Cenerimod - CAS 1262414-04-9
Catalog number: 1262414-04-9
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C25H31N3O5
Molecular Weight:
453.54
COA:
Inquire
Targets:
Others
Description:
Cenerimod is an active Lysosphingolipid receptor agonist originated by Actelion Pharmaceuticals and EC50 value is 2.7 nM. It is a S1P1/EDG1 receptor agonist and has a long-lasting immunomodulating effect through reducing the number of circulating and infiltrating T- and B-lymphocytes, without affecting their maturation, memory, or expansion. Cenerimod is in phase I/II clinical trials for the treatment of Systemic lupus erythematosus.
Purity:
98%
Appearance:
Powder
Synonyms:
ACT 334441;(S)-3-(4-(5-(2-cyclopentyl-6-methoxypyridin-4-yl)-1,2,4-oxadiazol-3-yl)-2-ethyl-6-methylphenoxy)propane-1,2-diol
Solubility:
Soluble in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
Systemic lupus erythematosus
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
KJKKMMMRWISKRF-FQEVSTJZSA-N
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
Canonical SMILES:
CCc1cc(cc(c1OC[C@H](CO)O)C)c2nc(on2)c3cc(nc(c3)OC)C4CCCC4
Current Developer:
Originator:Actelion Pharmaceuticals
1.Cenerimod, a novel selective S1P
Piali L;Birker-Robaczewska M;Lescop C;Froidevaux S;Schmitz N;Morrison K;Kohl C;Rey M;Studer R;Vezzali E;Hess P;Clozel M;Steiner B;Bolli MH;Nayler O Pharmacol Res Perspect. 2017 Dec;5(6). doi: 10.1002/prp2.370.
Sphingosine-1-phosphate receptor 1 (S1P;1; ) modulators sequester circulating lymphocytes within lymph nodes, thereby preventing potentially pathogenic autoimmune cells from exiting into the blood stream and reaching inflamed tissues. S1P;1; receptor modulation may thus offer potential to treat various autoimmune diseases. The first nonselective S1P;1-5; receptor modulator FTY720/fingolimod/Gilenya;®; has successfully demonstrated clinical efficacy in relapsing forms of multiple sclerosis. However, cardiovascular, hepatic, and respiratory side-effects were reported and there is a need for novel S1P;1; receptor modulators with better safety profiles. Here, we describe the discovery of cenerimod, a novel, potent and selective S1P;1; receptor modulator with unique S1P;1; receptor signaling properties and absence of broncho- and vasoconstrictor effects ex vivo and in vivo. Cenerimod dose-dependently lowered circulating lymphocyte counts in rats and mice after oral administration and effectively attenuated disease parameters in a mouse experimental autoimmune encephalitis (EAE) model. Cenerimod has potential as novel therapy with improved safety profile for autoimmune diseases with high unmet medical need.
2.Pharmacokinetics, Pharmacodynamics, Tolerability, and Food Effect of Cenerimod, a Selective S1P₁ Receptor Modulator in Healthy Subjects.
Juif PE;Baldoni D;Reyes M;Wilbraham D;Febbraro S;Vaclavkova A;Hoch M;Dingemanse J Int J Mol Sci. 2017 Dec 6;18(12). pii: E2636. doi: 10.3390/ijms18122636.
The pharmacokinetics, pharmacodynamics, tolerability, and food effect of cenerimod, a potent sphingosine-1-phosphate subtype 1 receptor modulator, were investigated in three sub-studies. Two double-blind, placebo-controlled, randomised studies in healthy male subjects were performed. Cenerimod was administered either as single dose (1, 3, 10 or 25 mg; Study 1) or once daily for 35 days (0.5, 1, 2 or 4 mg; Study 2). A two-period cross-over, open-label study was performed to assess the food effect (1 mg, Study 3). The pharmacokinetic profile of cenerimod was characterised by a ;t;max; of 5.0-6.2 h. Terminal half-life after single and multiple doses ranged from 170 to 199 h and 283 to 539 h, respectively. Food had no relevant effect on the pharmacokinetics of cenerimod. A dose-dependent decrease in lymphocyte count was observed after initiation of cenerimod and reached a plateau (maximum change from baseline: -64%) after 20-23 days of treatment. Lymphocyte counts returned to baseline values at end-of-study examination. One serious adverse event of circulatory collapse (25 mg dose group, maximum tolerated dose: 10 mg) and adverse events of mild-to-moderate intensity were reported. Treatment initiation was associated with transient decreases in heart rate and blood pressure at doses >1 and ≥10 mg, respectively.
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