1. GPCR/G Protein
  2. CCR
  3. Maraviroc

Maraviroc (Synonyms: UK-427857)

Cat. No.: HY-13004 Purity: 99.95%
Handling Instructions

Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV.

For research use only. We do not sell to patients.

Maraviroc Chemical Structure

Maraviroc Chemical Structure

CAS No. : 376348-65-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 68 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Estimated Time of Arrival: December 31
50 mg USD 348 In-stock
Estimated Time of Arrival: December 31
100 mg USD 624 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 11 publication(s) in Google Scholar

Top Publications Citing Use of Products

    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.

    View All CCR Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review


    Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV.

    IC50 & Target[1]


    3.3 nM (IC50, in HEK-293 cell membrane)


    5.2 nM (IC50, in HEK-293 cell membrane)


    7.2 nM (IC50, in HEK-293 cell membrane)

    HIV-1 (Ba-L)

    1.1 nM (IC50, in PM-1 cells)

    In Vitro

    Maraviroc (UK-427857) 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 (UK-427857) 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
    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


    Room temperature in continental US; may vary elsewhere.

    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (97.34 mM; Need ultrasonic)

    Ethanol : 6.5 mg/mL (12.65 mM; Need ultrasonic)

    Stock Solutions
    Concentration Solvent 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.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    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

    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

    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.


    Purity: 99.95%

    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2


    MaravirocUK-427857UK427857UK 427857CCRHIVCC chemokine receptorHuman immunodeficiency virusInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name



    Applicant Name *


    Email address *

    Phone number *


    Organization name *

    Department *


    Requested quantity *

    Country or Region *



    Bulk Inquiry

    Inquiry Information

    Product Name:
    Cat. No.:
    MCE Japan Authorized Agent: