti, Steven L.
supporting information; experimental part, p. 2666 - 2670 (2010/08/22)
Biaryl cyclohexene carboxylic acids were discovered as full and potent niacin receptor (GPR 109A) agonists. Compound 1e (MK-6892) displayed excellent receptor activity, good PK across species, remarkably clean off-target profiles, good ancillary pharmacology, and superior therapeutic window over niacin regarding the FFA reduction versus vasodilation in rats and dogs.
