| Identification | Back Directory | [Name]
Pyr10 | [CAS]
1315323-00-2 | [Synonyms]
Pyr10
PYR-10;PYR 10
Pyr10 >=98% (HPLC)
N-{4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl}-4-methylbenzenesulfonamide
Benzenesulfonamide, N-[4-[3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-4-methyl- | [Molecular Formula]
C18H13F6N3O2S | [MDL Number]
MFCD28411625 | [MOL File]
1315323-00-2.mol | [Molecular Weight]
449.37 |
| Chemical Properties | Back Directory | [Melting point ]
105-107 °C | [Boiling point ]
470.1±55.0 °C(Predicted) | [density ]
1.47±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (222.53 mM);Water : < 0.1 mg/mL (insoluble) | [form ]
Solid | [pka]
6.98±0.10(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
Pyr10 is a novelselective inhibitor of the transient receptor potential channel TRPC3. Pyr10 blocks carbachol-induced calcium entry into TRPC3-transfected HEK293 cells (IC50 = 0.72 μM)with significantly lower activity against STIM1/Orai1 mediated release of calcium from endoplasmic reticulum (store operated calcium entry) in BRL-2H3 cells (IC50 = 13.08 μM). | [in vivo]
Genetic deletion (TRPC3-/-) and pharmacological channel blockade with Pyr10 blunts ventricular cardiac fibroblast activation and myocardial fibrosis in N(ω)-nitro-l-arginine methyl ester (l-NAME) hypertensive mice[2]. | [IC 50]
TRPC3: 0.72 μM (IC50) | [storage]
Store at -20°C | [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. DOI:10.1111/j.1476-5381.2012.02126.x
[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. DOI:10.1089/ars.2018.7545 |
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| Company Name: |
Musechem
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| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
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