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505479 SIRT1/2/3 pan Inhibitor - CAS 1431411-60-7 - Calbiochem

505479
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1431411-60-7C₁₉H₂₇N₅O₂S

Products

Catalogue NumberPackaging Qty/Pack
5054790001 Glass bottle 10 mg
Description
OverviewA thienopyrimidinylcarboxamide that acts as a highly potent, reversible pan sirtuin (SIRT) inhibitor (IC50 = 15, 10, and 33 nM for SIRT1, 2, and 3, respectively). Shown to bind to the SIRT catalytic site and occupy both the nicotinamide C-pocket and acetyl lysine substrate channel. Exhibits high selectivity over a panel of protein kinases, nuclelar receptors, GPCRs, and ion-channels (IC50 > 10 µM). Poorly affects hERG and cytochrome P450s (> 50 µM). Exhibits desirable stability in microsomal preparations (human CLint = 15.8 µL/min/mg, mouse CLint = 12.7 µL/min/mg) and high solubility (297 µM), and low LogD (2.73).
Catalogue Number505479
Brand Family Calbiochem®
Synonymspan SIRT1/2/3 Inhibitor, 4-(4-(2-Pivalamidoethyl)piperidin-1-yl)thieno[3,2-d]pyrimidine-6-carboxamide
References
ReferencesDisch, J.S., et al. 2013. J. Med. Chem. 57, 1275.
Product Information
CAS number1431411-60-7
FormPale yellow powder
Hill FormulaC₁₉H₂₇N₅O₂S
Chemical formulaC₁₉H₂₇N₅O₂S
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetSIRT1/2/3
Purity≥97% by HPLC
Physicochemical Information
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 6 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
5054790001 04055977243871

Documentation

SIRT1/2/3 pan Inhibitor - CAS 1431411-60-7 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Disch, J.S., et al. 2013. J. Med. Chem. 57, 1275.
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.

Revision22-November-2013 JSW
Synonymspan SIRT1/2/3 Inhibitor, 4-(4-(2-Pivalamidoethyl)piperidin-1-yl)thieno[3,2-d]pyrimidine-6-carboxamide
DescriptionA thienopyrimidinylcarboxamide that acts as a highly potent, reversible pan sirtuin (SIRT) inhibitor (IC50 = 15, 10, and 33 nM for SIRT1, 2, and 3, respectively). Shown to bind to the SIRT catalytic site and occupy both the nicotinamide C-pocket and acetyl lysine substrate channel. Exhibits high selectivity over a panel of protein kinases, nuclelar receptors, GPCRs, and ion-channels (IC50 > 10 µM). Poorly affects hERG and cytochrome P450s (> 50 µM). Exhibits desirable stability in microsomal preparations (human CLint = 15.8 µL/min/mg, mouse CLint = 12.7 µL/min/mg) and high solubility (297 µM), and low LogD (2.73).
FormPale yellow powder
Intert gas (Yes/No) Packaged under inert gas
CAS number1431411-60-7
Chemical formulaC₁₉H₂₇N₅O₂S
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (10 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 6 months at -20°C.
Toxicity Standard Handling
ReferencesDisch, J.S., et al. 2013. J. Med. Chem. 57, 1275.