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Atazanavir

Atazanavir Suppliers list
Company Name: Alpha Biopharmaceuticals Co., Ltd
Tel: 0086-411-39042497
Email: sales@alphabiopharm.com
Products Intro: Product Name:Atazanavir
CAS:198904-31-3
Purity:>98% HPLC Package:5mg; 25mg; 100mg; 1g; 5g; 25g;100g Remarks:B0259
Company Name: Capot Chemical Co.,Ltd.
Tel: +86-571-85586718
Email: sales@capotchem.com
Products Intro: Product Name:BMS-232632
CAS:198904-31-3
Purity:98%(Min,HPLC) Package:100g;1kg;5kg,10kg,25kg,50kg
Company Name: Henan DaKen Chemical CO.,LTD.
Tel: +86-371-66670886
Email: info@dakenchem.com
Products Intro: Product Name:Atazanavir
CAS:198904-31-3
Purity:99% Package:100g,500g,1KG,10KG,100KG
Company Name: Henan Tianfu Chemical Co.,Ltd.
Tel: 0371-55170693
Email: info@tianfuchem.com
Products Intro: CAS:198904-31-3
Purity:99% Package:500G;1KG;5KG;25KG
Company Name: Guangzhou PI PI Biotech Inc
Tel: ;
Email: sales@pipitech.com;87478684@qq.com
Products Intro: Product Name:Atazanavir
CAS:198904-31-3
Purity:90%+ Package:10mg, 25mg, 50mg, 100mg, Other scale please email Sales@pipitech.com Remarks:3,12-Bis(1,1-dimethylethyl)-8-hydroxy-4,11-dioxo-9-(phenylmethyl)-6-[[4-(2-pyridinyl)phenyl]methyl]-dimethyl Ester

Lastest Price from Atazanavir manufacturers

  • Atazanavir
  • US $0.00 / Kg/Bag
  • 2021-09-29
  • CAS:198904-31-3
  • Min. Order: 1KG
  • Purity: 99%min
  • Supply Ability: 100KGS
  • Atazanavir
  • US $10.00 / KG
  • 2021-07-29
  • CAS:198904-31-3
  • Min. Order: 1KG
  • Purity: 99%
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  • Atazanavir
  • US $15.00-10.00 / KG
  • 2021-07-13
  • CAS:198904-31-3
  • Min. Order: 1KG
  • Purity: 99%+ HPLC
  • Supply Ability: Monthly supply of 1 ton
Atazanavir Basic information
Product Name:Atazanavir
Synonyms:CS-534;BMS-232632-05; REYATAZ;BMS23263205;CS-2210;BMS 232632 - Atazanavir | CGP 73547;atazanvir;Atazanavir, >=99%;Atazanavir Enantiomer;Atazanavir Isomer Impurity
CAS:198904-31-3
MF:C38H52N6O7
MW:704.86
EINECS:812-543-8
Product Categories:Inhibitor;peptides;API;All Inhibitors;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Chiral Reagents
Mol File:198904-31-3.mol
Atazanavir Structure
Atazanavir Chemical Properties
Melting point 207-2090C
alpha D -47° (c = 1 in ethanol)
density 1.178±0.06 g/cm3(Predicted)
storage temp. -20°C
pka11.11±0.46(Predicted)
form powder
color white to beige
CAS DataBase Reference198904-31-3
Safety Information
Hazardous Substances Data198904-31-3(Hazardous Substances Data)
MSDS Information
Atazanavir Usage And Synthesis
DescriptionAtazanavir is an inhibitor of human immunodeficiency virus type 1 (HIV-1) protease, an enzyme that is essential for the processing of Gag and Gag-Pol polyproteins into structural and enzymatic proteins required for viral replication. It has a similar pharmacophore motif to the other six widely marketed HIV protease inhibitors, most of which are based upon a hydroxyethylamine template. Uniquely, it possesses an aza-peptide motif but maintains many similar pharmacophore elements including lipophilic moieties that presumably bind to S2, S1, S′1 , and S′2 positions. Atazanavir is pseudo-symmetric about the central template, incorporating D-tert-Leucine at both termini. This compound is synthesized in about seven steps, with a key coupling of the chiral epoxide (derived from phenylalanine and imparting one chiral center) and N-tert-boc-N′-(4-[2-pyridyl]benzyl)hydrazine. Removal of both tert-Boc groups and double acylation with methoxycarbonyl-tert-Leucine provides the product. Another synthesis of atazanavir entails ten steps and utilizes α-(tert-bocamino) phenylpropanal as a chiral intermediate. It is a potent inhibitor of indinavir-resistant and saquinavir-resistant strains of HIV-1 (IC50=0.03–0.1 and 0.04–0.1 μM, respectively). In 300 patients who had failed previous treatment, atazanavir (400 mg once daily) was compared to lopinavir (400 mg twice daily) and ritonavir (100 mg); both arms additionally receiving two non-reverse transcriptase inhibitors. After 24 weeks, HIV RNA levels of <400 copies/mL were noted in 61% of patients receiving atazanavir and 81% of those taking lopinavir/ritonavir. After 96 weeks of therapy with atazanavir, HIV RNA copy levels were found to be <400 and <50 in 80 and 58% of patients, respectively. A study of the cross-resistance profile relative to other protease inhibitors using a panel of 551 clinical isolates (without prior atazanavir exposure but with cross-resistance to one or two other protease inhibitors; the majority had resistance to nelfinavir) showed that greater than 80% retained susceptibility to atazanavir. All of the resistant isolates from patients taking atazanavir had an I50 L substitution. The recommended dosage of atazanavir is 400 mg once daily. It has a mean half-life range of 7.9–6.5 h with about 60% bioavailability and moderate plasma protein binding (86% albumin and 89% alpha-1- acid glycoprotein (AAG)). Atazanavir was well tolerated in clinical studies and it displayed minimal lipid modulation when tested in combination with two non-reverse transcriptase inhibitors. Atazanavir had no effect on total cholesterol, low-density lipoprotein, and triglyceride levels when compared with other protease inhibitors that caused sustained elevations in these lipid levels.
Chemical PropertiesCrystalline Solid
OriginatorNovartis (US)
UsesAtazanavir is a novel azapeptide protease inhibitor (PI)
Usesenzyme inhibitor
UsesAtazanavir is a novel azapeptide HIV protease inhibitor (PI). Antiviral.
UsesAtazanavir is an inhibitor of HIV-1 protease (EC50 = 2.6 nM). In isolated cells, it has additive to moderately synergistic antiviral effects when combined with other antiretroviral drugs. As a result, it is commonly used in vivo in combination therapy for HIV-1 infection. Atazanavir competitively inhibits UDP-gluronosyltransferase, which conjugates bilirubin for clearance, leading to hyperbilirubinemia in a significant portion of those receiving atazanavir therapy.
DefinitionChEBI: A heavily substituted carbohydrazide that is an antiretroviral drug of the protease inhibitor (PI) class used to treat infection of human immunodeficiency virus (HIV).
Brand nameReyataz (Bristol-Myers Squibb).
Acquired resistanceMutations at positions 50 (I50L), 84 (I84V) and 88 (N88S) of the protease gene are associated with resistance.
General DescriptionAtazanavir is an antiretroviral agent that has been approvedby the FDA for use in combination with other anti-RTagents for the treatment of HIV infections. The drug is alwaysused in combination with RT inhibitors.
Pharmaceutical ApplicationsAn azapeptide formulated as the sulfate for oral use.
Mechanism of actionAtazanavir is dosed orally once daily, thus reducing "pill burden," and it appears to have minimal impact on lipid parameters but does increase total bilirubin. The drug is well absorbed when administered orally with food (bioavailability, ~68%). The drug is highly bound to plasma protein (86%) and is metabolized by CYP3A isoenzyme. Atazanavir is a moderate inhibitor of CYP3A, and potential drug–drug interactions are possible with CYP3A inhibitors and inducers.
PharmacokineticsOral absorption: c. 68%
Cmax 400 mg once daily: c. 3.15 μg/L
300 mg + ritonavir 100 mg once daily: c. 4.47 μg/L
Cmin 400 mg once daily: c. 0.27 μg/L
300 mg + ritonavir 100 mg once daily: c. 0.65 μg/L
Plasma half-life: c. 8.6 h (300 mg+ ritonavir 100 mg)
Volume of distribution: c. Not known/available
Plasma protein binding: c. 86%
Absorption
Administration with food enhances bioavailability and reduces pharmacokinetic variability. Absorption is dependent on gastric pH. It should be given separately from proton-pump inhibitors or H2-receptor antagonists. Buffered or entericcoated formulations should be given (with food) 2 h before or 1 h after co-administration of didanosine.
Distribution
It penetrates moderately well into the CNS. The semen:plasma ratio is 0.11–4.42. It is distributed into breast milk.
Metabolism
It is extensively metabolized by CYP3A4. Administration with ritonavir prevents metabolization and enhances the pharmacokinetic profile.
Excretion
Following a single 400 mg dose, 79% and 13% of the dose was recovered in the feces and urine, respectively. It should be used with caution in the presence of mild hepatic impairment and should not be used in patients with more severe hepatic impairment.
Clinical UseTreatment of HIV infection (in combination with other antiretroviral drugs)
Side effectsThe most common adverse reactions (≥2%) are nausea, jaundice/ scleral icterus, rash, headache, abdominal pain, vomiting, insomnia, peripheral neurological symptoms, dizziness, myalgia, diarrhea, depression and fever.
Tag:Atazanavir(198904-31-3) Related Product Information
Atazanavir Sulfate,Atazanavir Sulphate Des-N-(methoxycarbonyl)-L-tert-leucine Atazanavir-d5 Trihydrochloride ATAZANAVIR-D5, BISULFATE SALT Atazanavir, Bisulfate Salt See A790051 Des-N-(methoxycarbonyl)-L-tert-leucine Bis-Boc Atazanavir-d5 Atazanavir-D5 L-TERT-LEUCINE METHYLAMIDE Des-N-(methoxycarbonyl)-L-tert-leucine Atazanavir Trihydrochloride N-METHYL-N-(4-PYRIDIN-2-YLBENZYL)AMINE Atazanavir CHLOROPHOSPHONAZO III Methyl Parathion-methyl Bensulfuron methyl Thiophanate-methyl Methyl acrylate Methylparaben Kresoxim-methyl