1030612-90-8 Usage
Description
MK-8245 is a liver-targeted inhibitor of stearoyl-CoA desaturase (SCD; IC50s = 3, 3, and 1 nM for rat, mouse, and human SCD1, respectively). It is selective for SCD1 over Δ5- and Δ6-desaturases (IC50s = >100,000 nM). MK-8245 (20-60 mg/kg) reduces the hepatic, but not Harderian gland, ratio of oleic acid to stearic acid, a marker of chronic SCD activity, and blood glucose levels, without inducing the formation of skin lesions or eye squinting behavior, in a mouse model of high-fat diet-induced obesity. It also inhibits hepatitis C virus (HCV) replication without inducing cytotoxicity in LucNeo2 cells (IC50 = 39.8 nM).
Uses
This product is Informer compound X9 of the Aryl Halide Chemistry Informer Library developed by chemists at Merck & Co., Inc., Kenilworth, NJ, U.S., which contains 18 drug-like molecules representative of those encountered in complex synthesis. By screening a new reaction against the Informer Library, chemists can directly compare and analyse a reaction′s successes and shortcomings among different methods and various research teams. It may also be used to facilitate deeper method development for performance or utility.
references
[1] oballa rm, belair l, black wc, bleasby k, chan cc, desroches c, du x, gordon r, guay j, guiral s, hafey mj, hamelin e, huang z, kennedy b, lachance n, landry f, li cs, mancini j, normandin d, pocai a, powell da, ramtohul yk, skorey k, srensen d, sturkenboom w, styhler a, waddleton dm, wang h, wong s, xu l, zhang l. development of a liver-targeted stearoyl-coa desaturase (scd) inhibitor (mk-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia. j med chem. 2011 jul 28;54(14):5082-96.[2] lachance n, guiral s, huang z, leclerc jp, li cs, oballa rm, ramtohul yk, wang h, wu j, zhang l. discovery of potent and liver-selective stearoyl-coa desaturase (scd) inhibitors in an acyclic linker series. bioorg med chem lett. 2012 jan 1;22(1):623-7.
Check Digit Verification of cas no
The CAS Registry Mumber 1030612-90-8 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,3,0,6,1 and 2 respectively; the second part has 2 digits, 9 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 1030612-90:
(9*1)+(8*0)+(7*3)+(6*0)+(5*6)+(4*1)+(3*2)+(2*9)+(1*0)=88
88 % 10 = 8
So 1030612-90-8 is a valid CAS Registry Number.
1030612-90-8Relevant articles and documents
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia
Oballa, Renata M.,Belair, Liette,Black, W. Cameron,Bleasby, Kelly,Chan, Chi Chung,Desroches, Carole,Du, Xiaobing,Gordon, Robert,Guay, Jocelyne,Guiral, Sebastien,Hafey, Michael J.,Hamelin, Emelie,Huang, Zheng,Kennedy, Brian,Lachance, Nicolas,Landry, France,Li, Chun Sing,Mancini, Joseph,Normandin, Denis,Pocai, Alessandro,Powell, David A.,Ramtohul, Yeeman K.,Skorey, Kathryn,S?rensen, Dan,Sturkenboom, Wayne,Styhler, Angela,Waddleton, Deena M.,Wang, Hao,Wong, Simon,Xu, Lijing,Zhang, Lei
experimental part, p. 5082 - 5096 (2011/09/21)
The potential use of SCD inhibitors for the chronic treatment of diabetes and dyslipidemia has been limited by preclinical adverse events associated with inhibition of SCD in skin and eye tissues. To establish a therapeutic window, we embarked on designing liver-targeted SCD inhibitors by utilizing molecular recognition by liver-specific organic anion transporting polypeptides (OATPs). In doing so, we set out to target the SCD inhibitor to the organ believed to be responsible for the therapeutic efficacy (liver) while minimizing its exposure in the tissues associated with mechanism-based SCD depletion of essential lubricating lipids (skin and eye). These efforts led to the discovery of MK-8245 (7), a potent, liver-targeted SCD inhibitor with preclinical antidiabetic and antidyslipidemic efficacy with a significantly improved therapeutic window.
