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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Maraviroc (also known as UK-427857) is a potent, selective and non-competitive 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 as an antiviral agent for the treatment of HIV. In HeLa P4 cells, maraviroc inhibited binding of viral envelope gp120 to CCR5 with IC50 value of 11 nM and prevented the membrane fusion events, which were necessary for viral entry.
ln Vitro |
A powerful selective CCR5 antagonist, maraviroc (UK-427857) effectively inhibits the human immunodeficiency virus type 1 (HIV-1). With IC50s ranging from 7 to 30 nM for MIP-1β, MIP-1α, and RANTES, maraviroc suppresses events that follow chemokine-induced intracellular calcium redistribution. In a 5-day antiviral assay employing isolated multiple (Pooled), Maraviroc (UK-427857) is active (IC90) against HIV-1 Ba-L, a laboratory-engineered R5 strain, at low nanomolar doses [1]. The assay assessed IC90 on donor PBMC (3.1 nM), IC90 on single-donor PBMC (1.8 nM), or IC90 on PM-1 cells (1.1 nM).
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ln Vivo |
Following intravenous injection, clearance values were moderate to high in dogs and rats (74 and 21 mL/min/kg, respectively). In both species, maraviroc likewise exhibits a moderate volume of distribution (4.3 to 6.5 L/kg). Maraviroc has a half-life of 0.9 hours in rats and 2.3 hours in dogs. Dogs received 2 mg/kg orally, and 1.5 hours later, Cmax (256 ng/mL) was reached. 40% of the substance is bioavailable after administration. Roughly thirty percent of the oral dose is absorbed from the gut in rats, according to research on concentrations found in the portal vein following oral administration [1]. Maraviroc specifically decreases the recruitment of leukocytes harboring CCR5 in DSS/TNBS colitis and metastatic models, thereby mitigating the development of intestinal inflammation[2].
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Animal Protocol |
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References |
[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
[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. [3]. Romero-Sánchez MC, et al. Effect of maraviroc on HIV-disease progression-related biomarkers. Antimicrob Agents Chemother. 2012 Nov;56(11):5858-64. [4]. Huilin Mou, et al. NRSF and CCR5 Established Neuron-glia Communication during Acute and Chronic Stresses. Journal of Drug Metabolism & Toxicology. January 10, 2016 |
Molecular Formula |
C29H41F2N5O
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Molecular Weight |
513.6656
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CAS # |
376348-65-1
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Related CAS # |
Maraviroc-d6;1033699-22-7
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Appearance |
Solid powder
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SMILES |
FC1(C([H])([H])C([H])([H])C([H])(C([H])([H])C1([H])[H])C(N([H])[C@]([H])(C1C([H])=C([H])C([H])=C([H])C=1[H])C([H])([H])C([H])([H])N1[C@]2([H])C([H])([H])C([H])([H])[C@@]1([H])C([H])([H])C([H])(C2([H])[H])N1C(C([H])([H])[H])=NN=C1C([H])(C([H])([H])[H])C([H])([H])[H])=O)F
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.87 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.87 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.87 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (4.87 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 2.5 mg/mL (4.87 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 6: ≥ 0.5 mg/mL (0.97 mM) (saturation unknown) in 1% DMSO 99% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 7: 2% DMSO +Corn oil : 10 mg/mL |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.