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Maraviroc

Name: Maraviroc
Brand: Selleck Chemicals
SKU: S2003
Rating: 5 (46 reviews)

Synonyms: UK-427857

Catalog No.S2003 Purity: 99.99%

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. Maraviroc is used in the treatment of HIV infection.

Maraviroc Chemical Structure

CAS: 376348-65-1

Selleck's Maraviroc has been cited by 46 publications

Purity & Quality Control

Batch: Purity: 99.99%

99.99

Products often used together with Maraviroc

Pembrolizumab (anti-PD-1)

Maraviroc & Pembrolizumab show positive toxicity patterns in a phase I trial for metastatic colorectal cancer.

Haag GM, et al. Eur J Cancer. 2022 May;167:112-122.

Leronlimab (anti-CCR5)

Maraviroc and Leronlimab (PRO-140) together inhibit HIV-1JR-FL envelope-mediated membrane fusion in the RET cell-cell fusion assay.

Murga JD, et al. Antimicrob Agents Chemother. 2006 Oct;50(10):3289-96.

Etravirine

Maraviroc and Etravirine can be used in salvaging patients with complete nucleoside reverse transcriptase inhibitor (NRTI) resistance.

Vallabhaneni S, et al. J Int AIDS Soc. 2013 Jun 3;16(1):18449.

Vicriviroc Malate

Maraviroc and Vicriviroc reduce prostate cancer cell metastasis to the bones, brain, and viscera in immune-competent mice.

Jiao X, et al. Cancer Res. 2019 Oct 1;79(19):4801-4807.

Tenofovir Disoproxil Fumarate

Maraviroc and Tenofovir have context-specific effects on progesterone receptor B (PR-B) activation.

Enfield K, et al. Biochem Biophys Res Commun. 2020 Dec 17;533(4):1027-1033.

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Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
HeLa-P4	Function assay		Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay, IC50 = 0.0002 μM.	19171484
HeLa-P4	Function assay	20 hrs	Antagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assay, IC50 = 0.0002 μM.	21128663
TZM-bl	Function assay	3 days	Inhibition of CCR5 in human TZM-bl cells infected with HIV1 Bal R5 assessed as antiviral activity by measuring reduction in viral infection pre-incubated with cells followed by viral infection measured after 3 days by luciferase reporter gene assay, IC50 = 0.0002 μM.	28082070
TZM-bl	Function assay	48 hrs	Antagonist activity against CCR5 receptor in human TZM-bl cells assessed as inhibition of HIV-1 MGC26-induced cell-cell fusion between viral envelope protein expressing human HEK293 cells to TZM-bl cells after 48 hrs by luciferase reporter gene assay, IC50 = 0.00037 μM.	24563723
TZM-bl	Function assay	48 hrs	Antagonist activity against CCR5 receptor in human TZM-bl cells assessed as inhibition of HIV-1 YU2-induced cell-cell fusion between viral envelope protein expressing human HEK293 cells to TZM-bl cells after 48 hrs by luciferase reporter gene assay, IC50 = 0.00043 μM.	24563723
PM1	Antiviral assay		Antiviral activity against HIV1 Bal infected in human PM1 cells assessed as inhibition of viral replication, IC90 = 0.0007 μM.	19171484
PM1	Antiviral assay	5 days	Antiviral activity against CCR5-dependent HIV1 Ba-L infected in human PM1 cells assessed as reduction in virus infection measured after 5 days by luciferase reporter gene assay, IC50 = 0.001 μM.	30234300
SupT1	Antiviral assay	48 hrs	Antiviral activity against HIV-1 infected in human SupT1 cells assessed as inhibition of viral infectivity after 48 hrs by luciferase reporter gene assay, IC50 = 0.0011 μM.	24316669
TZM-bl	Function assay	48 hrs	Antagonist activity against CCR5 receptor in human TZM-bl cells assessed as inhibition of HIV-1 92RW-induced cell-cell fusion between viral envelope protein expressing human HEK293 cells to TZM-bl cells after 48 hrs by luciferase reporter gene assay, IC50 = 0.0013 μM.	24563723
CHO	Function assay	2 hrs	Displacement of [128I]RANTES from human CCR5 receptor coexpressed with Galphai6 in CHO cells after 2 hrs by scintillation counting, IC50 = 0.0014 μM.	20137937
TZM-bl	Function assay	48 hrs	Antagonist activity against CCR5 receptor in human TZM-bl cells assessed as inhibition of HIV-1 JR-FL-induced cell-cell fusion between viral envelope protein expressing human HEK293 cells to TZM-bl cells after 48 hrs by luciferase reporter gene assay, IC50 = 0.0016 μM.	24563723
HOS	Antiviral assay	5 days	Antiviral activity against CCR5-dependent HIV1 Ba-L infected in human HOS cells assessed as reduction in virus infection measured after 5 days by luciferase reporter gene assay, IC50 = 0.0019 μM.	30234300
HOS	Antiviral assay		Antiviral activity against HIV1 Ba-L infected in HOS cells assessed as inhibition of viral infection, IC50 = 0.002 μM.	19664920
MOLT4	Function assay	15 mins	Antagonist activity at CCR5 in Gqi5 transfected human MOLT4 cells assessed as inhibition of RANTES-stimulated Ca2+ influx preincubated for 15 mins followed by DAMGO challenge, IC50 = 0.0022 μM.	23682308
JC53-BL	Antiviral assay	3 days	Antiviral activity against CCR5-tropic recombinant HIV1 NLBal virus infected in JC53-BL cells assessed as inhibition of viral replication after 3 days by luciferase reporter gene assay, IC50 = 0.0028 μM.	20137937
JC53-BL	Antiviral assay	3 days	Antiviral activity against HIV1 NL4-3 infected in human JC53-BL cells assessed as luciferase activity after 3 days post infection, IC50 = 0.003 μM.	20417098
HOS	Antiviral assay	5 days	Antiviral activity against CCR5-dependent HIV1 SF162 infected in human HOS cells assessed as reduction in virus infection measured after 5 days by luciferase reporter gene assay, IC50 = 0.0047 μM.	30234300
NIH/3T3	Function assay	1 hr	Displacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hr, IC50 = 0.0052 μM.	29425816
SupT1	Antiviral assay	48 hrs	Antiviral activity against HIV1 infected in human SupT1 cells exposed to supernatant from HIV1 infected human 293T cells incubated for 48 hrs by firefly luciferase assay based single-cycle HIV1 replication assay, IC50 = 0.0055 μM.	25638498
TZM-bl	Antiviral assay	48 hrs	Antiviral activity against CCR5-dependent HIV1 SF162 infected in human TZM-bl cells assessed as reduction in virus infection measured after 48 hrs post infection by luciferase reporter gene assay, IC50 = 0.0067 μM.	30234300
HEK293	Function assay	10 mins	Antagonist activity at CCR5 (unknown origin) expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of RANTES-induced calcium flux preincubated for 10 mins followed by RANTES addition by fluo-4AM-based fluorescence assay, IC50 = 0.008 μM.	30234300
CHO	Function assay	10 mins	Antagonist activity against CCR5 (unknown origin) expressed in CHO cells co-expressing Galpha16 incubated for 10 mins assessed as inhibition of RANTES-induced calcium mobilization, IC50 = 0.0131 μM.	25638498
CHO	Function assay	10 mins	Inhibition of CCR5 (unknown origin) expressed in CHO cells assessed as inhibition of RANTES-induced intracellular Ca2+ mobilization after 10 mins by Fluo-4 AM staining-based fluorescence assay, IC50 = 0.02543 μM.	24316669
HEK293	Function assay	1.5 mins	Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay, IC50 = 17.3 μM.	23241029
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
NB-EBc1	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	29435139
Rh30	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
RD	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	29435139
Rh18	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
Click to View More Cell Line Experimental Data

Biological Activity

Description

Targets

CCR5 ^[3] (Cell-free assay)	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
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] At concentrations >1000 times the 50% inhibitory concentration, maraviroc did not inhibit other chemokine receptors (CCR1, 2, 3, 4, 7, and 8; CXCR1 and 2) to a clinically relevant degree^[3].
Kinase Assay	Inhibition of chemokine binding to CCR5
Kinase Assay	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	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.
Experimental Result Images	Methods	Biomarkers	Images	PMID
Experimental Result Images	Western blot	cleaved caspase-3 / cleaved caspase-9 / cleaved PARP / XIAP / Survivin / c-IAP1 / c-IAP2 / Bax / Bad / Bcl2 / Bcl-xl		28469959

In Vivo
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]
Animal Research	Animal Models	Humanized BALB/c-Rag2−/−γc−/− and BALB/c-Rag1−/−γc−/− (RAG-hu) mice
	Dosages	~64 μg
	Administration	A 25 μL volume of the gel formulation is carefully applied in to the vaginal vault of mice.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT04966429	Recruiting	Post Stroke Cognitive Impairment	Tel-Aviv Sourasky Medical Center\|Hadassah Medical Organization\|Soroka University Medical Center	May 1 2021	Phase 2
NCT04710199	Completed	Virus Diseases	Fundación Pública Andaluza para la gestión de la Investigación en Sevilla	February 23 2021	Phase 2
NCT02881762	Completed	Hepatitis C\|Human Immunodeficiency Virus	University of Maryland Baltimore\|ViiV Healthcare	June 1 2017	Phase 4
NCT02778204	Completed	HIV Infections	National Institute of Allergy and Infectious Diseases (NIAID)\|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)\|ViiV Healthcare\|GlaxoSmithKline	June 5 2017	Phase 1
NCT02741323	Completed	HIV Infections\|Kidney Diseases	National Institute of Allergy and Infectious Diseases (NIAID)	January 1 2017	Phase 2

References

Chemical lnformation & Solubility

Molecular Weight	513.67	Formula	C₂₉H₄₁F₂N₅O
CAS No.	376348-65-1	SDF	Download Maraviroc SDF
Smiles	CC1=NN=C(N1C2CC3CCC(C2)N3CCC(C4=CC=CC=C4)NC(=O)C5CCC(CC5)(F)F)C(C)C
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (194.67 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	Clear solution	5%DMSO 1 Corn oil	1.2mg/ml (2.34mM)	Taking the 1 mL working solution as an example, add 50 μL of 24 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.	In vivo Formulation Calculator
Clear solution	10% DMSO 1 40% PEG 300 2 5%Tween80 3 45% water	12.5mg/ml (24.33mM)	Taking the 1 mL working solution as an example, add 100 μL of 125mg/ml clear DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue adding Dilute 450 μL ddH2O to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml (9.73mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO + % + % Tween 80 + % ddH₂O

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
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Frequently Asked Questions

Question 1:
What’s the vehicle do you recommend to dissolve the compound for in vivo experiments?

Answer:
S2003 Maraviroc can be dissolved in 5% DMSO/castor oil at 62 mg/ml as suspension for oral administration. As to a clear solution for injection, following three vehicles at 10mg/ml will help: 1. 2% DMSO/castor oil; 2. 2%DMSO/sunflower oil; 3. 2%DMSO/30%PEG 300/ddH2O.

CCR Signaling Pathway Map

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):