| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg | |||
| 100mg | |||
| 250mg | |||
| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
S1PR1 ( EC50 = 1 nM ); S1PR5 ( EC50 = 36 nM ); S1PR5 ( EC50 = 228 nM ); S1PR4 ( EC50 = 2134 nM )
Cenerimod selectively targets and activates the sphingosine-1-phosphate receptor 1 (S1P1). Upon binding to S1P1, cenerimod induces receptor internalization and degradation, leading to the functional antagonism of S1P1 signaling on lymphocytes. This prevents the egress of lymphocytes from lymph nodes and other secondary lymphoid organs, reducing the number of circulating lymphocytes available to infiltrate target tissues. This mechanism reduces the lymphocyte-mediated immune response and inflammation in autoimmune diseases. |
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| ln Vitro |
Cenerimod is a very strong S1P1 receptor agonist in (35S)-GTPγS assays utilizing preparations of HUVEC cell membranes, with an EC50 of 2 nM[1].
Cenerimod increases Ca2+ signaling and activates G protein in CHO cells, with EC50s of 1 nM and 124 nM, respectively[1]. Cenerimod (5 μM; 24 h) prevents fibroblasts from producing collagen[2]. Cenerimod exhibits potent in vitro activity as an S1P1 agonist, with high selectivity over other S1P receptor subtypes. It effectively induces S1P1 internalization and degradation in lymphocytes, as demonstrated in cell-based assays. The compound has been shown to reduce lymphocyte migration in vitro and to modulate cytokine production in immune cells. Cenerimod's selectivity and potency make it a promising candidate for the treatment of autoimmune diseases. |
| ln Vivo |
Cenerimod (0.1-10 mg/kg; a single p.o.) reversibly and dose-dependently decreases the number of circulating lymphocytes in rats[1].
Cenerimod (6 mg/kg/day for 30 days; p.o.) attenuates disease in a mouse experimental autoimmune encephalitis (EAE) model[1]. Cenerimod (10 mg/kg/day for 42 days; p.o.) reduces lung and skin fibrosis in Scl-cGVHD mice[2]. Cenerimod has demonstrated in vivo efficacy in preclinical models of autoimmune diseases, including models of systemic lupus erythematosus (SLE) and multiple sclerosis. In these models, oral administration of cenerimod reduced lymphocyte counts in the blood and tissues, decreased inflammatory cytokine production, and ameliorated disease symptoms. The compound has also been evaluated in clinical trials for SLE, where it showed promising results in reducing disease activity and flares. |
| Enzyme Assay |
Cenerimod's activity can be assessed using in vitro receptor binding assays to measure its affinity for S1P1 and other S1P receptor subtypes. Radioligand binding assays using 33P-S1P or other labeled ligands are commonly used. The compound's ability to induce S1P1 internalization can be evaluated using flow cytometry or fluorescence microscopy in cells expressing fluorescently tagged S1P1. Functional assays measuring GTPγS binding or cAMP accumulation are used to assess receptor activation.
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| Cell Assay |
Cellular assays for cenerimod involve treating lymphocytes with the compound and measuring S1P1 internalization, cell migration, and cytokine production. S1P1 internalization can be assessed by flow cytometry using antibodies against S1P1 or by microscopy. Lymphocyte migration assays using transwell chambers are used to measure the compound's effects on cell migration. Cytokine production can be measured by ELISA or multiplex assays.
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| Animal Protocol |
Male Wistar rats weighing 294-510 g
0.1, 0.3, 1, 3 and 10 mg/kg A single p.o. In vivo animal model protocols for cenerimod involve oral administration to animal models of autoimmune diseases. In SLE models (e.g., MRL/lpr mice or NZB/W F1 mice), the compound is administered daily, and disease progression is monitored by measuring proteinuria, anti-dsDNA antibody levels, and histopathological analysis of kidney tissues. In multiple sclerosis models (EAE), clinical scores and histopathological analysis of the spinal cord are performed. |
| ADME/Pharmacokinetics |
Cenerimod is an orally active compound with favorable pharmacokinetic properties. It is well-absorbed after oral administration and has a half-life that supports once-daily dosing. The compound is extensively metabolized in the liver, and its metabolites are excreted primarily in the urine and feces. Pharmacokinetic data from clinical trials have shown dose-proportional exposure and low inter-patient variability. Dose adjustment is required in patients with hepatic impairment.
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| Toxicity/Toxicokinetics |
Cenerimod has a well-characterized safety profile from clinical trials. Common adverse effects include bradycardia, headache, and gastrointestinal disturbances. As an S1P receptor modulator, cenerimod can cause a transient decrease in heart rate upon treatment initiation, requiring dose titration. Other potential adverse effects include infections due to immunosuppression, macular edema, and liver enzyme elevations.
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| References | |
| Additional Infomation |
Cenerimod is currently being used in clinical trials for the treatment of systemic lupus erythematosus (SLE).
Drug Indication Treatment of systemic lupus erythematosus (SLE) Treatment with cenerimod is associated with a transient decrease in heart rate. Macular edema has been reported with other S1P receptor modulators and may also occur with cenerimod. Infections are a potential risk due to the immunosuppressive effects of the compound. |
| Molecular Formula |
C25H31N3O5
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|---|---|
| Molecular Weight |
453.54
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| Exact Mass |
453.226
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| Elemental Analysis |
C, 66.21; H, 6.89; N, 9.27; O, 17.64
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| CAS # |
1262414-04-9
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| Related CAS # |
1262414-04-9
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| PubChem CID |
49871973
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| Appearance |
White to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
670.7±65.0 °C at 760 mmHg
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| Flash Point |
359.4±34.3 °C
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| Vapour Pressure |
0.0±2.2 mmHg at 25°C
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| Index of Refraction |
1.578
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| LogP |
5.92
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
33
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| Complexity |
592
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| Defined Atom Stereocenter Count |
1
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| SMILES |
OC[C@H](O)COC1=C(C)C=C(C2=NOC(C3=CC(C4CCCC4)=NC(OC)=C3)=N2)C=C1CC
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| InChi Key |
KJKKMMMRWISKRF-FQEVSTJZSA-N
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| InChi Code |
InChI=1S/C25H31N3O5/c1-4-16-10-18(9-15(2)23(16)32-14-20(30)13-29)24-27-25(33-28-24)19-11-21(17-7-5-6-8-17)26-22(12-19)31-3/h9-12,17,20,29-30H,4-8,13-14H2,1-3H3/t20-/m0/s1 SMILES
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| Chemical Name |
(2S)-3-[4-[5-(2-cyclopentyl-6-methoxypyridin-4-yl)-1,2,4-oxadiazol-3-yl]-2-ethyl-6-methylphenoxy]propane-1,2-diol
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| Synonyms |
ACT-334441; ACT334441; ACT 334441
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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 |
| 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: ~100 mg/mL (~220.5 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.51 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 (5.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2049 mL | 11.0244 mL | 22.0488 mL | |
| 5 mM | 0.4410 mL | 2.2049 mL | 4.4098 mL | |
| 10 mM | 0.2205 mL | 1.1024 mL | 2.2049 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 |
| NCT05672576 | Recruiting | Drug: Cenerimod Drug: Placebo |
Lupus Erythematosus, Systemic | Idorsia Pharmaceuticals Ltd. | June 26, 2023 | Phase 3 |
| NCT05648500 | Recruiting | Drug: Cenerimod Drug: Placebo |
Lupus Erythematosus, Systemic | Idorsia Pharmaceuticals Ltd. | December 13, 2022 | Phase 3 |
| NCT04819464 | Recruiting | Drug: Cenerimod | Healthy Hepatic Impairment |
Idorsia Pharmaceuticals Ltd. | August 19, 2021 | Phase 1 |
| NCT02914223 | Completed | Drug: Cenerimod | Healthy Subjects | Idorsia Pharmaceuticals Ltd. | September 1, 2016 | Phase 1 |
| NCT05004311 | Completed | Drug: Cenerimod | Healthy Renal Impairment |
Idorsia Pharmaceuticals Ltd. | September 27, 2021 | Phase 1 |
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