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Ro24-7429 

Cat. No. M28317
Ro24-7429  Structure
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Biological Activity

Ro24-7429 is a potent and orally active HIV-1 transactivator protein Tat antagonist. Ro24-7429 is also a runt-related transcription factor 1 (RUNX1) inhibitor. Ro24-7429 has anti-HIV, antifibrotic and anti-inflammatory effects.

Chemical Information
Molecular Weight 272.73
Formula C14H13ClN4
CAS Number 139339-45-0
Form Solid
Solubility (25°C) DMSO 62.5 mg/mL (ultrasonic)
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] A Ehret, et al. J Virol. Resistance of chimpanzee T cells to human immunodeficiency virus type 1 Tat-enhanced oxidative stress and apoptosis

[2] B J Dezube, et al. J Cardiovasc Pharmacol. Pentoxifylline for the treatment of HIV infection and its complications

[3] H Maehr, et al. Bioorg Med Chem. An alternate synthesis of the Tat-antagonist 7-chloro-N-methyl-5-(1H-pyrrol-2-yl)-3H-1,4-benzodiazepin-2-amine

[4] M Margalith, et al. AIDS Res Hum Retroviruses. Interactions between HIV-1 and cytomegalovirus in human osteosarcoma cells carrying both viruses

[5] M Braddock, et al. J Virol. Inhibition of human immunodeficiency virus type 1 Tat-dependent activation of translation in Xenopus oocytes by the benzodiazepine Ro24-7429 requires trans-activation response element loop sequences

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Keywords: Ro24-7429  supplier, HIV Protease, inhibitors, activators


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