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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).

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Synonyme: (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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      Übersicht

      Replacement Information

      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
      Applications
      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
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      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
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Bestellnummer GTIN
      533974 0

      Documentation

      Literatur

      Übersicht
      Oballa, R.M., et al. 2011. J. Med. Chem. 54, 5082.
      Datenblatt

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision20-November-2015 JSw
      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
      DescriptionA 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).
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1030612-90-8
      Chemical formulaC₁₇H₁₆BrFN₆O₄
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      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.
      Toxicity Standard Handling
      ReferencesOballa, R.M., et al. 2011. J. Med. Chem. 54, 5082.