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Pyr10

  Cat. No.:  DC23945   Featured
Chemical Structure
1315323-00-2
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Field of application
Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels[1].
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1315323-00-2
Chemical Name: Benzenesulfonamide, N-[4-[3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-4-methyl-
Synonyms: Pyr-10;Pyr 10
SMILES: O=S(=O)(NC1C=CC(N2C(C(F)(F)F)=CC(C(F)(F)F)=N2)=CC=1)C1C=CC(C)=CC=1
Formula: C18H13F6N3O2S
M.Wt: 449.3701
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [1]. Schleifer H, et al. Novel pyrazole compounds for pharmacological discrimination between receptor-operated and store-operated Ca(2+) entry pathways. Br J Pharmacol. 2012 Dec;167(8):1712-1722. [2]. Saliba Y, et al. Transient Receptor Potential Canonical 3 and Nuclear Factor of Activated T Cells C3 Signaling Pathway Critically Regulates Myocardial Fibrosis. Antioxid Redox Signal. 2019 Jun 1;30(16):1851-1879.
Description: Pyr10 is a novel TRPC3-selective inhibitor, IC50 of Ca2+ influx inhibition by Pyr10 in carbachol-stimulated YFP-TRPC3-transfected HEK293 cells for ROCE and thapsigargin-depleted native RBL-2H3 cells for SOCE is 0.72 uM and 13.08 uM.
Target: IC50 value: 0.72 uM (TRPC3-ROCE), 13.08 uM (SOCE) [1] Target: TRPC3
In Vitro: Pyr10 displays substantial selectivity for TRPC3-mediated responses (18-fold) and the selective block of TRPC3 channels by Pyr10 barely affected mast cell activation.[1]
References: [1]. Schleifer H, et al. Novel pyrazole compounds for pharmacological discrimination between receptor-operated and store-operated Ca(2+) entry pathways. Br J Pharmacol. 2012 Dec;167(8):1712-1722. [2]. Obermayer D, et al. Microwave-assisted and continuous flow multistep sy
MSDS
COA
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2018-0101
2018-0101
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