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613810 TNAP Inhibitor - CAS 496014-13-2 - Calbiochem

613810
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概述

Replacement Information

重要规格表

CAS #Empirical Formula
496014-13-2C₁₇H₁₆N₂O₄S

Products

产品目录编号包装 数量 / 包装
613810-10MGCN 10 mg
Description
OverviewA cell-permeable quinolinyl-benzenesulfonamide compound that acts as a potent reversible inhibitor against tissue-nonspecific (TN) alkaline phosphatase (AP) activity (IC50 = 190 nM) with CYP2C19 being the only other known target, while exhibiting little or no inhibitory activity in over 250 assays involving other enzymes, including, but not limited to, placental and intestinal APs (IC50 > 100 µM), PHOSPHO1 phosphatase, and NPP1 phosphodiesterase. Kinetic studies indicate that the inhibition is uncompetitive with respect to the phosphate donor substrate and noncompetitive with respect to the acceptor substrate, indicating an allosteric inhibition mechanism. Subcutaneous dosing in rats in vivo is reported to result in plasma inhibitor concentrations in the therapeutic range (Cmax = 1.5 µg/ml 1 hr after 4.13 mg/kg by s.c.).
Catalogue Number613810
Brand Family Calbiochem®
Synonyms2,5-Dimethoxy-N-(quinolin-3-yl)benzenesulfonamide, Tissue-Nonspecific Alkaline Phosphatase Inhibitor, MLS-0038949
References
ReferencesDahl, R., et al. 2009. J. Med. Chem. 52, 6919.
Product Information
CAS number496014-13-2
FormWhite solid
Hill FormulaC₁₇H₁₆N₂O₄S
Chemical formulaC₁₇H₁₆N₂O₄S
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥95% 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 store at (4°C). Stock solutions are stable for up to 6 months at 4°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
产品目录编号 GTIN
613810-10MGCN 04055977263572

Documentation

TNAP Inhibitor - CAS 496014-13-2 - Calbiochem MSDS

职位

物料安全数据表 (MSDS) 

TNAP Inhibitor - CAS 496014-13-2 - Calbiochem 分析证书

标题批号
613810

参考

参考信息概述
Dahl, R., et al. 2009. J. Med. Chem. 52, 6919.
数据表

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.

Revision19-April-2011 RFH
Synonyms2,5-Dimethoxy-N-(quinolin-3-yl)benzenesulfonamide, Tissue-Nonspecific Alkaline Phosphatase Inhibitor, MLS-0038949
DescriptionA cell-permeable quinolinyl-benzenesulfonamide compound that acts as a potent reversible inhibitor against tissue-nonspecific (TN) alkaline phosphatase (AP) activity (IC50 = 190 nM) with CYP2C19 being the only other known target, while exhibiting little or no inhibitory activity in over 250 assays involving other enzymes, including, but not limited to, placental and intestinal APs (IC50 >100 µM), PHOSPHO1 phosphatase, and NPP1 phosphodiesterase. Kinetic studies indicate that the inhibition is uncompetitive with respect to the phosphate donor substrate and noncompetitive with respect to the acceptor substrate, indicating an allosteric inhibition mechanism. Subcutaneous dosing in rats in vivo is reported to result in plasma inhibitor concentrations in the therapeutic range (Cmax = 1.5 µg/ml 1 hr after 4.13 mg/kg by s.c.).
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
CAS number496014-13-2
Chemical formulaC₁₇H₁₆N₂O₄S
Structure formulaStructure formula
Purity≥95% 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 store at (4°C). Stock solutions are stable for up to 6 months at 4°C.
Toxicity Standard Handling
ReferencesDahl, R., et al. 2009. J. Med. Chem. 52, 6919.