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Delavirdine mesylate

Cat. No. M2173
Delavirdine mesylate Structure
Synonym:

U-90152

Size Price Availability Quantity
10mg USD 52  USD52 In stock
50mg USD 95  USD95 In stock
100mg USD 165  USD165 In stock
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Quality Control & Documentation
Biological Activity

Delavirdine mesylate (U-90152) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used as part of highly active antiretroviral therapy (HAART) for the treatment of human immunodeficiency virus (HIV) type 1. Delavirdine mesylate selectively inhibits HIV-1 reverse transcriptase (RNA-dependent DNA polymerase) over other cellular polymerases with IC50 values of 0.26, 440 and >550 μM for HIV-1 reverse transcriptase, DNA polymerase α and DNA polymerase δ. U-90152 (Delavirdine mesylate) blocked the replication in peripheral blood lymphocytes of 25 primary HIV-1 isolates with a mean 50% effective dose of 0.066 +/- 0.137 microM.

Chemical Information
Molecular Weight 552.67
Formula C22H28N6O3S.CH3SO3H
CAS Number 147221-93-0
Solubility (25°C) DMSO
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] Dueweke TJ, et al. Antimicrob Agents Chemother. U-90152, a potent inhibitor of human immunodeficiency virus type 1 replication.

[2] Pagano PJ, et al. J Infect Dis. In vitro inhibition of human immunodeficiency virus type 1 by a combination of delavirdine (U-90152) with protease inhibitor U-75875 or interferon-alpha.

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