Maraviroc

SKU: orb1301149

Description

Maraviroc is a selective CCR5 antagonist that potently inhibits the binding of chemokines MIP-1α, MIP-1β, and RANTES. It blocks HIV-1 entry via CCR5 and is widely used in virology research for studying viral entry mechanisms, coreceptor tropism, and in antiviral assays both in vitro and in vivo.

Research Area

Immunology & Inflammation, Infectious Disease & Virology, Pharmacology & Drug Discovery, Protein Biochemistry

Key Properties

• CAS Number: 376348-65-1
• MW: 513.67
• Purity: >99.99% (May vary between batches)
• Formula: C₂₉H₄₁F₂N₅O
• SMILES: CC(C)c1nnc(C)n1[C@@H]1C[C@@H]2CC[C@H](C1)N2CC[C@H](NC(=O)C1CCC(F)(F)CC1)c1ccccc1
• Target: HIV Protease,CCR
• Solubility: DMSO:255 mg/mL (496.43 mM);Ethanol:51.4 mg/mL (100.06 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (9.73 mM)

Bioactivity

• Target IC50:
  R5 HIV-1 (Ba-L):6.4 nM|MIP-1α:3.3 nM|HeLa P4 cells:0.2 nM|MIP-1β:7.2 nM|HOS cells:2 nM|RANTES:5.2 nM|HIV-1 (Ba-L):1.1 nM (in PM-1 cells)|CHO cells:1.4 nM|TZM-bl cells:0.0002 µM
• In Vivo:
  In canines, oral administration of Maraviroc at a dosage of 2 mg/kg resulted in peak concentrations of 256 ng/ml at 1.5 hours with a bioavailability of 40%. In rats, the half-life of Maraviroc was approximately 0.9 hours, with around 30% of the administered dose being absorbed from the intestine. Experiments in female RAG-hu mice demonstrated that Maraviroc provided complete protection against HIV-1 infection.
• In Vitro:
  Maraviroc (IC50=7-30 nM) inhibits the downstream intracellular calcium redistribution induced by chemokines in MIP-1β, MIP-1α, and RANTES.
• Cell Research:
  Drug susceptibility assays are performed in 24-well tissue culture plates. Duplicate eight-point dilution series of Maraviroc are prepared in DMSO and medium to yield a final DMSO concentration of 0.1% (vol/vol) in the assay. PHA-stimulated PBMC or PM-1 cells are infected with virus for 1 hour at 37 °C. Cells are subsequently washed once, and 3.6 × 105 PBMC or 2.0 × 105 PM-1 cells are added to each well of assay plates containing diluted Maraviroc. Plates are incubated for 5 days (lab-adapted strains) or 7 days (primary isolates) at 37 °C in a humidified 5% CO2 (vol/vol) atmosphere.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Celsentri, CC chemokine receptor, CCR, Human immunodeficiency virus, HIVProtease, HIV Protease, HIV, Maraviroc, Inhibitor, inhibit, MIP-1β, MIP-1α, RANTES, Selzentry, UK 427857, UK427857, UK-427857

Compound Identifiers

PubChem CID

3002977