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Tariquidar methanesulfonate, hydrate

Cat. No. M14251
Tariquidar methanesulfonate, hydrate Structure
Synonym:

XR9576 methanesulfonate, hydrate

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Biological Activity

Tariquidar methanesulfonate, hydrate (XR9576 methanesulfonate, hydrate) is a potent and specific inhibitor of P-glycoprotein (P-gp) with a Kd of 5.1 nM.

Chemical Information
Molecular Weight 892.99
CAS Number 625375-83-9
Solubility (25°C) DMSO ≥ 180 mg/mL
Storage 2-8°C, dry, sealed
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] A Tomillero, et al. Methods Find Exp Clin Pharmacol. Gateways to clinical trials

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  Catalog
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Keywords: Tariquidar methanesulfonate, hydrate, XR9576 methanesulfonate, hydrate supplier, P-glycoprotein, inhibitors, activators


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