ChemicalBook > Product Catalog >API >Synthetic Anti-infective Drugs >Antiviral drugs >Maraviroc

Maraviroc

Maraviroc Suppliers list
Company Name: Capot Chemical Co.,Ltd.
Tel: +86 (0)571-855 867 18
Email: sales@capotchem.com
Products Intro: Product Name:Maraviroc
CAS:376348-65-1
Purity:98%(Min,HPLC) Package:100g;1kg;5kg,10kg,25kg,50kg
Company Name: Henan DaKen Chemical CO.,LTD.
Tel: +86-371-55531817
Email: info@dakenchem.com
Products Intro: Product Name:Maraviroc
CAS:376348-65-1
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:376348-65-1
Purity:99% Package:500G;1KG;5KG;25KG
Company Name: Mainchem Co., Ltd.
Tel: +86-0592-6210733
Email: sales@mainchem.com
Products Intro: Product Name:Maraviroc
CAS:376348-65-1
Company Name: Nanjing ChemLin Chemical Industry Co., Ltd.
Tel: 025-83697070;product@chemlin.com.cn
Email: product@chemlin.com.cn
Products Intro: CAS:376348-65-1
Purity:98% Package:g-Kg Remarks:White powder

Lastest Price from Maraviroc manufacturers

  • Maraviroc
  • US $10.00 / KG
  • 2019-04-19
  • CAS:376348-65-1
  • Min. Order: 1KG
  • Purity: 99%
  • Supply Ability: 10mt
  • Maraviroc
  • US $2.00 / kg
  • 2019-04-01
  • CAS:376348-65-1
  • Min. Order: 1kg
  • Purity: 99%
  • Supply Ability: 100kg
Maraviroc Basic information
Product Name:Maraviroc
Synonyms:maroviroc;4,4-Difluoro-N-{(1S)-3-[3-(3-isopropyl-5-methyl-4H-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]oct-8-yl]-1-phenylpropyl}cyclohexanecarboxamide;Maraviroc(Selzentry);4,4-difluoro-N-[(1S)-3-[(1R,3R,5S)-3-[3-Methyl-5-(propan-2-yl)-4H-1,2,4-triazol-4-yl]-8-azabicyclo[3.2.1]octan-8-yl]-1-phenylpropyl]cyclohexane-1-carboxaMide;Celsentri;4,4-difluoro-N-((1R)-3-(3-(3-isopropyl-5-Methyl-4H-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl)-1-phenylpropyl)cyclohexanecarboxaMide;4,4-difluoro-N-(3-(3-(3-isopropyl-5-Methyl-4H-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl)-1-phenylpropyl)cyclohexanecarboxaMide;Maraviroc API
CAS:376348-65-1
MF:C29H41F2N5O
MW:513.67
EINECS:609-456-0
Product Categories:Anti-AIDS;Chiral Reagents;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Pfizer compounds;UK-427857, Celsentri;Other APIs
Mol File:376348-65-1.mol
Maraviroc Structure
Maraviroc Chemical Properties
Melting point 79-81°C
storage temp. Store at +4°C
solubility DMSO: >30mg/mL
pka7.3(at 25℃)
form white powder
optical activity[α]-15/D
CAS DataBase Reference376348-65-1(CAS DataBase Reference)
Safety Information
Hazard Codes Xn
Risk Statements 48/22
Safety Statements 22-36
WGK Germany 1
MSDS Information
Maraviroc Usage And Synthesis
Chemical PropertiesBrown Solid
UsesPotent, non-competitive CCR5 receptor antagonist; inhibits binding of HIV viral coat protein gp120. Antiviral
UsesMaraviroc is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM, respectively
DefinitionChEBI: A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 4,4-difluorocyclohexanecarboxylic acid and the primary amino group of (1S)-3-[(3-exo)-3-(3-isopropyl-5-methyl-4H-1,2,4- riazol-4-yl)-8-azabicyclo[3.2.1]oct-8-yl]-1-phenylpropylamine. An antiretroviral drug, it prevents the interaction of HIV-1 gp120 and chemokine receptor 5 (CCR5) necessary for CCR5-tropic HIV-1 to enter cells.
Acquired resistanceIn most patients (c. 60%) failure of response is associated with the selection of virus that can use CXCR4 as its entry co-receptor. Evidence for the selection of virus that continues to use CCR5 has also been described.
Pharmaceutical ApplicationsA spirodiketopiperazine formulated as tablets for oral use.
PharmacokineticsOral absorption: c. 33% (300 mg dose)
Cmax 150 mg twice daily: c. 332 μg/L*
Cmin 150 mg twice daily: c. 101 μg/L*
Plasma half-life: c. 13.2 h (30 mg iv administration)
Volume of distribution: c. 194 L
Plasma protein binding: c. 76%
Absorption
The absolute bioavailability of a 100 mg dose is 23% and is predicted to be 33% after a 300 mg dose. Co-administration of a 300 mg tablet and a high-fat meal has resulted in reduced Cmax and AUC by 33% in healthy volunteers. However, because no food restrictions were enacted during clinical trials, maraviroc may be taken with or without food.
Distribution
Animal experiments suggest low CSF concentrations around 10% of free plasma concentrations. It is not known whether it passes into breast milk. A study of genital tract secretions and vaginal tissue in healthy HIV-uninfected female volunteers suggest a concentration in cervicovaginal fluid more than four-fold higher than that in plasma.
Metabolism
It is a substrate for CYP3A4 and P-glycoprotein, but does not appear to inhibit or induce CYP3A4.
Excretion
Seventy-six and 19% of a radiolabeled maraviroc dose were recovered in the feces and urine, respectively.
Clinical UseTreatment of HIV infection (in combination with other antiretroviral drugs) in treatment-experienced patients
On November 20, 2009, the US Food and Drug Administration approved a supplemental new drug application to expand the indication for maraviroc to include combination antiretroviral treatment of treatmentnaive adults infected with CCR5-tropic HIV virus
Side effectsThere has been some concern that CCR5 blockade may result in decreased immune surveillance and a subsequent increased risk of development of malignancies (e.g. lymphomas). Genetic deficiency of the CCR5 co-receptor is also known to be a risk factor for the development of symptomatic West Nile virus infection. No evidence for an increase in either of these potential risks has so far emerged.
The toxicity profile appears relatively benign. The most common adverse events described so far include diarrhea, fatigue, headache and nausea. In placebo-controlled studies the only differences to emerge were fever (6% versus 4% in the placebo group) and headache (2% versus 6% with placebo). Discontinuation because of adverse events was uncommon and the same in both groups.
Maraviroc Preparation Products And Raw materials
Tag:Maraviroc(376348-65-1) Related Product Information
3-Hydroxymethyl Maraviroc 1-Piperidinepropanamine, -phenyl- 4-(3,5-DIMETHYL-4H-1,2,4-TRIAZOL-4-YL)PIPERIDINE Cyclohexanecarboxamide, 4,4-difluoro- Cyclohexanecarboxaldehyde, 4,4-difluoro- (9CI) Cyclohexanemethanamine, 4,4-difluoro- METHYL-(1-PHENYL-3-PYRROLIDIN-1-YL-PROPYL)-AMINE 3-(2,6-DIMETHYL-PIPERIDIN-1-YL)-PROPYLAMINE Maraviroc Methyl acrylate Methanol Kresoxim-methyl Methylparaben Basic Violet 1 Paraquat dichloride Acetonitrile Methyl acetate Methyl bromide