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Cabotegravir

Cat. No. M10371
Cabotegravir Structure
Synonym:

S/GSK1265744; GSK744

Size Price Availability Quantity
10mg USD 50  USD50 In stock
25mg USD 105  USD105 In stock
50mg USD 187  USD187 In stock
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Quality Control & Documentation
Biological Activity

Cabotegravir, also known as S/GSK1265744 or GSK744, is potent HIV integrase inhibitor. Cabotegravir is an inhibitor of OAT1 (IC50 0.81 μM) and OAT3 (IC50 0.41 μM).

Chemical Information
Molecular Weight 405.35
Formula C19H17F2N3O5
CAS Number 1051375-10-0
Solubility (25°C) DMSO 14 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] Raphael J Landovitz, et al. Curr Opin HIV AIDS. The promise and pitfalls of long-acting injectable agents for HIV prevention

[2] Gary David Bowers, et al. Xenobiotica. Disposition and metabolism of cabotegravir: a comparison of biotransformation and excretion between different species and routes of administration in humans

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Keywords: Cabotegravir, S/GSK1265744; GSK744 supplier, HIV Protease, inhibitors, activators

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