Maraviroc (UK427857)

Alias: UK427857; UK-427,857;UK-427857;UK-427,857; UK 427857;Selzentry; Celsentri; Selzentry;
Cat No.:V1810 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 (UK427857) Chemical Structure CAS No.: 376348-65-1
Product category: CCR
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
500mg
Other Sizes

Other Forms of Maraviroc (UK427857):

  • Maraviroc-d6
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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.

Biological Activity I Assay Protocols (From Reference)
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).
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].
Animal Protocol
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; ~64 μg; A 25 μL volume of the gel formulation is carefully applied in to the vaginal vault of mice.
Humanized BALB/c-Rag2 / γc / and BALB/c-Rag1 / γc / (RAG-hu) mice
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
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C29H41F2N5O
Molecular Weight
513.67
CAS #
376348-65-1
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
Synonyms
UK427857; UK-427,857;UK-427857;UK-427,857; UK 427857;Selzentry; Celsentri; Selzentry;
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 100 mg/mL (194.7 mM)
Water:<1 mg/mL
Ethanol:100 mg/mL (194.7 mM)
Solubility (In Vivo)
2%DMSO+Corn oil: 10 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
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.

Calculator

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Biological Data
  • Maraviroc

    Effects of maraviroc on CCR5-mediated signaling. Antimicrob Agents Chemother. 2005 Nov;49(11):4721-32.
  • Maraviroc

    Maraviroc-dependent inhibition of gp120 binding to CCR5 (red) and gp160-CCR5-mediated cell-cell fusion (black). Antimicrob Agents Chemother. 2005 Nov;49(11):4721-32.
  • Maraviroc

    Representative dose response for maraviroc-dependent inhibition of HIV strain Ba-L replication in pooled isolated peripheral blood lymphocytes (blue line and data points) compared to that with RANTES (red line and data points). Antimicrob Agents Chemother. 2005 Nov;49(11):4721-32.
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