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> Maraviroc [376348-65-1]

Maraviroc [376348-65-1]

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Referência HY-13004-10mg

Tamanho : 10mg

Marca : MedChemExpress

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Description

Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV.

IC50 & Target[1]

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)

Cellular Effect
Cell Line Type Value Description References
HOS CC50
> 200 nM
Compound: MVC
Cytotoxicity against human HOS cells after 48 hrs by MTT assay
Cytotoxicity against human HOS cells after 48 hrs by MTT assay
[PMID: 30234300]
PBMC CC50
> 200 nM
Compound: MVC
Cytotoxicity against human PBMC after 48 hrs by MTT assay
Cytotoxicity against human PBMC after 48 hrs by MTT assay
[PMID: 30234300]
TZM CC50
> 200 μM
Compound: MVC
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]
In Vitro

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.

Maraviroc Related Antibodies

Solvant et solubilité
In Vitro: 

DMSO : 50 mg/mL (97.34 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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
Pureté et documentation
Références

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