Maraviroc Inhibitor CAS No. 376348-65-1

Cat. No.	Name	Size	Price
KI0368	Maraviroc	5 mg	$120
	Maraviroc	25 mg	$420
	Maraviroc	100 mg	$1232

Chemical Characteristic

Product Name	Maraviroc
Synonyms	Selzentry, UK-427857
CAS No.	376348-65-1
Molecular Weight	513.67
Formula	C₂₉H₄₁F₂N₅O
Chemical Name	4,4-difluoro-N-((S)-3-(3-(3-isopropyl-5-methyl-4H-1,2,4-triazol-4-yl)-8-aza-bicyclo[3.2.1]octan-8-yl)-1-phenylpropyl)cyclohexanecarboxamide
Smiles	C1(CCC(CC1)(F)F)C(=O)NC(CCN1[C@H]2CC(C[C@@H]1CC2)n1c(nnc1C(C)C)C)c1ccccc1
Chemical Structure

Biological activities

Maraviroc is a selective CCR5 antagonist. The average IC90 of maraviroc against CCR5-tropic HIV-1 viruses is 2 nM. Maraviroc has potent anti-human immunodeficiency virus type 1 (HIV-1) activity and favorable pharmacological properties. Maraviroc blocks binding of viral envelope, gp120, to CCR5 to prevent the membrane fusion events necessary for viral entry. Maraviroc has no detectable in vitro cytotoxicity against a wide range of receptors and enzymes, including the hERG ion channel with IC50 of >10 μM. Maraviroc inhibits MIP-1α, MIP-1β and RANTES with IC50 of 3.3, 7.2 and 5.2 nM, respectively. Maraviroc inhibits not only MIP-1β-stimulated γ-S-GTP binding to HEK-293 cell membranes, but also the downstream event of chemokine-induced intracellular calcium redistribution, with IC50 ranging from 7 to 30 nM obtained against MIP-1β, MIP-1α and RANTES. Maraviroc suppresses the activity of HIV-1 envelope binding to CCR5 with an IC50 of 11 nM. Maraviroc inhibits HIV-1 Ba-L using either isolated multiple donor PBMC, single-donor PBMC and PM-1 cells with IC90 of 3.1, 1.8 and 1.1 nM, respectively. Maraviroc reveals potent antiviral activity against the primary CCR5-tropic HIV-1 isolates with geometric mean IC90 of 2.0 nM and ranging from 0.5 to 13.4 nM. The half-life values (t_{1/2) of maraviroc are 0.9 and 2.3 hours in rat and dog, resepctively. Following oral administration (2 mg/kg) of maraviroc to the dog, the C_{max (256 ng/mL) occurrs 1.5 hours post-dose, and the bioavailability is 40%. For the rat, approximately 30% of the administered dose is absorbed from the intestinal tract.^[1] Maraviroc has moderate lipophilicity(logD = 2.1) and basicity (pKa = 7.3), and a relatively highmolecular weight and hydrogen bonding capacity (oneH-bond donor and six H-bond acceptors). Oral maraviroc using intraportal vein sampling reveals that approximately 30% of the dose is absorbed by rats, while in dogs more than 70% is absorbed.^[2] Maraviroc is widely distributed, with a Vd of ~194 L. Maraviroc is moderately metabolized in the liver (65.3%), primarily via the cytochrome P450 3A4 isozyme. Maraviroc has an elimination t_{1/2 of 15.9 to 22.9 hours.^[3]}}}

References

[1] Dorr P, et al. Maraviroc (UK-427,857), a potent, orally bioavailable, and selective small-molecule inhibitor of chemokine receptor CCR5 with broad-spectrum anti-human immunodeficiency virus type 1 activity. Antimicrob Agents Chemother. 2005, 49(11): 4721-4732. [2] Meanwell NA, et al. Maraviroc, a chemokine CCR5 receptor antagonist for the treatment of HIV infection and AIDS. Curr Opin Investig Drugs. 2007, 8(8): 669-681. [3] Lieberman-Blum SS, et al. Maraviroc: a CCR5-receptor antagonist for the treatment of HIV-1 infection. Clin Ther. 2008, 30(7):1228-1250.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.

KareBay^TM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.

About

KareBay^TM Biochem
Sitemap
Blog

Custom Services

Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassry Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services

Biochemical Products

Small Molecule Inhibitors
Bioactive Compounds
Primary Antibodies
Peptides
Amino Acids
Reagents
Fluorescent dyes
Intermediates
PCR

KareBay^TM Biochem, Inc.
11 Deer Park Drive, Suite 102A
Monmouth Junction, NJ 08852

Telephone

: 732-823-1545

Fax

: 732-823-1349

product@karebaybio.com
service@karebaybio.com
support@karebaybio.com