| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
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| Targets |
S1PR1
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|---|---|
| ln Vivo |
Mocravimod hydrochloride (KRP-203) reduces atherosclerosis in LDL-R/ mice [1].
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| Animal Protocol |
Inbred male DA (MHC haplotype: RT1a) rats
0.1 and 1 mg/kg Orally; daily; for 100 days |
| References |
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| Additional Infomation |
Mocravimod Hydrochloride is the hydrochloride salt form of mocravimod, a sphingosine 1-phosphate (S1P) receptor agonist, with potential immunosuppressive activity. Upon administration of mocravimod, this agent binds to S1P receptors on lymphocytes, which prevents binding of serum S1P to S1P receptors and leads to S1P receptor internalization. This reduces the number of circulating blood leukocytes and accelerates lymphocyte homing into peripheral lymph nodes, thereby preventing their infiltration into peripheral inflammatory sites. This agent also decreases the production of inflammatory cytokines by lymphocytes, such as interferon gamma (IFN-g), interleukin-12 (IL-12), and tumor necrosis factor (TNF).
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| 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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