1. GPCR/G Protein
  2. CCR

Maraviroc (Synonyms: UK-427857; Selzentry; Celsentri)

Cat. No.: HY-13004 Purity: 99.34%
Handling Instructions

Maraviroc is a selective CCR5 antagonist, inhibits MIP-1α (IC50, 3.3 nM), MIP-1β (IC50, 7.2 nM), and RANTES (IC50, 5.2 nM) binding to cell membrane preparations of CCR5-expressing HEK-293.

For research use only. We do not sell to patients.
Maraviroc Chemical Structure

Maraviroc Chemical Structure

CAS No. : 376348-65-1

Size Stock
10 mM * 1 mL in DMSO Get quote
5 mg USD 60 Get quote
10 mg USD 108 Get quote
50 mg USD 348 Get quote
100 mg USD 624 Get quote

* Please select Quantity before adding items.

Customer Review

    Maraviroc purchased from MCE. Usage Cited in: Front Pharmacol. 2017 May 3;8:230.

    Inhibition of total and phosphorylation levels of CCR5, PKC δ, and p38 in MIP-1β-induced U937 cells by WTD. Cells are pretreated with PMA for 48 h and then incubated with or without WTD or MVC for 2 h. Subsequently, cells are stimulated with MIP-1β (25 nM). After 10 min of stimulation, cells are collected to detect total and phosphorylated (p) CCR5 (A), PKC δ (B), and p38 (C) by western blotting.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References


    Maraviroc is a selective CCR5 antagonist, inhibits MIP-1α (IC50, 3.3 nM), MIP-1β (IC50, 7.2 nM), and RANTES (IC50, 5.2 nM) binding to cell membrane preparations of CCR5-expressing HEK-293.

    IC50 & Target

    IC50: 3.3 nM (MIP-1α), 7.2 nM (MIP-1β), 5.2 nM (RANTES)[1]

    In Vitro

    Maraviroc is a selective CCR5 antagonist with potent anti-human immunodeficiency virus type 1 (HIV-1) activity. Maraviroc inhibits the downstream event of chemokine-induced intracellular calcium redistribution, with IC50s ranging from 7 to 30 nM obtained against MIP-1β, MIP-1α and RANTES. Maraviroc is active (IC90) at low nanomolar concentrations against HIV-1 Ba-L (a lab-adapted R5 strain) when measured in a 5-day antiviral assay using either isolated multiple (pooled) donor PBMC (IC90, 3.1 nM), single-donor PBMC (IC90, 1.8 nM) or PM-1 cells (IC90, 1.1 nM)[1].

    In Vivo

    Clearance values are moderate to high in both rat and dog species following i.v. administration (74 and 21 mL/min/kg, respectively). Maraviroc also has a moderate volume of distribution in both species (4.3 to 6.5 liters/kg). The half-life values of maraviroc are 0.9 h in the rat and 2.3 h in the dog. Following oral administration (2 mg/kg) to the dog, the Cmax(256 ng/mL) occurs 1.5 h. post-dose, and the bioavailability is 40%. For the rat, investigation of the concentrations obtain in the portal vein following oral administration indicated that approximately 30% of the administered dose is absorbed from the intestinal tract[1]. In the DSS/TNBS colitis and in the transfer model, Maraviroc attenuates development of intestinal inflammation by selectively reducing the recruitment of CCR5 bearing leukocytes[2]

    Clinical Trial
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 1.9468 mL 9.7339 mL 19.4678 mL
    5 mM 0.3894 mL 1.9468 mL 3.8936 mL
    10 mM 0.1947 mL 0.9734 mL 1.9468 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay

    Binding of 125I-labeled MIP-1α, MIP-1β, and RANTES to CCR5 is measured essentially using intact HEK-293 cells stably expressing the receptor or membrane preparations thereof. Briefly, cells are resuspended in binding buffer (50 mM HEPES containing 1 mM CaCl2, 5 mM MgCl2, and 0.5% bovine serum albumin [BSA] and adjusted to pH 7.4) to a density of 2×106 cells/mL. For membrane preparations, phosphate-buffered saline (PBS)-washed cells are resuspended in lysis buffer (20 mM HEPES, 1 mM CaCl2, 1 tablet COMPLETE per 50 mL, pH 7.4; Boehringer) prior to homogenization in a Polytron hand-held homogenizer, ultracentrifugation (40,000× g for 30 min), and resuspension in binding buffer to a protein concentration of 0.25 mg/mL (12.5 μg of membrane protein is used in each well of a 96-well plate). 125I-radiolabeled MIP-1α, MIP-1β, and RANTES are prepared and diluted in binding buffer to a final concentration of 400 pM in the assay. Appropriate maraviroc dilutions are added to each well to a final volume of 100 μL, the assay plates incubated for 1 h, and the contents filtered through preblocked and washed Unifilter plates which are counted following overnight drying[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay

    Maraviroc is prepared in DMSO and stored, and then diluted with appropriate media (DMSO 0.1%) before use[1].

    HEK-293 cell aliquots (100 μL at 1×106 cells/mL) are plated into poly-D-lysine-coated plates and incubated at 37°C overnight. A 1:1 mix of soluble recombinant human CD4 (sCD4) (diluted to 4.5 nM in culture medium) and HIV-1 gp120 is incubated at room temperature for 15 min prior to its addition to PBS-washed cells in the presence of dilutions of maraviroc to enable IC50 determination. The assay plates are incubated at 37°C for 1 h and washed. Eu3+-labeled anti-gp120 antibody (1/500 dilution in assay buffer) is added to each well (50 μL) and incubated for 1 h. The plate is washed three times with wash buffer prior to the addition of enhancement solution (200 μL/well) and measurement of Eu3+ fluorescence (Victor2multilabel counter; “Europium” protocol). Nonspecific binding is taken as the fluorescence measured for gp120 incubated with cells in the absence of preincubation with sCD4[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration

    Maraviroc is dissolved in DMSO and then diluted with PBS or saline.

    Rats and Dogs[1]
    Preclinical pharmacokinetic studies are carried out with maraviroc following a single intravenous and oral administration to both male Sprague-Dawley rats (1 mg/kg of body weight given intravenously [i.v.] and 10 mg/kg given orally [p.o.]; n=2) and male beagle dogs (0.5 mg/kg i.v. and 2 mg/kg p.o; n=4). Plasma samples are taken for up to 24 h postdose, and the concentrations of unchanged maraviroc are determined using a specific high-performance liquid chromatography-tandem mass spectrum assay.
    Splenocytes are collected from 6-10 week old CCR5-/- mice or wild-type controlmice (n=8 per group) and naive CD4+ CD45RBhigh T-cells are isolated by cell sorting. A total of 3×105 CD45RBhigh cells are then injected intravenously into Rag1-/- mice that are subsequently weighed and assessed for fecal score every 20 days to evaluate IBD development. To investigate whether Maraviroc rescues from intestinal inflammation induced by transfer colitis, Rag1-/- mice are injected with CD4+ CD45RB-/- T-cells and 34 days later randomized into either a control group (no further treatment, n=6) or treatment with Maraviroc, 50 mg/kg/d Maraviroc per os (n=4) for 3 weeks, 5 d/week. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight




    CAS No.



    O=C(C1CCC(F)(F)CC1)N[[email protected]](C2=CC=CC=C2)CCN3[[email protected]]4C[[email protected]@H](N5C(C)=NN=C5C(C)C)C[[email protected]@H]3CC4

    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    Maraviroc is dissolved in sterilized PBS[4].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.


    Purity: 99.34%

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name



    Applicant name *


    Email address *

    Phone number *


    Organization name *

    Country *


    Requested quantity *


    Bulk Inquiry

    Inquiry Information

    Product Name:
    Cat. No.: