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648494

Sigma-Aldrich

TRPC3 Channel Inhibitor III, Pyr10

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Synonym(s):
TRPC3 Channel Inhibitor III, Pyr10, N-(4-(3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)-4-methylbenzenesulfonamide
Empirical Formula (Hill Notation):
C18H13F6N3O2S
CAS Number:
Molecular Weight:
449.37
UNSPSC Code:
12352200
NACRES:
NA.77

Assay

≥98% (HPLC)

Quality Level

form

semisolid
solid

potency

720 nM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

orange-brown
white to off-white

solubility

DMSO: 100 mg/mL

shipped in

wet ice

storage temp.

2-8°C

General description

A cell-permeable pyrazole derivative that acts as a selective blocker of the transient receptor potential cation channel TRPC3-medated ROCE (receptor-operated Ca2+ entry) and inhibits Carbachol- (Cat. No. 212385) induced Ca2+ entry in TRPC3-expressing HEK293 cells (IC50 = 0.72 µM; by Fura-2), while exhibiting much reduced potency against Stim1 and Orai1-coupled CRAC (Ca2+ release-activated Ca2+) channel-mediated SOCE (store-operated Ca2+ entry) in RBL-2H3 cells (IC50 = 13.08 µM; by Fura-2). A great complement to Pyr2 (Cat. No. 203890), Pyr 3 (Cat. No. 648490), and Pyr6 (Cat. No. 203891) in Ca2+ signaling studies.
A cell-permeable pyrazole derivative that acts as a selective blocker of the transient receptor potential cation channel TRPC3-medated ROCE (receptor-operated Ca2+ entry) and inhibits Carbachol- (Cat. No. 212385) induced Ca2+ entry in TRPC3-expressing HEK293 cells (IC50 = 0.72 µM; by Fura-2; peak current density pA/pF = -1.01 and -18.50, respectively, with or without 3 µM Pyr10 by whole cell clamp), while exhibiting much reduced potency against Stim1 and Orai1-coupled CRAC (Ca2+ release-activated Ca2+) channel-mediated SOCE (store-operated Ca2+ entry) in RBL-2H3 cells (IC50 = 13.08 µM; by Fura-2; pA/pF = -4.39 and -7.50, respectively, with or without 3 µM Pyr10). A great complement to Pyr2 (Cat. No. 203890), Pyr 3 (Cat. No. 648490), and Pyr6 (Cat. No. 203891) in Ca2+ signaling studies.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
TRPC3
Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Schleifer, H. et al. 2012. Br. J. Pharmacol.167, 1712.

Legal Information

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

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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