Maraviroc
Based on 59 publication(s) in Google Scholar
Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.98%
- CAS. Nr.: 376348-65-1
- Formel: C29H41F2N5O
- Molecular Weight:513.67
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Maraviroc
More- Cell. 2022 Jun 23;185(13):2234-2247.e17. [Abstract]
- Cell Stem Cell. 2026 Jan 8;33(1):44-57.e7. [Abstract]
- Cell Mol Immunol. 2026 Jun;23(6):701-718. [Abstract]
- Cell Mol Immunol. 2023 Aug;20(8):908-923. [Abstract]
- Cancer Res. 2025 Jun 20. [Abstract]
- Nat Commun. 2021 Dec 8;12(1):7122. [Abstract]
- Nat Commun. 2020 Nov 25;11(1):5994. [Abstract]
- Sci Transl Med. 2026 May 27;18(851):eadv8372. [Abstract]
- Adv Sci (Weinh). 2026 Jul;13(39):e20095. [Abstract]
- Adv Sci (Weinh). 2026 May 6:e21975. [Abstract]
- Adv Sci (Weinh). 2025 Jul 21:e00950. [Abstract]
- Adv Sci (Weinh). 2025 Jun 19:e16476. [Abstract]
- Adv Sci (Weinh). 2024 Sep 20:e2408598. [Abstract]
- J Biomed Sci. 2026 Jan 9;33(1):10. [Abstract]
- Redox Biol. 2026 Apr:91:104093. [Abstract]
- Research (Wash D C). 2025 Oct 20:8:0932. [Abstract]
- J Immunother Cancer. 2026 May 12;14(5):e012347. [Abstract]
- Pharmacol Res. 2024 Sep 16:107422. [Abstract]
- Cancer Lett. 2024 Jun 1:591:216892. [Abstract]
- Proc Natl Acad Sci U S A. 2026 Jan 20;123(3):e2426767123. [Abstract]
- Cell Commun Signal. 2025 Sep 2;23(1):388. [Abstract]
- J Environ Manage. 2022 Oct 1:319:115735. [Abstract]
- Phytomedicine. 2024 Jan:123:155238. [Abstract]
- J Orthop Translat . 2024 Jun 24:47:144-160. [Abstract]
- Biomed Pharmacother. 2024 Mar:172:116301. [Abstract]
- Biomed Pharmacother. 2020 Sep;129:110506. [Abstract]
- Stem Cell Res Ther. 2022 Jun 11;13(1):247. [Abstract]
- Ecotoxicol Environ Saf. 2024 Dec:288:117344. [Abstract]
- Biochem Pharmacol. 2026 Mar 22:249:117925. [Abstract]
- CNS Neurosci Ther. 2023 Jan;29(1):317-330. [Abstract]
- J Affect Disord. 2020 Dec 1;277:755-764. [Abstract]
- Front Pharmacol. 2017 May 3:8:230. [Abstract]
- J Photochem Photobiol A Chem. 2025 Nov 15;473:116930.
- Int Immunopharmacol. 2024 Sep 19;142(Pt B):113195. [Abstract]
- Int Immunopharmacol. 2024 May 23:135:112331. [Abstract]
- Am J Physiol Cell Physiol. 2024 May 1;326(5):C1320-C1333. [Abstract]
- Int Immunopharmacol. 2023 Sep 5;124(Pt A):110855. [Abstract]
- Neuropharmacology. 2024 Aug 15:254:109981. [Abstract]
- Molecules. 2023 Jan 25;28(3):1195. [Abstract]
- Int J Antimicrob Agents. 2019 Dec;54(6):814-819. [Abstract]
- Genes Immun. 2025 Dec 24. [Abstract]
- Lab Invest. 2020 Apr;100(4):619-629. [Abstract]
- Antiviral Res. 2020 Oct;182:104902. [Abstract]
- Drug Metab Dispos. 2019 Sep;47(9):954-960. [Abstract]
- Sci Rep. 2020 Nov 25;10(1):20508. [Abstract]
- Cytokine. 2018 Oct:110:70-77. [Abstract]
- Front Biosci (Landmark Ed). 2025 Apr 23;30(4):37430. [Abstract]
- Nucl Med Biol. 2024 May-Jun:132-133:108906. [Abstract]
- Res Sq. 2026 Jun 2.
- Res Sq. 2026 May 20:rs.3.rs-9499667. [Abstract]
- SSRN. 2026 Apr 18.
- bioRxiv. 2026 Jan 9:2026.01.08.698403. [Abstract]
- Res Sq. 2025 Apr 16.
- bioRxiv. 2024 September 03.
- bioRxiv. 2024 Jan 29.
- bioRxiv. 2023 Nov 17.
- Research Square Preprint. 2023 Aug 3.
- J SUN Yat⁃sen Univ (Med Sci). 2018,39(1):41-47.
- Journal of Drug Metabolism & Toxicology. January 10, 2016.
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Cell Migration/Invasion Assay
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In Vivo Efficacy Study
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IHC
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In Vivo Efficacy Study
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WB
Biologische Aktivität
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MIP-1α-CCR5 3.3 nM (IC50, in HEK-293 cell membrane) |
RANTES-CCR5 5.2 nM (IC50, in HEK-293 cell membrane) |
MIP-1β-CCR5 7.2 nM (IC50, in HEK-293 cell membrane) |
HIV-1 (Ba-L) 1.1 nM (IC50, in PM-1 cells) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HOS | CC50 |
>200 nM
Compound: MVC
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Cytotoxicity against human HOS cells after 48 hrs by MTT assay
Cytotoxicity against human HOS cells after 48 hrs by MTT assay
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[PMID: 30234300] |
| PBMC | CC50 |
>200 nM
Compound: MVC
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Cytotoxicity against human PBMC after 48 hrs by MTT assay
Cytotoxicity against human PBMC after 48 hrs by MTT assay
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[PMID: 30234300] |
| TZM | CC50 |
>200 μM
Compound: MVC
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Cytotoxicity against human TZM-bl cells after 48 hrs by MTT assay
Cytotoxicity against human TZM-bl cells after 48 hrs by MTT assay
|
[PMID: 30234300] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 376348-65-1
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Appearance Solid
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Molecular Weight 513.67
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Formel C29H41F2N5O
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Color White to off-white
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SMILES
O=C(C1CCC(F)(F)CC1)N[C@H](C2=CC=CC=C2)CCN3[C@H]4C[C@@H](N5C(C)=NN=C5C(C)C)C[C@@H]3CC4
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Synonyms
UK-427857
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (59)
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Journal Impact Factor
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Most Recent
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Cell
2022 Jun 23;185(13):2234-2247.e17. PMID: 35709748 -
Cell Stem Cell
Transcriptional code for circuit integration in the injured brain by transplanted human neurons. [Abstract]2026 Jan 8;33(1):44-57.e7. PMID: 41512834 -
Cell Mol Immunol
USP21 drives immune evasion in colorectal cancer via deubiquitination and stabilization of β-catenin. [Abstract]2026 Jun;23(6):701-718. PMID: 42091690 -
Cell Mol Immunol
A subpopulation of CD146+ macrophages enhances antitumor immunity by activating the NLRP3 inflammasome. [Abstract]2023 Aug;20(8):908-923. PMID: 37308559 -
Cancer Res
Tumor-Specific MHC-II Activates CD4+ and CD8+ T cells in Head and Neck Squamous Cell Carcinoma to Boost Immunotherapy Efficacy. [Abstract]2025 Jun 20. PMID: 40540325 -
Nat Commun
2021 Dec 8;12(1):7122. PMID: 34880260 -
Nat Commun
Prevention of CaCl2-induced aortic inflammation and subsequent aneurysm formation by the CCL3-CCR5 axis. [Abstract]2020 Nov 25;11(1):5994. PMID: 33239616
Maraviroc purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Nov 25;11(1):5994. [Abstract]
Aortic diameters in CaCl2-treated mice after maraviroc (intraperitoneally injected with 10 mg/kg , daily for 3 weeks) application (n = 4 each).
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Sci Transl Med
CCR5 and CD74 are potential therapeutic targets for necroinflammation in preclinical cholesterol crystal embolism. [Abstract]2026 May 27;18(851):eadv8372. PMID: 42202044 -
Adv Sci (Weinh)
2026 Jul;13(39):e20095. PMID: 41972457 -
Adv Sci (Weinh)
Enhancing CAR-T Cell Efficacy in Solid Tumors by Inhibiting CCL5/VEGF-Mediated Angiogenesis. [Abstract]2026 May 6:e21975. PMID: 42089445 -
Adv Sci (Weinh)
The CXCL10-CXCR3 Axis Induces Tumor-Associated Neutrophils to Interfere with CTLs-Mediated Antitumor Activity in EBV-Associated Epithelial Cancers. [Abstract]2025 Jul 21:e00950. PMID: 40686457
Maraviroc purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jul 21:e00950. [Abstract]
Freshly isolated neutrophils were pre-treated overnight with culture supernatant from AGS or AGS-EBV cells (H), supplemented with Maraviroc (1 µM).
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Adv Sci (Weinh)
Scaffolding Protein ENH Promotes Tumor Angiogenesis and Growth Through Macrophage Recruitment and Polarization. [Abstract]2025 Jun 19:e16476. PMID: 40536254
Maraviroc purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jun 19:e16476. [Abstract]
LLC‐Vector and LLC‐ENH‐OV tumor growth in mice treated with or without maraviroc (i.p., 10 mg/kg, every other day).
Maraviroc purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jun 19:e16476. [Abstract]
Representative images of IF staining for CD31 and IHC staining for F4/80 in LLC‐Vector and LLC‐ENH‐OV tumors sections treated with or without maraviroc (i.p., 10 mg kg−1, every other day i.p., 10 mg/kg, every other day ).
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Adv Sci (Weinh)
Blockade of CCR5+ T Cell Accumulation in the Tumor Microenvironment Optimizes Anti-TGF-β/PD-L1 Bispecific Antibody. [Abstract]2024 Sep 20:e2408598. PMID: 39303165 -
J Biomed Sci
2026 Jan 9;33(1):10. PMID: 41508046 -
Redox Biol
PP4 modulates macrophage-neutrophil crosstalk to restrict CCL5 -driven NETosis in sepsis. [Abstract]2026 Apr:91:104093. PMID: 41723906 -
Research (Wash D C)
2025 Oct 20:8:0932. PMID: 41122266 -
J Immunother Cancer
CXCL16-driven CD4+ T cells orchestrate immunosurveillance against MHC-I-deficient hepatocellular tumors. [Abstract]2026 May 12;14(5):e012347. PMID: 42120180 -
Pharmacol Res
Orosomucoid 2 is an endogenous regulator of neuronal mitochondrial biogenesis and promotes functional recovery post-stroke. [Abstract]2024 Sep 16:107422. PMID: 39293585 -
Cancer Lett
Anlotinib enhanced CD8+ T cell infiltration via induction of CCL5 improves the efficacy of PD-1/PD-L1 blockade therapy in lung cancer. [Abstract]2024 Jun 1:591:216892. PMID: 38621459 -
Proc Natl Acad Sci U S A
CCR5 marks a subset of mouse hematopoietic stem cells that are myeloid primed and expand with age. [Abstract]2026 Jan 20;123(3):e2426767123. PMID: 41538244 -
Cell Commun Signal
AXL and MERTK facilitate tissue repair in severe acute pancreatitis via a CCR5-dependent neutrophil and macrophage crosstalk. [Abstract]2025 Sep 2;23(1):388. PMID: 40898178 -
J Environ Manage
Efficient removal of anti-HIV drug - maraviroc from natural water by peroxymonosulfate and TiO2 photocatalytic oxidation: Kinetic studies and identification of transformation products. [Abstract]2022 Oct 1:319:115735. PMID: 35863307 -
Phytomedicine
Ginsenoside Rg1 treats ischemic stroke by regulating CKLF1/CCR5 axis-induced neuronal cell pyroptosis. [Abstract]2024 Jan:123:155238. PMID: 38128394 -
J Orthop Translat
2024 Jun 24:47:144-160. PMID: 39027343 -
Biomed Pharmacother
Soluble epoxide hydrolase inhibitor (TPPU) alleviates ferroptosis by regulating CCL5 after intracerebral hemorrhage in mice. [Abstract]2024 Mar:172:116301. PMID: 38377737 -
Biomed Pharmacother
Interplay of drug transporters P-glycoprotein (MDR1), MRP1, OATP1A2 and OATP1B3 in passage of maraviroc across human placenta. [Abstract]2020 Sep;129:110506. PMID: 32768979 -
Stem Cell Res Ther
Intramyocardial injected human umbilical cord-derived mesenchymal stem cells (HucMSCs) contribute to the recovery of cardiac function and the migration of CD4+ T cells into the infarcted heart via CCL5/CCR5 signaling. [Abstract]2022 Jun 11;13(1):247. PMID: 35690805 -
Ecotoxicol Environ Saf
Endosulfan promotes cell growth, migration and invasion via CCL5/CCR5 axis in MCF-7 cells. [Abstract]2024 Dec:288:117344. PMID: 39549571 -
Biochem Pharmacol
Recruitment of tumor-associated macrophages via the CCL4-CCR5 axis promotes immune escape through PD-1 signaling in lung adenocarcinoma. [Abstract]2026 Mar 22:249:117925. PMID: 41876018 -
CNS Neurosci Ther
2023 Jan;29(1):317-330. PMID: 36440924 -
J Affect Disord
The role of CCR5 in the protective effect of Esculin on lipopolysaccharide-induced depressive symptom in mice. [Abstract]2020 Dec 1;277:755-764. PMID: 33065814 -
Front Pharmacol
Wu-Tou Decoction in Rheumatoid Arthritis: Integrating Network Pharmacology and In Vivo Pharmacological Evaluation. [Abstract]2017 May 3:8:230. PMID: 28515692
Maraviroc purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2017 May 3:8:230. [Abstract]
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.
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Int Immunopharmacol
The RIG-I-like receptor signaling pathway triggered by Staphylococcus aureus promotes breast cancer metastasis. [Abstract]2024 Sep 19;142(Pt B):113195. PMID: 39303544 -
Int Immunopharmacol
Involvement of CCR5 on interstitial macrophages in the development of lung fibrosis in severe asthma. [Abstract]2024 May 23:135:112331. PMID: 38795597 -
Am J Physiol Cell Physiol
The myokine CCL5 recruits subcutaneous preadipocytes and promotes intramuscular fat deposition in obese mice. [Abstract]2024 May 1;326(5):C1320-C1333. PMID: 38497114 -
Int Immunopharmacol
Inflammatory regulation by restraining M2 microglial polarization: Neurodestructive effects of Kallikrein-related peptidase 8 activation in intracerebral hemorrhage. [Abstract]2023 Sep 5;124(Pt A):110855. PMID: 37678029 -
Neuropharmacology
CCR5 antagonist maraviroc alleviates doxorubicin-induced neuroinflammation and neurobehavioral deficiency by regulating NF-κB/NLRP3 signaling in a breast cancer mouse model. [Abstract]2024 Aug 15:254:109981. PMID: 38704022 -
Molecules
Multivariate Chemometric Comparison of Forced Degradation and Electrochemical Oxidation LC-MS Profiles of Maraviroc. [Abstract]2023 Jan 25;28(3):1195. PMID: 36770862 -
Int J Antimicrob Agents
2019 Dec;54(6):814-819. PMID: 31479744 -
Genes Immun
Recruitment of CCR5+ inflammatory monocytes in pulmonary tissue contributes to acute lung injury. [Abstract]2025 Dec 24. PMID: 41444399 -
Lab Invest
CCL8 secreted by tumor-associated macrophages promotes invasion and stemness of glioblastoma cells via ERK1/2 signaling. [Abstract]2020 Apr;100(4):619-629. PMID: 31748682 -
Antiviral Res
The chemokine receptor antagonist cenicriviroc inhibits the replication of SARS-CoV-2 in vitro. [Abstract]2020 Oct;182:104902. PMID: 32739404 -
Drug Metab Dispos
Interactions between Maraviroc and the ABCB1, ABCG2, and ABCC2 Transporters: An Important Role in Transplacental Pharmacokinetics. [Abstract]2019 Sep;47(9):954-960. PMID: 31266750 -
Sci Rep
Multiple myeloma hinders erythropoiesis and causes anaemia owing to high levels of CCL3 in the bone marrow microenvironment. [Abstract]2020 Nov 25;10(1):20508. PMID: 33239656 -
Cytokine
Chemokine receptor antagonist block inflammation and therapy Japanese encephalitis virus infection in mouse model. [Abstract]2018 Oct:110:70-77. PMID: 29704821 -
Front Biosci (Landmark Ed)
Macrophage Notch1 Participates in LPS-Induced Acute Lung Injury via Regulating CCR5 Expression in Mice. [Abstract]2025 Apr 23;30(4):37430. PMID: 40302346 -
Nucl Med Biol
Second generation Al18F-labeled D-amino acid peptide for CXCR4 targeted molecular imaging. [Abstract]2024 May-Jun:132-133:108906. PMID: 38518400 -
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Res Sq
2026 May 20:rs.3.rs-9499667. PMID: 42239782 -
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bioRxiv
Donor Macrophage Depletion Permits Post-Transplant Tolerance Induction in a Murine Islet Transplant Model. [Abstract]2026 Jan 9:2026.01.08.698403. PMID: 41542550 -
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Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (194.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 6.5 mg/mL (12.65 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 1% DMSO 99% Saline
Solubility: ≥ 0.5 mg/mL (0.97 mM); Clear solution
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
Mice[2]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (282 KB)
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SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Korean - KR (418 KB)
- Portuguese - PT (418 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Dorr P, et al. Maraviroc (UK-427,857), a potent, orally bioavailable, and selective small-molecule inhibitor of chemokine receptor CCR5 with broad-spectrum anti-human immunodeficiency virus type 1 activity. Antimicrob Agents Chemother. 2005 Nov;49(11):472 [Content Brief]
[2]. Mencarelli A, et al. Highly specific blockade of CCR5 inhibits leukocyte trafficking and reduces mucosal inflammation in murine colitis. Sci Rep. 2016 Aug 5;6:30802. [Content Brief]
[3]. Romero-Sánchez MC, et al. Effect of maraviroc on HIV-disease progression-related biomarkers. Antimicrob Agents Chemother. 2012 Nov;56(11):5858-64. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 1.9468 mL | 9.7339 mL | 19.4678 mL | 48.6694 mL |
| 5 mM | 0.3894 mL | 1.9468 mL | 3.8936 mL | 9.7339 mL | |
| 10 mM | 0.1947 mL | 0.9734 mL | 1.9468 mL | 4.8669 mL | |
| DMSO | 15 mM | 0.1298 mL | 0.6489 mL | 1.2979 mL | 3.2446 mL |
| 20 mM | 0.0973 mL | 0.4867 mL | 0.9734 mL | 2.4335 mL | |
| 25 mM | 0.0779 mL | 0.3894 mL | 0.7787 mL | 1.9468 mL | |
| 30 mM | 0.0649 mL | 0.3245 mL | 0.6489 mL | 1.6223 mL | |
| 40 mM | 0.0487 mL | 0.2433 mL | 0.4867 mL | 1.2167 mL | |
| 50 mM | 0.0389 mL | 0.1947 mL | 0.3894 mL | 0.9734 mL | |
| 60 mM | 0.0324 mL | 0.1622 mL | 0.3245 mL | 0.8112 mL | |
| 80 mM | 0.0243 mL | 0.1217 mL | 0.2433 mL | 0.6084 mL | |
| 100 mM | 0.0195 mL | 0.0973 mL | 0.1947 mL | 0.4867 mL |