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Delavirdine mesylate

Cat. No. M2173
Delavirdine mesylate Structure
Synonym:

U-90152

Size Price Availability Quantity
100mg USD 162  USD180 In stock
500mg USD 414  USD460 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 552.67
Formula C22H28N6O3S.CH3SO3H
CAS Number 147221-93-0
Purity >98%
Solubility DMSO
Storage at -20°C
References

U-90152, a potent inhibitor of human immunodeficiency virus type 1 replication.
Dueweke TJ, et al. Antimicrob Agents Chemother. 1993 May;37(5):1127-31. PMID: 7685995.

In vitro inhibition of human immunodeficiency virus type 1 by a combination of delavirdine (U-90152) with protease inhibitor U-75875 or interferon-alpha.
Pagano PJ, et al. J Infect Dis. 1995 Jan;171(1):61-7. PMID: 7528253.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Delavirdine mesylate, U-90152 supplier, HIV Protease, inhibitors

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