MK-8245 - CAS 1030612-90-8
Catalog number: 1030612-90-8
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
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Targets:
Stearoyl-CoA Desaturase (SCD)
Description:
MK-8245 is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy.
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Purity:
0.98
Related CAS:
1415559-41-9 (TFA)
Appearance:
Solid powder
Synonyms:
4-(2-Bromo-5-fluorophenoxy)-1-[5-(2H-tetrazol-5-yl)-3-isoxazolyl]piperidine; MK-8245; MK8245; MK8245
MSDS:
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InChIKey:
UDXUBDGJHLPKFJ-UHFFFAOYSA-N
InChI:
1S/C15H14BrFN6O2/c16-11-2-1-9(17)7-12(11)24-10-3-5-23(6-4-10)14-8-13(25-20-14)15-18-21-22-19-15/h1-2,7-8,10H,3-6H2,(H,18,19,21,22)
Canonical SMILES:
FC1=CC=C(Br)C(OC2CCN(C3=NOC(C4=NNN=N4)=C3)CC2)=C1
1.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 RM1, 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, Sørensen D, Sturken J Med Chem. 2011 Jul 28;54(14):5082-96. doi: 10.1021/jm200319u. Epub 2011 Jun 28.
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.
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