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Maraviroc (UK-427857) CCR5 antagonist

Cat.No.S2003

Maraviroc is a 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 in the treatment of HIV infection.

Maraviroc (UK-427857) CCR antagonist Chemical Structure

Chemical Structure

Molecular Weight: 513.67

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	Integrase Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite Reverse Transcriptase HIV
Other CCR Inhibitors	Cenicriviroc INCB3344 SB-297006 ZK756326 2HCl BX471 (ZK-811752) Adaptavir (DAPTA) R243 RS102895 BMS-813160 AZD2098

Q&A of Maraviroc (UK-427857): Insights Rooted in Extensive Publications, Every Answer Cited

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Solubility in DMSO or Water

In vitro
Batch:

DMSO : 100 mg/mL (194.67 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 100 mg/mL (194.67 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 100 mg/mL (194.67 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 100 mg/mL (194.67 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 100 mg/mL (194.67 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.200mg/ml (2.34mM)	Taking the 1 mL working solution as an example, add 50 μL of 24 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	10% DMSO 1 40% PEG 300 2 5%Tween80 3 45% water Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	12.500mg/ml (24.33mM)	Taking the 1 mL working solution as an example, add 100 μL of 125mg/ml clear DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue adding Dilute 450 μL ddH2O to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.73mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	7.500mg/ml (14.60mM)	Taking the 1 mL working solution as an example, add 50 μL of 150 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Read more about Maraviroc (UK-427857) solubility in DMSO or water

Search directly for a cell line, or select a cell line to find matched working concentrations

Read more about Maraviroc (UK-427857) working concentrations for cell culture treatment

Maraviroc (UK-427857) is a potent inhibitor of HIV-1 (IC90 in vitro), CCR5, TBI, FCS, CIBI, ICH, pain, opioid effectiveness, HIV, HIV-1 RNA (<50 copies/mL), CCL5, Acute lymphoblastic leukemia, Acute myeloid leukemia, Hodgkin lymphoma, MSC recruitment, monocyte recruitment, tumor cell growth, doxorubicin, brentuximab vedotin, heterospheroid formation, cell viability, tumor growth (>50% reduction), monocyte accumulation, Treg migration, lung metastasis, angiogenesis, metastasis, survival, immune-suppressive myeloid cells, antitumor immunity, thoracic metastasis, trastuzumab resistance, CAF growth, tumor xenograft growth, macrophages, CRC, MSC-induced tumor xenograft growth, tumor cell migration, tumor cell invasion, Gastric cancer cell dissemination, M1 polarization of microglia, microglia migration, invasion, xenograft growth, proliferation, caspase activation, Bax increase, cell cycle progression, PDAC liver metastasis, macrophage migration, overall survival, behavioural outcomes, motor performance, cognitive outcomes, dendritic spine preservation, axonal projections to contralateral cortex, inflammatory response, CREB/DLK signalling, Akt, vasculature, endothelial cell migration, mTOR/Akt pathway, M1/M2 macrophages, cancer cell killing, migration, breast cancer cell homing to the lungs, prostate cancer metastasis, M1 macrophages, pro-migratory chemokines and cytokines, T cell agglomeration, macrophage repolarisation, tumour-promoting inflammation, liver metastases, inflammation, IL-6, sICAM1, sVCAM-1, arterial stiffness, neointimal development, endothelial function, circulating endothelial microparticles, leukocyte-endothelial adhesion, IL-6 secretion, IL-8 secretion, sICAM1 secretion, sVCAM1 secretion, senescence, STAT1 pathways, PDK1 pathways, AKT pathways, HIV-induced BBB dysfunction. Maraviroc (UK-427857) exhibits the greatest inhibitory potency toward HIV-1 RNA.

Read more about selectivity & specificity

Mechanism of Action

Information	Maraviroc (UK-427857) is a potent, allosteric CCR5 antagonist. It affects CCL5/CCR5 and PI3K/AKT signaling pathways by binding to the receptor's transmembrane domain and stabilizing its inactive conformation, effectively inhibiting HIV-1 entry, macrophage polarization, and inflammation.
Read more about Maraviroc (UK-427857) IC50 for cell-based and cell-free assays
Primary Applications and Mechanism of Action

Read more about Maraviroc (UK-427857) Mechanism of Action

Chemical Information, Storage & Stability

Molecular Weight	513.67	Formula	C₂₉H₄₁F₂N₅O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	376348-65-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	UK-427857			Smiles	CC1=NN=C(N1C2CC3CCC(C2)N3CCC(C4=CC=CC=C4)NC(=O)C5CCC(CC5)(F)F)C(C)C

Read more about storage & stability

Read more comparative analysis about Maraviroc (UK-427857)

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
What vehicle do you recommend to dissolve it for in vivo experiments?

Answer:
It can be dissolved in 5% DMSO/castor oil at 62 mg/ml as suspension for oral administration. As to a clear solution for injection, following three vehicles at 10mg/ml will help: 1. 2% DMSO/castor oil; 2. 2%DMSO/sunflower oil; 3. 2%DMSO/30%PEG 300/ddH2O.

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions

Concentration (start):

Dilution-folds:

Computed Result

C1=C0/X	C1:		LOG(C1):
C2=C1/X	C2:		LOG(C2):
C3=C2/X	C3:		LOG(C3):
C4=C3/X	C4:		LOG(C4):
C5=C4/X	C5:		LOG(C5):
C6=C5/X	C6:		LOG(C6):
C7=C6/X	C7:		LOG(C7):
C8=C7/X	C8:		LOG(C8):