Art. -Nr.: HY-13660

Mocravimod hydrochloride

(Synonyms: KRP-203)

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

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).

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Reinheit: 99.99%
CAS. Nr.: 509088-69-1
Formel: C₂₄H₂₇Cl₂NO₃S
Molecular Weight:480.45

Speicherung:

4°C, sealed storage, away from moisture

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

Mocravimod hydrochloride Chemical Structure

CAS. Nr.: 509088-69-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

S1PR1^[1]

Alle LPL Receptor Isoform-spezifische Produkte anzeigen :

Alle Akt Isoform-spezifische Produkte anzeigen :

Alle GSK-3 Isoform-spezifische Produkte anzeigen :

Alle JAK Isoform-spezifische Produkte anzeigen :

Alle STAT Isoform-spezifische Produkte anzeigen :

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 509088-69-1
Appearance Solid
Molecular Weight 480.45
Formel C₂₄H₂₇Cl₂NO₃S
Color White to off-white
SMILES

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

KRP-203
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

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

Publications (2)

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Journal Impact Factor

Cell Biol Toxicol

The novel sphingosine-1-phosphate receptor modulator KRP-203 prevents myocardial ischemia-reperfusion injury by preserving mitochondrial function through activation of the RISK and SAFE signaling pathways. [Abstract]

2025 Nov 27;41(1):159. PMID: 41307722
bioRxiv

Sphingosine-1-phosphate receptor modulators resensitize FLT3-ITD acute myeloid leukemia cells with NRAS mutations to FLT3 inhibitors. [Abstract]

2025 Nov 24:2025.11.21.689510. PMID: 41341164

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0814 mL

10.4069 mL

20.8138 mL

5 mM

0.4163 mL

2.0814 mL

4.1628 mL

10 mM

0.2081 mL

1.0407 mL

2.0814 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.20 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Dertschnig S, et al. Mocravimod, a Selective Sphingosine-1-Phosphate Receptor Modulator, in Allogeneic Hematopoietic Stem Cell Transplantation for Malignancy. Transplant Cell Ther. 2023 Jan;29(1):41.e1-41.e9. [Content Brief]

[2]. Suzuki et al. PS11.7: Mocravimod, a novel immunosuppressant, not only suppresses immune rejection but also promotes engraftment of intraportally transplanted islets by its anti-inflammatory and anti-coagulant effects. Transplantation 109(10S):p S28, October 2025.

[3]. Potì F, et al. Mocravimod, sphingosine 1-phosphate receptor type 1 agonist, ameliorates atherosclerosis in LDL-R-/- mice. Arterioscler Thromb Vasc Biol. 2013 Jul;33(7):1505-12. [Content Brief]

[4]. Wu N, et al. The novel sphingosine-1-phosphate receptor modulator Mocravimod prevents myocardial ischemia-reperfusion injury by preserving mitochondrial function through activation of the RISK and SAFE signaling pathways. Cell Biol Toxicol. 2025 Nov 27;41(1):159. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Mocravimod hydrochloride

2 Cited Publications

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Mocravimod hydrochloride

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Publications Citing Use of MedChemExpress (MCE) Mocravimod hydrochloride

Alle LPL Receptor Isoform-spezifische Produkte anzeigen

Alle Akt Isoform-spezifische Produkte anzeigen

Alle GSK-3 Isoform-spezifische Produkte anzeigen

Alle JAK Isoform-spezifische Produkte anzeigen

Alle STAT Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Mocravimod hydrochloride Related Classifications

Art. -Nr.: HY-13660