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Maraviroc (UK427857)

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Maraviroc (UK427857)
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Cat #: V1810 CAS #: 376348-65-1 Purity ≥ 98%

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.

References: 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

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Molecular Weight (MW)513.67
Molecular FormulaC29H41F2N5O
CAS No.376348-65-1
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 100 mg/mL (194.7 mM)r
Water:<1 mg/mLr
Ethanol: 100 mg/mL (194.7 mM)
Solubility In Vivo2% DMSO+Corn oil: 10 mg/mL
SynonymsUK427857; UK-427,857; UK-427857; UK-427,857; UK 427857; Selzentry; Celsentri; Selzentry;
ProtocolIn VitroMaraviroc (UK-427857) is a selective CCR5 antagonist with potent anti-human immunodeficiency virus type 1 (HIV-1) activity. Maraviroc inhibits chemokine-induced downstream events of intracellular calcium redistribution, to MIP-1β, MIP-1α, and ICs of RTES50 The range is 7 to 30 nM. Maraviroc (UK-427857) is active against HIV-1 Ba-L, a laboratory-engineered R5 strain, at low nanomolar concentrations (IC).90), using isolated multiple (combined) donor PBMC (IC) for measurement in a 5-day antiviral assay90, 3.1 nM), single-donor PBMC (IC90, 1.8 nM) or PM-1 cells (IC).90,1.1 nM)
In VivoClearance values for rats and dogs after intravenous administration were moderate to high (74 mL/min/kg, respectively). Maraviroc also has a moderate volume of distribution in both species (21.4 to 3.6 l/kg). The half-life value of Maraviroc is 5.0 h in rats and 9.2 h in dogs. After giving the dog orally (3 mg/kg), C.max (256 ng/mL) occurs in 1.5 hours. After administration, bioavailability is 40%. In rats, studies of concentrations obtained in the portal vein after oral administration have shown that approximately 30% of the administered dose is absorbed from the intestine
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM1.9468 mL9.7339 mL19.4678 mL38.9355 mL
5mM0.3894 mL1.9468 mL3.8936 mL7.7871 mL
10mM0.1947 mL0.9734 mL1.9468 mL3.8936 mL
20mM0.0973 mL0.4867 mL0.9734 mL1.9468 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (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.