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533974 Stearoyl-CoA Desaturase-1 Inhibitor II, MK-8245 - CAS 1030612-90-8 - Calbiochem

Stearoyl-CoA Desaturase-1 Inhibitor II, MK-8245, CAS 1030612-90-8, is a highly potent and selective inhibitor of liver stearoyl-CoA desaturase-1 (IC₅₀ = 1, 3, and 3 nM for human, rat, & mouse).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: (5-(3-(4-(2-Bromo-5-fluorophenoxy)-1-piperidinyl)-1,2-oxazol-5-yl)-2H-tetrazol-2-yl)acetic acid, Liver-Targeting SCD1 Inhibitor, MK8245

Primary Target: SCD1
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      Overview

      Key Spec Table

      CAS #Empirical Formula
      1030612-90-8C₁₇H₁₆BrFN₆O₄
      Description
      OverviewA moderately cell-permeable, orally active, non-toxic isoxazolyl-tetrazolo acetic acid based compound that acts as a highly potent and selective inhibitor of liver stearoyl-CoA desaturase-1 (SCD1; IC50 = 1, 3, and 3 nM for human, rat, and mouse, respectively). Does not exhibit any affinity towards Δ-5 and Δ-6 desaturases (> 100 mM). It is taken up by hepatocytes via organic anion transporting polypeptides (OATP-1B1 and -1B3) to block SCD1 activity (IC50 = 5 nM in human). Displays only a trivial uptake in non-OATP cells (IC50 = 1.066 uM in HepG2 cells). Shown to improve insulin sensitivity and glucose clearance in diet-induced obese mice (ED50 = 7 mg/kg when given at 20 mg/kg, b.i.d; p.o.). Displays favorable pharmacokinetic profile with a clearance rate of 15 ml/min/kg and t1/2 = 0.7 h (at 10 mg/kg, p.o. in fasting male C57BL6 mice).

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number533974
      Brand Family Calbiochem®
      Synonyms(5-(3-(4-(2-Bromo-5-fluorophenoxy)-1-piperidinyl)-1,2-oxazol-5-yl)-2H-tetrazol-2-yl)acetic acid, Liver-Targeting SCD1 Inhibitor, MK8245
      References
      ReferencesOballa, R.M., et al. 2011. J. Med. Chem. 54, 5082.
      Product Information
      CAS number1030612-90-8
      FormOff-white solid
      Hill FormulaC₁₇H₁₆BrFN₆O₄
      Chemical formulaC₁₇H₁₆BrFN₆O₄
      Quality LevelMQ100
      Biological Information
      Primary TargetSCD1
      Primary Target IC<sub>50</sub>1, 3, and 3 nM for human, rat, and mouse, respectively
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalogue Number GTIN
      533974 0