2. GPCR/G Protein Immunology/Inflammation Anti-infection
  3. CCR HIV
  4. Vicriviroc maleate

Vicriviroc maleate  (Synonyms: SCH-417690 maleate; SCH-D maleate)

Cat. No.: HY-17377 Purity: 99.91%
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Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is a potent, selective, oral bioavailable and CNS penetrated antagonist of CCR5, with a Ki of 2.5 nM, and also inhibits HIV-1 in PBMC cells, with IC90s of 3.3 nM (JrFL), 2.8 nM (ADA-M), 1.8 nM (301657), 4.9 nM (JV1083) and 10 nM (RU 570).

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Vicriviroc maleate Chemical Structure

Vicriviroc maleate Chemical Structure

CAS No. : 599179-03-0

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Solid + Solvent
10 mM * 1 mL in DMSO
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Solution
10 mM * 1 mL in DMSO USD 254 In-stock
Solid
5 mg USD 231 In-stock
10 mg USD 374 In-stock
25 mg USD 748 In-stock
50 mg USD 1188 In-stock
100 mg USD 1892 In-stock
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Vicriviroc maleate Related Antibodies

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

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Description

Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is a potent, selective, oral bioavailable and CNS penetrated antagonist of CCR5, with a Ki of 2.5 nM, and also inhibits HIV-1 in PBMC cells, with IC90s of 3.3 nM (JrFL), 2.8 nM (ADA-M), 1.8 nM (301657), 4.9 nM (JV1083) and 10 nM (RU 570).

IC50 & Target[1]

CCR5

2.5 nM (Ki)

HIV-1 (301657)

1.8 nM (IC90, in PBMC cells)

HIV-1 (ADA-M)

2.8 nM (IC90, in PBMC cells)

HIV-1 (JrFL)

3.3 nM (IC90, in PBMC cells)

HIV-1 (JV1083)

4.9 nM (IC90, in PBMC cells)

HIV-1 (RU 570)

10 nM (IC90, in PBMC cells)

In Vitro

Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is a potent, selective and oral bioavailable inhibitor of CCR5, with a Ki of 2.5 nM, and also inhibits HIV-1 in PBMC cells, with IC90s of 3.3 (JrFL), 2.8 (ADA-M), 1.8 (301657), 4.9 (JV1083) and 10 nM (RU 570). In addition, Vicriviroc maleate shows a mean IC50 and IC90 of 0.45 nM and 4 nM for a panel of HIV isolates, and has weak activity against hERG activity (IC50, 5.8 μM)[1]. Vicriviroc maleate inhibits chemotactic response to MIP-1α with IC50 values below 1 nM, and suppresses RANTES-induced signaling with a mean IC50 of 4.2 ± 1.3 nM. Vicriviroc maleate potently suppresses all the viral isolates tested, with geometric mean EC50s of 0.04-2.3 nM and IC90s of 0.45-18 nM[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Vicriviroc maleate Related Antibodies
In Vivo

Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate; 10 mg/kg) has good oral availablity in rats and monkeys, with no acute CNS or GI effects in rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

649.70

Formula

C32H42F3N5O6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1(N2C[C@H](C)N([C@H](C3=CC=C(C(F)(F)F)C=C3)COC)CC2)CCN(C(C4=C(C)N=CN=C4C)=O)CC1.O=C(O)/C=C\C(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (76.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 25 mg/mL (38.48 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5392 mL 7.6959 mL 15.3917 mL
5 mM 0.3078 mL 1.5392 mL 3.0783 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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 (3.85 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 (3.85 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References
Cell Assay
[2]

Ficoll-purified peripheral blood mononuclear cells (PBMCs) are stimulated in vitro with phytohemagglutinin (PHA) (5 μg/mL) and interleukin-2 (IL-2) (50 U/mL) for 3 to 7 days. The cells are resuspended at 4 × 106/mL in complete medium (RPMI, 10% fetal bovine serum [FBS], 50 U/mL IL-2), seeded into 96-well plates (2 × 105/well), incubated with an equal volume of culture medium containing compound (Vicriviroc) for 1 h at 37°C, and infected in triplicate with 25 to 100 50% tissue culture infectious doses (TCID50) per well of viral inoculum for 3 to 4 h. Cells are washed twice in phosphate-buffered saline (PBS) to remove residual virus and are cultured with compound for 4 to 6 days. HIV-1 replication is quantified by measurement of extracellular p24 antigen in the supernatants by enzyme-linked immunosorbent assay. The 50% effective concentrations (EC50s) and EC90s for each virus are determined using Graphpad PRISM software[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.5392 mL 7.6959 mL 15.3917 mL 38.4793 mL
5 mM 0.3078 mL 1.5392 mL 3.0783 mL 7.6959 mL
10 mM 0.1539 mL 0.7696 mL 1.5392 mL 3.8479 mL
15 mM 0.1026 mL 0.5131 mL 1.0261 mL 2.5653 mL
20 mM 0.0770 mL 0.3848 mL 0.7696 mL 1.9240 mL
25 mM 0.0616 mL 0.3078 mL 0.6157 mL 1.5392 mL
30 mM 0.0513 mL 0.2565 mL 0.5131 mL 1.2826 mL
DMSO 40 mM 0.0385 mL 0.1924 mL 0.3848 mL 0.9620 mL
50 mM 0.0308 mL 0.1539 mL 0.3078 mL 0.7696 mL
60 mM 0.0257 mL 0.1283 mL 0.2565 mL 0.6413 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Vicriviroc maleate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Vicriviroc599179-03-0SCH-417690SCH-DSCH417690SCH 417690CCRHIVCC chemokine receptorHuman immunodeficiency virusInhibitorinhibitorinhibit

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