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Maraviroc

Catalog No. T6016 CAS 376348-65-1

Synonyms: Celsentri, UK-427857, Selzentry

Maraviroc (Selzentry) is a C-C Chemokine Receptor Type 5 (CCR5) antagonist, and for MIP-1α(IC50=3.3 nM), MIP-1β (IC50=7.2 nM) and RANTES(IC50=5.2 nM).Maraviroc inhibits HIV-1 entry via CCR5 coreceptor interaction.

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Maraviroc, CAS 376348-65-1

Pack Size	Availability	Price/USD
5 mg	In stock	$ 47.00
10 mg	In stock	$ 87.00
25 mg	In stock	$ 163.00
50 mg	In stock	$ 287.00
100 mg	In stock	$ 517.00
200 mg	In stock	$ 667.00
500 mg	In stock	$ 1,050.00
1 mL * 10 mM (in DMSO)	In stock	$ 54.00

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Purity: 100%

Purity: 99.55%

Purity: 99.21%

Purity: 98.53%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Maraviroc (Selzentry) is a C-C Chemokine Receptor Type 5 (CCR5) antagonist, and for MIP-1α(IC50=3.3 nM), MIP-1β (IC50=7.2 nM) and RANTES(IC50=5.2 nM).Maraviroc inhibits HIV-1 entry via CCR5 coreceptor interaction.
Targets&IC50	MIP-1α:3.3 nM, RANTES:5.2 nM, MIP-1β:7.2 nM
In vitro	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 vivo	Maraviroc (IC50=7-30 nM) inhibits the downstream intracellular calcium redistribution induced by chemokines in MIP-1β, MIP-1α, and RANTES.
Kinase Assay	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	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)

Synonyms	Celsentri, UK-427857, Selzentry
Molecular Weight	513.67
Formula	C29H41F2N5O
CAS No.	376348-65-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 38.5 mg/mL (75 mM)

Ethanol: 51.4 mg/mL (100 mM)

References and Literature

1. Dorr P, et al. Antimicrob Agents Chemother. 2005, 49(11), 4721-4732. 2. Neff CP, et al. PLoS One. 2011, 6(6), e20209. 3. Tan S, Li J Q, Cheng H, et al. The anti-parasitic drug suramin potently inhibits formation of seminal amyloid fibrils and their interaction with HIV-1[J]. Journal of Biological Chemistry. 2019: jbc. RA118. 006797. 4. Yang J Y, Zhang J, Lu R, et al. T cell–derived exosomes induced macrophage inflammatory protein‐1α/β drive the trafficking of CD8+ T cells in oral lichen planus[J]. Journal of cellular and molecular medicine. 2020

Citations

1. Yang J Y, Zhang J, Lu R, et al. T cell–derived exosomes induced macrophage inflammatory protein‐1α/β drive the trafficking of CD8+ T cells in oral lichen planus. Journal of Cellular and Molecular Medicine. 2020 2. Tan S, Li J Q, Cheng H, et al. The anti-parasitic drug suramin potently inhibits formation of seminal amyloid fibrils and their interaction with HIV-1. Journal of Biological Chemistry. 2019: jbc. RA118. 006797 3. Wu Q, Cui L, Ma W, et al.A novel small-molecular CCR5 antagonist promotes neural repair after stroke.Acta Pharmacologica Sinica.2023: 1-13. 4. Horie M, Takagane K, Itoh G, et al.Exosomes secreted by ST3GAL5 high cancer cells promote peritoneal dissemination by establishing a pre‐metastatic microenvironment.Molecular Oncology.2023

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Neurodegenerative Disease Compound Library Drug Repurposing Compound Library Membrane Protein-targeted Compound Library EMA Approved Drug Library Clinical Compound Library Anti-Alzheimer's Disease Compound Library Approved Drug Library NO PAINS Compound Library Cytokine Inhibitor Library

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Keywords

Maraviroc 376348-65-1 Immunology/Inflammation Microbiology/Virology Proteases/Proteasome HIV Protease CCR CC chemokine receptor UK427857 inhibit Human immunodeficiency virus Celsentri HIV Inhibitor UK 427857 UK-427857 Selzentry inhibitor

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