| Identification | Back Directory | [Name]
Abediterol | [CAS]
1262414-04-9 | [Synonyms]
CS-2487
Abediterol
ACT-334441
ACT-334441; ACT334441; 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
1,2-Propanediol, 3-[4-[5-(2-cyclopentyl-6-methoxy-4-pyridinyl)-1,2,4-oxadiazol-3-yl]-2-ethyl-6-methylphenoxy]-, (2S)- | [Molecular Formula]
C25H31N3O5 | [MOL File]
1262414-04-9.mol | [Molecular Weight]
453.53 |
| Chemical Properties | Back Directory | [Boiling point ]
670.7±65.0 °C(Predicted) | [density ]
1?+-.0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:100.0(Max Conc. mg/mL);220.49(Max Conc. mM) | [form ]
A crystalline solid | [pka]
13.44±0.20(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Uses]
Cenerimod (ACT-334441) is a potent, selective and orally active S1P1 receptor modulator, with an EC50 of 1 nM. Cenerimod shows more than 36 fold selctivity for hS1P1 over hS1P2, hS1P3, hS1P4, and hS1P5 receptor subtypes (EC50s=>10000, 228, 2134, and 36 nM, respectively). Cenerimod can attenuate murine experimental autoimmune encephalomyelitis (EAE) and murine sclerodermatous[1][2]. | [in vivo]
Cenerimod (0.1-10 mg/kg; a single p.o.) reversibly reduces the number of circulating lymphocytes in a dose-dependent manner 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.) attenuates skin and lung fibrosis in Scl-cGVHD mice[2]. | Animal Model: | Male Wistar rats weighing 294-510 g[1] | | Dosage: | 0.1, 0.3, 1, 3 and 10 mg/kg | | Administration: | A single p.o. | | Result: | Effectively and reversibly reduced the blood lymphocyte counts, with a plateau reached after a single oral dose of 1 mg/kg. |
| [IC 50]
S1PR1: 1 nM (EC50); S1PR5: 36 nM (EC50); S1PR5: 228 nM (EC50); S1PR4: 2134 nM (EC50) | [storage]
Store at -20°C | [References]
[1] Piali L, et, al. Cenerimod, a novel selective S1P 1 receptor modulator with unique signaling properties. Pharmacol Res Perspect. 2017 Dec;5(6):e00370. DOI:10.1002/prp2.370
[2] Kano M, et, al. Attenuation of murine sclerodermatous models by the selective S1P 1 receptor modulator cenerimod. Sci Rep. 2019 Jan 24;9(1):658. DOI:10.1038/s41598-018-37074-9 |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
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