Free shipping on all orders over $ 500

Atazanavir Sulfate

Cat. No. M1657
Atazanavir Sulfate Structure
Synonym:

BMS-232632, Reyataz, CGP-73547

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL USD 68  USD68 In stock
5mg USD 40  USD40 In stock
10mg USD 65  USD65 In stock
25mg USD 110  USD110 In stock
50mg USD 180  USD180 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

Atazanavir sulfate (BMS-232632, Reyataz) is a sulfate salt form of atazanavir (BMS-232632) that is an highly potent HIV protease inhibitor with EC50 and EC90 of 2.6~5.3 nM and 9~15 nM in cell culture. Atazanavir (BMS-232632) blocks the cleavage of viral precursor proteins in HIV-infected cells. Atazanavir (BMS-232632) is generally more potent than the five currently approved HIV-1 Prt inhibitors. Furthermore, Atazanavir (BMS-232632) is highly selective for HIV-1 Prt and exhibits cytotoxicity only at concentrations 6,500- to 23, 000-fold higher than that required for anti-HIV activity.

Protocol (for reference only)
Cell Experiment
Cell lines MT-2 and CEM-SS cells, monocytes/macrophages, and PBMCs
Preparation method To determine cytotoxicity, host cells were incubated in the presence of serially diluted inhibitors for 6 days and cell viability was quantitated using an XTT [2,3-bis(2-methoxy-4-nitro-5-sulfophenyl-2H-tetrazolium-5-carboxanilide] assay to calculate the 50% cytotoxic concentrations (CC50s) (42). To assess the effect of human serum proteins on antiviral activity, the 10% fetal calf serum normally used for assays was replaced with 40% adult human serum (Sigma) or 1 mg of α1-acid glycoprotein (Sigma)/ml.
Concentrations 0~100 μM
Incubation time 6 days
Animal Experiment
Animal models male Wistar rats model
Formulation 50% ethanol-50% normal saline
Dosages 80mg/kg/min
Administration constant intravenous infusion
Chemical Information
Molecular Weight 802.93
Formula C38H52N6O7.H2SO4
CAS Number 229975-97-7
Solubility (25°C) DMSO 100 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] Cavaco-Silva et al. J Antimicrob Chemother. Mutations selected in HIV-2-infected patients failing a regimen including atazanavir.

[2] Rivero-Juarez et al. AIDS Res Hum Retroviruses. Atazanavir-based antiretroviral therapy is associated with higher hepatitis C virus viral load in HIV/hepatitis C virus patients.

[3] Gibellini et al. AIDS. The protease inhibitor atazanavir triggers autophagy and mitophagy in human preadipocytes.

[4] Di Biagio et al. J Antimicrob Chemother. Duration of first-line antiretroviral therapy with tenofovir and emtricitabine combined with atazanavir/ritonavir, efavirenz or lopinavir/ritonavir in the Italian ARCA cohort.

[5] Rusconi et al. BMC Infect Dis. Efficacy and safety of a dual boosted protease inhibitor-based regimen, atazanavir and fosamprenavir/ritonavir, against HIV: experience in a pediatric population.

[6] Hruz PW, et al. Antimicrob Agents Chemother. GS-8374, a novel HIV protease inhibitor, does not alter glucose homeostasis in cultured adipocytes or in a healthy-rodent model system.

[7] Robinson BS, et al. Antimicrob Agents Chemother. BMS-232632, a highly potent human immunodeficiency virus protease inhibitor that can be used in combination with other available antiretroviral agents.

Related HIV Protease Products
Arg-Val-(Nle-p-nitro)-Phe-Glu-Ala-Nle-NH2

Arg-Val-(Nle-p-nitro)-Phe-Glu-Ala-Nle-NH2 is a fluorogenic substrate of HIV-1 protease.

Ac-Ser-Gln-Asn-Tyr-Pro-Val-Val-NH2

Ac-Ser-Gln-Asn-Tyr-Pro-Val-Val-NH2 is a substrato peptídico of HIV-1 protease.

HIV-1, HIV-2 Protease Substrate

HIV-1, HIV-2 Protease Substrate is the substrate of HIV-1, HIV-2 protease.

HIV Protease Substrate IV

HIV Protease Substrate IV is a substrate of HIV protease.

Herpes virus inhibitor 2

Herpes virus inhibitor 2 is a herpes virus inhibitor and disrupts herpes virus ribonucleotide reductase quaternary structure.

  Catalog
Abmole Inhibitor Catalog




Keywords: Atazanavir Sulfate, BMS-232632, Reyataz, CGP-73547 supplier, HIV Protease, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.