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GSK-7975A

Cat. No. M14198
GSK-7975A Structure
Size Price Availability Quantity
5mg USD 120  USD120 In stock
10mg USD 200  USD200 In stock
25mg USD 410  USD410 In stock
50mg USD 700  USD700 In stock
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Quality Control & Documentation
Biological Activity

GSK-7975A is a potent and orally available CRAC channel inhibitor.

Chemical Information
Molecular Weight 397.3
CAS Number 1253186-56-9
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] Sofie De Moudt, et al. GSK-7975A, an inhibitor of Ca 2+ release-activated calcium channels, depresses isometric contraction of mouse aorta

[2] Ningyong Xu, et al. Impact of Na+ permeation on collective migration of pulmonary arterial endothelial cells

[3] Isabel Galeano-Otero, et al. SARAF and Orai1 Contribute to Endothelial Cell Activation and Angiogenesis

[4] Xuexin Zhang, et al. Distinct pharmacological profiles of ORAI1, ORAI2, and ORAI3 channels

[5] Louise V Rice, et al. Characterization of selective Calcium-Release Activated Calcium channel blockers in mast cells and T-cells from human, rat, mouse and guinea-pig preparations

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  Catalog
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Keywords: GSK-7975A supplier, Calcium Channel, inhibitors, activators


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