Maraviroc

Catalog No.S2003 Synonyms: UK-427857

Maraviroc Chemical Structure

Molecular Weight(MW): 513.67

Maraviroc is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM in cell-free assays, respectively.

Size Price Stock Quantity  
In DMSO USD 98 In stock
USD 70 In stock
USD 270 In stock
USD 770 In stock

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3 Customer Reviews

  • CCR5 antagonists block FBS-induced breast cancer cell invasion. 3D reconstruction of FBS-induced invasion into collagen gels by Hs578T (A) or SUM-159 (C) breast cancer cells in presence of CCR5 antagonists (100 nmol/L). The corresponding quantifications (mean ±SEM, n = 3) and analysis (Bonferronit test) are displayed in B and D.

    Cancer Res 2012 72(15), 3839-50. Maraviroc purchased from Selleck.

    (E)CAF-induced migration of Huh7 cells was blocked by antagonists of chemokine receptors. CCR2 antagonist (INCB3284, 100 nM), CCR5 antagonist (Maraviroc, 100 nM) and selective CCR1 and CCR3 antagonists (UCB35625, 100 nM) were added to CAF-CM in the transwell assay.

    Cancer Lett, 2016, 379(1):49-59.. Maraviroc purchased from Selleck.

  • Analysis of receptor mechanisms mediating the induction of MMP-9 expression in THP-1 cells by AFP. Maraviroc, an inhibitor of chemokine receptor CCR5, was added to the cells in the indicated concentrations 1 hour before addition of 50 μg/ml AFP or 150 ng/ml RANTES. After 24 hours of cell stimulation, conditioned media were collected and analyzed for MMP-9 activity by the method of zymography

    2010 Dr. Johanna Weiss of University Hospital Heidelberg. Maraviroc purchased from Selleck.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Maraviroc is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM in cell-free assays, respectively.
Targets
MIP-1α [1]
(Cell-free assay)
RANTES [1]
(Cell-free assay)
MIP-1β [1]
(Cell-free assay)
3.3 nM 5.2 nM 7.2 nM
In vitro

Maraviroc inhibits MIP-1β-stimulated γ-S-GTP binding to HEK-293 cell membranes, indicating its ability to inhibit chemokine-dependent stimulation of GDP-GTP exchange at the CCR5/G protein complex. Maraviroc also 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. In the same experiments, Maraviroc does not trigger release of intracellular calcium at concentrations up to 10 μM, indicating that it is devoid of CCR5 agonist activity. Consistent with this, Maraviroc fails to induce CCR5 internalization. Maraviroc is active at low nanomolar concentrations against HIV-1 Ba-L. Maraviroc inhibits all 200 pseudotyped viruses with a geometric mean IC90 of 13.7 nM. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa-P4 cells NG\LOJZHfW6ldHnvckBie3OjeR?= Mm\UNlAh\GG7cx?= NH70TmRCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IFPDVlUhemWlZYD0c5Ih\XiycnXzd4VlKGmwIFjlUIEuWDRiY3XscJMh[29vZYjwdoV{e2mwZzDDSFQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBqdm[3c3nvckB1dyCKSW[g[5AyOjBiZYjwdoV{e2WmIHnuJGNJVy22YYSxNEBk\WyuczDh[pRmeiB{MDDodpMh[nliY3XscE1k\WyuIH\1d4lwdiCjc4PhfUwhUUN3ME2wMlIhdk1? M1nEZVIyOTJ6Nk[z
rhesus monkey Chem-1 cell M1HYTWZ2dmO2aX;uJIF{e2G7 NEDISnQyOjBibXnudy=> M2HzbmRqe3CuYXPlcYVvfCCxZjDbNVI2UV1vTVnQMVFidHCqYTDmdo9uKEOFUkWgbY4heminc4XzJI1wdmuneTDDbIVuNTFiY3XscEBu\W2kcnHu[ZMh[W[2ZYKgNVIxKG2rboOgZpkhdGmzdXnkJJNkcW62aXzsZZRqd25iY3;1cpRqdmdiYX7hcJl{cXNuIFvpQVAvOjRibl2= M4TTflI{Pjh{M{C4
human TZM-bl cells MUnGeY5kfGmxbjDhd5NigQ>? MUS0PEBp MWHBcpRi\2:waYP0JIFkfGm4aYT5JIFo[Wmwc4SgR2NTPSC{ZXPldJRweiCrbjDoeY1idiCWWl2tZowh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDITXYuOSCPR1OyOk1qdmS3Y3XkJINmdGxvY3XscEBnfXOrb36gZoV1f2WnbjD2bZJidCCnbo\lcI9x\SCycn;0[YlvKGW6cILld5NqdmdiaIXtZY4hUEWNMkmzJINmdGy|IITvJHRbVS2kbDDj[YxteyCjZoTldkA1QCCqcoOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDJR|UxRTBwM{egcm0> MXOyOFU3Ozd{Mx?=
CHO cells MlXkSpVv[3Srb36gZZN{[Xl? NWjYWJpnOiCq Ml33SIl{eGyjY3Xt[Y51KG:oIGuxNlhKZVKDTmTFV{Bnem:vIHj1cYFvKEOFUkWgdoVk\XC2b4KgZ49mgHC{ZYPz[YQhf2m2aDDHZYxxcGGrNjDpckBEUE9iY3XscJMh[W[2ZYKgNkBpenNiYomgd4NqdnSrbHzheIlwdiClb4XueIlv\yxiSVO1NF0yNjRibl2= M1TQcVIxOTN5OUO3
HOS cells NXrKRY5YTnWwY4Tpc44h[XO|YYm= NIjQUJZCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJUVZzIFLhMWwhcW6oZXP0[YQhcW5iSF;TJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZidnnyZYwhcW6oZXP0bY9vNCCLQ{WwQVIhdk1? MlP5NVk3PjR7MkC=
HEK293 cells NIjYNWpHfW6ldHnvckBie3OjeR?= MUfJcohq[mm2aX;uJI9nKGi3bXHuJG1CXEVzLX3l[IlifGWmIFHTVEshfXC2YXvlJIV5eHKnc4Pl[EBqdiCKRVuyPVMh[2WubIOgZYZ1\XJiMT61JI1qdnNiYomg[ox2d3Knc3PlcoNmKGG|c3H5MEBKSzVyPUG3MlMh|pyv Mme1NlMzPDFyMkm=
human astrocytes MYHGeY5kfGmxbjDhd5NigQ>? M4rNc|ExOCCwTR?= NHL1[2c{OCC2bzC2NEBucW6| M2iwemJqdmSrbnegZYZncW6rdImgeI8hS0OUNT;NU3IhcW5iaIXtZY4h[XO2cn;jfZRmeyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKFJ3IFjJWk0yKFOIMU[yJIlv\mWldHnvckBjgSCvZXHzeZJqdmdiVHH0JJBzd3SnaX6g[ZhxemW|c3nvckBifCBzMECgcm0heHKnaX7jeYJifGWmIH\vdkA{OCC2bzC2NEBucW6|IH\vcIxwf2WmIHL5JJZqemGuIHnu[oVkfGmxbjDt[YF{fXKnZDDh[pRmeiBzODDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5 MkTTNlM3QDJ|MEi=

... Click to View More Cell Line Experimental Data

In vivo The half-life values of Maraviroc are 0.9 hour in the rat and 2.3 hours in the dog. Following oral administration (2 mg/kg) to the dog, the Cmax (256 ng/ml) occurred 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] Female RAG-hu mice are challenged vaginally with HIV-1 an hour after intravaginal application of the Maraviroc gel. Maraviroc gel treated mice are fully protected against vaginal HIV-1 challenge in contrast to placebo gel treated mice which all became infected. Vaginal administration of Maraviroc fully protects mice against HIV-1 vaginal challenge. While there is a clear pattern of CD4 T cell decline in placebo-gel treated and viral challenged mice, their levels are stable in mice receiving Maraviroc gel. [2]

Protocol

Kinase Assay:[1]
+ Expand

Inhibition of chemokine binding to CCR5:

Binding of 125I-labeled MIP-1α, MIP-1β, and RANTES to CCR5 is measured 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) 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. Maraviroc dilutions are added to each well to a final volume of 100 μL, the assay plates incubate for 1 hour, and the contents filter through preblocked and washed Unifilter plates which are counted following overnight drying.
Cell Research:[1]
+ Expand
  • Cell lines: PHA-stimulated PBMC or PM-1 cells
  • Concentrations: 0-1 μM
  • Incubation Time: 5 days or 7 days
  • Method: 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)
Animal Research:[2]
+ Expand
  • Animal Models: Humanized BALB/c-Rag2−/−γc−/− and BALB/c-Rag1−/−γc−/− (RAG-hu) mice
  • Formulation: Dissolved in phosphate-buffered saline, sterile-filtered and adjusted to a final concentration of 4 mg/mL (7.8 mM). A 3.4% gel preparation of hydroxyl-ethyl cellulose (HEC) is added to achieve a final concentration of 5 mM Maraviroc in 2.2% HEC gel.
  • Dosages: ~64 μg
  • Administration: A 25 μL volume of the gel formulation is carefully applied in to the vaginal vault of mice.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (194.67 mM)
Ethanol 100 mg/mL (194.67 mM)
Water <1 mg/mL
In vivo 2% DMSO+corn oil 10mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 513.67
Formula

C29H41F2N5O

CAS No. 376348-65-1
Storage powder
in solvent
Synonyms UK-427857

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02990312 Not yet recruiting Hiv|Kidney Transplant|HIV Reservoir|CCR5 University of Maryland January 2017 Phase 4
NCT02741323 Recruiting HIV Infections National Institute of Allergy and Infectious Diseases (NIAID) January 2017 Phase 2
NCT02881762 Not yet recruiting Hepatitis C|Human Immunodeficiency Virus University of Maryland|ViiV Healthcare September 2016 Phase 4
NCT02519777 Recruiting HIV Infections National Institute of Allergy and Infectious Diseases (NIAID) March 2016 Phase 4
NCT02625207 Completed Healthy Subjects ViiV Healthcare|Pfizer November 2015 Phase 1
NCT02480894 Completed HIV/AIDS Bristol-Myers Squibb July 2015 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID