1. GPCR/G Protein NF-κB Metabolic Enzyme/Protease Immunology/Inflammation PI3K/Akt/mTOR Stem Cell/Wnt Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  2. LPL Receptor Reactive Oxygen Species (ROS) Akt GSK-3 JAK STAT
  3. Mocravimod hydrochloride

Mocravimod hydrochloride  (Synonyms: KRP-203)

Cat. No.: HY-13660 Purity: 99.99%
Handling Instructions Technical Support

Mocravimod (hydrochloride) is an orally active sphingosine-1-phosphate receptor (S1PR) modulator that blocks the signal required by T cells to egress from lymph nodes and other lymphoid organs. Mocravimod (hydrochloride) preferentially binds to S1PR1 over S1PR2 and S1PR3 in cardiomyocytes. Mocravimod (hydrochloride) significantly lowered the concentration of reactive oxygen species (ROS), prevented mitochondrial permeability transition pore opening, boosted mitochondrial membrane potential (MMP), and increased phosphorylation of AKT, EKR, GSK-3β, JAK2, and STAT3. Mocravimod (hydrochloride) retains T cell effector function. Mocravimod (hydrochloride) can be used for the study of acute myelogenous leukemia, diabetes and Myocardial Ischemia-Reperfusion Injury (MIRI).

For research use only. We do not sell to patients.

Mocravimod hydrochloride

Mocravimod hydrochloride Chemical Structure

CAS No. : 509088-69-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
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200 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Mocravimod hydrochloride:

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Mocravimod (hydrochloride) is an orally active sphingosine-1-phosphate receptor (S1PR) modulator that blocks the signal required by T cells to egress from lymph nodes and other lymphoid organs. Mocravimod (hydrochloride) preferentially binds to S1PR1 over S1PR2 and S1PR3 in cardiomyocytes. Mocravimod (hydrochloride) significantly lowered the concentration of reactive oxygen species (ROS), prevented mitochondrial permeability transition pore opening, boosted mitochondrial membrane potential (MMP), and increased phosphorylation of AKT, EKR, GSK-3β, JAK2, and STAT3. Mocravimod (hydrochloride) retains T cell effector function. Mocravimod (hydrochloride) can be used for the study of acute myelogenous leukemia, diabetes and Myocardial Ischemia-Reperfusion Injury (MIRI)[1][2][3][4].

IC50 & Target

S1PR1[1]

In Vitro

Mocravimod (KRP203) (0.2-5 μM, 24 h) (hydrochloride) significantly improves the survival rate of the hypoxia-reoxygenation (H/R) H9c2 cells, reduces lactate dehydrogenase (LDH) release, and decreases apoptosis[4].
Mocravimod (0.2-1 μM, 24 h) (hydrochloride) significantly reduces reactive oxygen species (ROS) levels, improves mitochondrial membrane potential, and inhibits the opening of the mitochondrial permeability transition pore (mPTP) in hypoxia-reoxygenation (H/R) H9c2 cells[4].
Mocravimod (0.2-1 μM, 24 h) (hydrochloride) inhibits the expression of mitochondrial-mediated apoptosis pathway proteins such as cytochrome C, caspase-9, and caspase-3[4].
Mocravimod (0.2-1 μM, 24 h) (hydrochloride) significantly increases the phosphorylation levels of key signaling pathway proteins in hypoxia-reoxygenation (H/R) H9c2 cells, including AKT (Ser473), ERK (Thr202/Tyr204), GSK-3β (Ser9), JAK2 (Tyr1007/1008), and STAT3 (Ser727)[4].

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

Apoptosis Analysis[1]

Cell Line: Hypoxia-Reoxygenation (H/R) H9c2 Cells
Concentration: 0.2 μM, 1 μM, 5 μM
Incubation Time: 24 h
Result: Induced apoptosis.

Western Blot Analysis[1]

Cell Line: Hypoxia-Reoxygenation (H/R) H9c2 Cells
Concentration: 0.2 μM, 1 μM
Incubation Time: 24 h
Result: Inhibited the expression of mitochondrial-mediated apoptosis pathway proteins such as cytochrome C, caspase-9, and caspase-3.
In Vivo

Mocravimod (KRP203) (once daily/twice daily, 1-5 days) (hydrochloride) significantly improves the survival rate of islet transplantation in C57BL/6 mice with diabetes induced by intravenous streptozotocin[2].
Mocravimod (3.0 mg/kg, i.p., thrice weekly) (hydrochloride) significantly inhibits the development of atherosclerotic lesions in mice on a high-cholesterol diet, and this effect was independent of changes in blood lipids, but rather by regulating the infiltration of inflammatory cells within plaques[3].

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

Animal Model: Low-density lipoprotein receptor-deficient mice (LDL-R-/-) on cholesterol-rich diet[3].
Dosage: 3 mg/kg
Administration: I.p., thrice weekly for 6-16 weeks
Result: Significantly reduced the lesion area of the aortic root and the entire aorta.
Decreased levels of macrophages (MOMA-2 positive) and T cells (CD3 positive) in plaques.
No effect on plasma lipid levels (total cholesterol, HDL cholesterol, triglycerides), body weight, or liver and kidney function parameters (such as ALT, BUN, creatinine).
Decreased CD4+ and CD8+ T cells in the spleen and lymph nodes, with decreased expression of the activation marker CD69.
Decreased MHC-II expression (activation marker) in F4/80+ macrophages and CD11c+ dendritic cells; reduced cytokine (TNF-α, MCP-1, IL-6) production after in vitro stimulation.
Clinical Trial
Molecular Weight

480.45

Formula

C24H27Cl2NO3S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OCC(CCC1=CC=C(SC2=CC=CC(OCC3=CC=CC=C3)=C2)C=C1Cl)(N)CO.[H]Cl

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 : 200 mg/mL (416.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0814 mL 10.4069 mL 20.8138 mL
5 mM 0.4163 mL 2.0814 mL 4.1628 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.

  • 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 (5.20 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 (5.20 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.99%

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
DMSO 1 mM 2.0814 mL 10.4069 mL 20.8138 mL 52.0345 mL
5 mM 0.4163 mL 2.0814 mL 4.1628 mL 10.4069 mL
10 mM 0.2081 mL 1.0407 mL 2.0814 mL 5.2035 mL
15 mM 0.1388 mL 0.6938 mL 1.3876 mL 3.4690 mL
20 mM 0.1041 mL 0.5203 mL 1.0407 mL 2.6017 mL
25 mM 0.0833 mL 0.4163 mL 0.8326 mL 2.0814 mL
30 mM 0.0694 mL 0.3469 mL 0.6938 mL 1.7345 mL
40 mM 0.0520 mL 0.2602 mL 0.5203 mL 1.3009 mL
50 mM 0.0416 mL 0.2081 mL 0.4163 mL 1.0407 mL
60 mM 0.0347 mL 0.1734 mL 0.3469 mL 0.8672 mL
80 mM 0.0260 mL 0.1301 mL 0.2602 mL 0.6504 mL
100 mM 0.0208 mL 0.1041 mL 0.2081 mL 0.5203 mL
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  • 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.

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Product Name:
Mocravimod hydrochloride
Cat. No.:
HY-13660
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