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Pyr10

Cat. No. M14285
Pyr10 Structure
Size Price Availability Quantity
5mg USD 64  USD64 In stock
10mg USD 98  USD98 In stock
50mg USD 360  USD360 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 449.37
CAS Number 1315323-00-2
Solubility (25°C) DMSO 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Anna Creismas, et al. TRPC3, but not TRPC1, as a good therapeutic target for standalone or complementary treatment of DMD

[2] Janyerson Dannys Pereira da Silva, et al. Pharmacological characterization of the calcium influx pathways involved in nitric oxide production by endothelial cells

[3] Dae-Wi Kim, et al. Comparative genomic analysis of pyrene-degrading Mycobacterium species: Genomic islands and ring-hydroxylating dioxygenases involved in pyrene degradation

[4] Ins lvarez-Miguel, et al. Differences in TRPC3 and TRPC6 channels assembly in mesenteric vascular smooth muscle cells in essential hypertension

[5] H Schleifer, et al. Novel pyrazole compounds for pharmacological discrimination between receptor-operated and store-operated Ca(2+) entry pathways

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  Catalog
Abmole Inhibitor Catalog




Keywords: Pyr10 supplier, TRP Channel, inhibitors, activators

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