613810

TNAP Inhibitor

The TNAP Inhibitor, also referenced under CAS 496014-13-2, controls the biological activity of TNAP. This small molecule/inhibitor is primarily used for Cell Structure applications.

• Synonym(s): TNAP Inhibitor, 2,5-Dimethoxy-N-(quinolin-3-yl)benzenesulfonamide, Tissue-Nonspecific Alkaline Phosphatase Inhibitor, MLS-0038949, MLS-0038949, 2,5-Dimethoxy-N-(quinolin-3-yl)benzenesulfonamide, Tissue-Nonspecific Alkaline Phosphatase Inhibitor
• Empirical Formula (Hill Notation): C₁₇H₁₆N₂O₄S
• CAS Number: 496014-13-2
• Molecular Weight: 344.38
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 50 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C17H16N2O4S/c1-22-14-7-8-16(23-2)17(10-14)24(20,21)19-13-9-12-5-3-4-6-15(12)18-11-13/h3-11,19H,1-2H3
• InChI key: JZSPHTPWUXNQGB-UHFFFAOYSA-N

Description

General description

A 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 (C_max = 1.5 µg/ml 1 hr after 4.13 mg/kg by s.c.).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and store at (4°C). Stock solutions are stable for up to 6 months at 4°C.

Other Notes

Dahl, R., et al. 2009. J. Med. Chem.52, 6919.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3