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) Mitochondrial Metabolism Akt GSK-3 JAK STAT
  3. Mocravimod

Mocravimod  (Synonyms: KRP-203 free base)

Cat. No.: HY-109038 Purity: 98.39%
Handling Instructions Technical Support

Mocravimod (KRP-203 free base) is a sphingosine-1-phosphate receptor (S1PR) modulator that blocks the signal required by T cells to egress from lymph nodes and other lymphoid organs. Mocravimod preferentially binds to S1PR1 over S1PR2 and S1PR3 in cardiomyocytes. Mocravimod 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 retains T cell effector function. Mocravimod 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

Mocravimod Chemical Structure

CAS No. : 509092-16-4

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
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Customer Review

Based on 2 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Mocravimod (KRP-203 free base) is a sphingosine-1-phosphate receptor (S1PR) modulator that blocks the signal required by T cells to egress from lymph nodes and other lymphoid organs. Mocravimod preferentially binds to S1PR1 over S1PR2 and S1PR3 in cardiomyocytes. Mocravimod 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 retains T cell effector function. Mocravimod can be used for the study of acute myelogenous leukemia, diabetes and Myocardial Ischemia-Reperfusion Injury (MIRI)[1][2][3][4].

IC50 & Target

S1PR1

 

GSK-3β

 

STAT3

 

JAK2

 

In Vitro

Mocravimod (0.2-5 μM, 24 h) 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) 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) 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) 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[4]

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[4]

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 (once daily/twice daily, 1-5 days) significantly improves the survival rate of islet transplantation in C57BL/6 mice with diabetes induced by intravenous Streptozotocin (HY-13753)[2].
Mocravimod (3.0 mg/kg, i.p., thrice weekly) 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.
Molecular Weight

443.99

Formula

C24H26ClNO3S

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (225.23 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 2.2523 mL 11.2615 mL 22.5230 mL
5 mM 0.4505 mL 2.2523 mL 4.5046 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Working solution concentration: mg/mL
Purity & Documentation
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. 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 2.2523 mL 11.2615 mL 22.5230 mL 56.3076 mL
5 mM 0.4505 mL 2.2523 mL 4.5046 mL 11.2615 mL
10 mM 0.2252 mL 1.1262 mL 2.2523 mL 5.6308 mL
15 mM 0.1502 mL 0.7508 mL 1.5015 mL 3.7538 mL
20 mM 0.1126 mL 0.5631 mL 1.1262 mL 2.8154 mL
25 mM 0.0901 mL 0.4505 mL 0.9009 mL 2.2523 mL
30 mM 0.0751 mL 0.3754 mL 0.7508 mL 1.8769 mL
40 mM 0.0563 mL 0.2815 mL 0.5631 mL 1.4077 mL
50 mM 0.0450 mL 0.2252 mL 0.4505 mL 1.1262 mL
60 mM 0.0375 mL 0.1877 mL 0.3754 mL 0.9385 mL
80 mM 0.0282 mL 0.1408 mL 0.2815 mL 0.7038 mL
100 mM 0.0225 mL 0.1126 mL 0.2252 mL 0.5631 mL
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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.

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Mocravimod
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