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Sigma-Aldrich

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

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About This Item

Empirical Formula (Hill Notation):
C17H16N2O4S
CAS Number:
496014-13-2
Molecular Weight:
344.38
UNSPSC Code:
12352200
NACRES:
NA.77

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

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 (Cmax = 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

wgk_germany

WGK 3

Certificates of Analysis (COA)

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Andrew C Yang et al.
Nature, 583(7816), 425-430 (2020-07-03)
The vascular interface of the brain, known as the blood-brain barrier (BBB), is understood to maintain brain function in part via its low transcellular permeability1-3. Yet, recent studies have demonstrated that brain ageing is sensitive to circulatory proteins4,5. Thus, it is

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