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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
Cenerimod (ACT-334441) is a potent and orally bioavailable immunomodulator, which exhibited an EC50 of 2.7 nM. Cenerimod is an agonist for the G protein-coupled receptor S1 P1/EDG1, and it reduces the amount of circulating and infiltrating T- and B-lymphocytes without impairing their maturation, memory, or expansion. This results in a potent and prolonged immunomodulatory effect. Cenerimod may be helpful in the treatment or prevention of illnesses linked to immune system activation.
Targets |
S1PR1 ( EC50 = 1 nM ); S1PR5 ( EC50 = 36 nM ); S1PR5 ( EC50 = 228 nM ); S1PR4 ( EC50 = 2134 nM )
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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]. |
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]. |
Animal Protocol |
Male Wistar rats weighing 294-510 g
0.1, 0.3, 1, 3 and 10 mg/kg A single p.o. |
References |
Molecular Formula |
C25H31N3O5
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Molecular Weight |
453.54
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Exact Mass |
453.23
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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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Appearance |
Solid powder
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SMILES |
CCC1=C(C(=CC(=C1)C2=NOC(=N2)C3=CC(=NC(=C3)OC)C4CCCC4)C)OC[C@H](CO)O
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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 |
The chemical structure of cenerimod. Pharmacol Res Perspect . 2017 Dec;5(6):e00370. td> |
Cenerimod does not induce contraction of rat mesenteric artery. Pharmacol Res Perspect . 2017 Dec;5(6):e00370. td> |
Cenerimod does not induce rat trachea ring contraction. Pharmacol Res Perspect . 2017 Dec;5(6):e00370. td> |