| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
S1PR1
S1PR1 (sphingosine 1-phosphate receptor type 1) and S1P4. Mocravimod is an agonist of S1P1 and S1P4 with high potency. S1P receptors are G protein-coupled receptors that regulate lymphocyte trafficking, immune function, and vascular integrity. |
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| ln Vitro |
Mocravimod shows EC50 values of 1 nM for S1P1 and 10 nM for S1P4. It is a potent agonist with high selectivity for S1P1 and S1P4. Detailed in vitro activity against additional receptors has not been extensively reported.
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| ln Vivo |
Mocravimod hydrochloride (KRP-203) reduces atherosclerosis in LDL-R/ mice [1].
Mocravimod hydrochloride (0.1 and 1 mg/kg/day, oral) has been evaluated in a rat cardiac allograft model. It ameliorates atherosclerosis in LDL-R-/- mice. Mocravimod regulates chronic colitis in interleukin-10 gene-deficient mice. The compound is orally active with immunosuppressive effects. |
| Enzyme Assay |
S1P1 receptor binding assay: Membranes from cells expressing human S1P1 are incubated with varying concentrations of Mocravimod and [³³P]-S1P in binding buffer at room temperature for 60-90 min. Nonspecific binding is determined with excess unlabeled S1P. Bound radioactivity is measured by filtration. IC50 or Ki values are calculated. S1P1 functional activity: GTPγS binding assay measures receptor activation.
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| Cell Assay |
Lymphocyte trafficking assay: Human peripheral blood mononuclear cells or mouse splenocytes are treated with Mocravimod at varying concentrations for 1-4 hours. Cell migration toward S1P is measured using a Transwell chamber assay. The inhibition of S1P-induced lymphocyte migration is calculated. Alternatively, S1P1 internalization is assessed by flow cytometry.
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| Animal Protocol |
Inbred male DA (MHC haplotype: RT1a) rats
0.1 and 1 mg/kg Orally; daily; for 100 days Rat cardiac allograft model: Rats receive heart transplants from mismatched donors. Mocravimod hydrochloride is administered orally at 0.1 or 1 mg/kg/day. Graft survival is monitored. Mouse colitis model: IL-10 gene-deficient mice (which develop chronic colitis) are treated with Mocravimod orally. Disease severity is assessed by body weight, colon length, histological scoring, and inflammatory cytokine levels. |
| ADME/Pharmacokinetics |
Mocravimod is orally active with potent immunosuppressive effects. It has been evaluated in animal models at doses of 0.1 and 1 mg/kg/day. Detailed pharmacokinetic parameters including bioavailability, half-life, Cmax, and AUC have been reported in preclinical and clinical studies.
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| Toxicity/Toxicokinetics |
Toxicity has been evaluated in preclinical studies. As an S1P receptor agonist, Mocravimod shares class-specific effects including potential bradycardia, lymphopenia, and immunosuppression. The compound has been studied for safety in animal models and early clinical trials for ulcerative colitis.
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| References |
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| Additional Infomation |
Moclavimod hydrochloride is the hydrochloride form of moclavimod, a sphingosine-1-phosphate (S1P) receptor agonist with potential immunosuppressive activity. After administration, moclavimod binds to S1P receptors on lymphocytes, thereby preventing the binding of serum S1P to its receptors and leading to S1P receptor internalization. This reduces the number of leukocytes in the circulating blood and accelerates lymphocyte homing to peripheral lymph nodes, thus preventing their infiltration into sites of peripheral inflammation. Furthermore, the drug can reduce inflammatory cytokines produced by lymphocytes, such as interferon-γ (IFN-γ), interleukin-12 (IL-12), and tumor necrosis factor (TNF).
Mocravimod (KRP-203) is a potent, orally active S1P1 and S1P4 agonist with EC50 values of 1 nM and 10 nM, respectively. It is an immunosuppressant that has been studied in preclinical models of transplant rejection, atherosclerosis, and colitis. The compound has been investigated for ulcerative colitis and other immune-mediated diseases. No approved上市 status has been reported. |
| Molecular Formula |
C24H27CL2NO3S
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|---|---|
| Molecular Weight |
480.44708
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| Exact Mass |
479.108
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| Elemental Analysis |
C, 60.00; H, 5.66; Cl, 14.76; N, 2.92; O, 9.99; S, 6.67
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| CAS # |
509088-69-1
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| Related CAS # |
Mocravimod; 509092-16-4
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| PubChem CID |
11155873
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| Appearance |
White to off-white solid powder
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| Boiling Point |
657.1ºC at 760 mmHg
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| Melting Point |
199-200ºC (DEC.)
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| Flash Point |
351.2ºC
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| LogP |
6.187
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
31
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| Complexity |
487
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OCC(CCC1=CC=C(SC2=CC=CC(OCC3=CC=CC=C3)=C2)C=C1Cl)(N)CO.[H]Cl
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| InChi Key |
MYIFLDFUXIHOCJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H26ClNO3S.ClH/c25-23-14-22(10-9-19(23)11-12-24(26,16-27)17-28)30-21-8-4-7-20(13-21)29-15-18-5-2-1-3-6-18;/h1-10,13-14,27-28H,11-12,15-17,26H2;1H
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| Chemical Name |
2-amino-2-[2-[2-chloro-4-(3-phenylmethoxyphenyl)sulfanylphenyl]ethyl]propane-1,3-diol;hydrochloride
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| Synonyms |
MOCRAVIMOD HYDROCHLORIDE; KRP-203 HCl; KRP-203; KRP203; KRP 203; KRP-203 hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~200 mg/mL (~416.3 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.20 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.20 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.20 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2081 mL | 1.0407 mL | 2.0814 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03019887 | Completed | Drug: reduction of risperidone, haloperidol, olanzapine, quetiapine, aripiprazole, paliperidone, levomepromazine, perphenazine |
Schizophrenia Relapse | Juntendo University | April 2011 | Not Applicable |
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