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GSK1702934A 

Cat. No. M30920
GSK1702934A  Structure
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Biological Activity

GSK1702934A is a selective TRPC3 agonist. GSK1702934A modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3.

Chemical Information
Molecular Weight 395.52
Formula C22H25N3O2S
CAS Number 924377-85-5
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage Powder -20°C
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] Gaëlle Rached, et al. Adv Sci (Weinh). TRPC3 Regulates Islet Beta-Cell Insulin Secretion

[2] Kimber L Boekell, et al. PLoS One. Trpc6 gain-of-function disease mutation enhances phosphatidylserine exposure in murine platelets

[3] Pei-Lin Yang, et al. J Biol Chem. GSK1702934A and M085 directly activate TRPC6 via a mechanism of stimulating the extracellular cavity formed by the pore helix and transmembrane helix S6

[4] Oleksandra Tiapko, et al. Chem Sci. Lipid-independent control of endothelial and neuronal TRPC3 channels by light

[5] Bernhard Doleschal, et al. Cardiovasc Res. TRPC3 contributes to regulation of cardiac contractility and arrhythmogenesis by dynamic interaction with NCX1

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Keywords: GSK1702934A  supplier, TRP Channel, inhibitors, activators


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