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Bictegravir

Cat. No. M9113
Bictegravir Structure
Synonym:

GS-9883

Size Price Availability Quantity
1mg USD 40  USD40 In stock
5mg USD 70  USD70 In stock
10mg USD 120  USD120 In stock
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Quality Control & Documentation
Biological Activity

Bictegravir (GS-9883) is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.

Chemical Information
Molecular Weight 449.38
Formula C21H18F3N3O5
CAS Number 1611493-60-7
Solubility (25°C) DMSO: ≥ 60 mg/mL (Need ultrasonic and warming)
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] Chloe Orkin, et al. Fixed-dose combination bictegravir, emtricitabine, and tenofovir alafenamide versus dolutegravir-containing regimens for initial treatment of HIV-1 infection: week 144 results from two randomised, double-blind, multicentre, phase 3, non-inferiority trials

[2] No authors listed. Bictegravir

[3] Emma D Deeks. Bictegravir/Emtricitabine/Tenofovir Alafenamide: A Review in HIV-1 Infection

[4] No authors listed. Bictegravir

[5] Vincenzo Spagnuolo, et al. Bictegravir

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Keywords: Bictegravir, GS-9883 supplier, Integrase, inhibitors, activators


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