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Pyr10

Product NamePyr10
CAS1315323-00-2
MFC18H13F6N3O2S
MW449.37
EINECS
MOL File1315323-00-2.mol

Chemical Properties

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
InChI	1S/C18H13F6N3O2S/c1-11-2-8-14(9-3-11)30(28,29)26-12-4-6-13(7-5-12)27-16(18(22,23)24)10-15(25-27)17(19,20)21/h2-10,26H,1H3
InChIKey	CVALMMCIOLXHDM-UHFFFAOYSA-N
SMILES	FC(F)(F)c1[n](nc(c1)C(F)(F)F)c2ccc(cc2)N[S](=O)(=O)c3ccc(cc3)C

Safety Information

WGK Germany	WGK 3
Storage Class	11 - Combustible Solids

Usage And Synthesis

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 novel, selective 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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