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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).

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

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
Catalogue Number GTIN
533974 0

Documentation

References

Reference overview
Oballa, R.M., et al. 2011. J. Med. Chem. 54, 5082.
Data Sheet

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.