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Doravirine

Cat. No. M20577
Doravirine Structure
Synonym:

MK1439

Size Price Availability Quantity
5mg USD 140  USD140 In stock
10mg USD 235  USD235 In stock
25mg USD 450  USD450 In stock
50mg USD 690  USD690 In stock
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Quality Control & Documentation
Biological Activity

Doravirine is a novel HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50 values of 12, 9.7, and 9.7 nM against the wild type (WT) and K103N and Y181C reverse transcriptase (RT) mutants, respectively, in a biochemical assay. Doravirine is highly specific with minimum off-target activities.

Chemical Information
Molecular Weight 425.75
Formula C17H11C1F3N5O3
CAS Number 1338225-97-0
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] Guangdi Li, et al. Acta Pharm Sin B. Approved HIV reverse transcriptase inhibitors in the past decade

[2] Alexander J Stockdale, et al. Curr Opin HIV AIDS. Doravirine: its role in HIV treatment

[3] No authors listed. Doravirine

[4] No authors listed. Doravirine

[5] Matt S Anderson, et al. Clin Pharmacokinet. A Two-Way Steady-State Pharmacokinetic Interaction Study of Doravirine (MK-1439) and Dolutegravir

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Keywords: Doravirine, MK1439 supplier, Reverse Transcriptase, inhibitors, activators


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