Free shipping on all orders over $ 500

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
Free Delivery on orders over USD 500 Bulk Inquiry?

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

Related TRP Channel Products
N-Oleoyl glutamine

N-oleoyl-glutamine is a PM20D1-regulated N-acyl amino acids (NAAs).

N-Oleoyl valine

N-Oleoyl valine is a N-acyl valine compound that acts as a TRPV3 receptor antagonist.

TAT-M2NX

TAT-M2NX (tatM2NX) is a TRPM2 inhibitor with specific neuroprotective activity in male mice.

SOR-C13

SOR-C13, a carboxy-terminal truncated peptide, is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM.

GsMTx4 TFA

GsMTx4 TFA is a spider venom peptide that selectively inhibits cation permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. In addition, GsMTx4 TFA blocks cation-selective stretch-activated channels (SACs) and attenuates lysophosphatidylcholine (LPC)-induced astrocytotoxicity and microglial cell reactivity.

  Catalog
Abmole Inhibitor Catalog




Keywords: Pyr10 supplier, TRP Channel, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.