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![Озанимод структурированное изображение](/CAS/20180808/GIF/1306760-87-1.gif)
Озанимод
- английское имяOzanimod
- CAS №1306760-87-1
- CBNumberCB42716147
- ФормулаC23H24N4O3
- мольный вес404.46
- EINECS814-246-9
- номер MDLMFCD28386168
- файл Mol1306760-87-1.mol
химическое свойство
Температура плавления | 134-137°C |
Температура кипения | 648.3±65.0 °C(Predicted) |
плотность | 1.30±0.1 g/cm3(Predicted) |
температура хранения | -20°C Freezer |
растворимость | DMSO (Slightly), Methanol (Slightly) |
форма | Solid |
пка | 14.73±0.10(Predicted) |
цвет | White to Off-White |
ИнЧИКей | XRVDGNKRPOAQTN-FQEVSTJZSA-N |
SMILES | C(#N)C1=CC(C2ON=C(C3=CC=CC4=C3CC[C@@H]4NCCO)N=2)=CC=C1OC(C)C |
FDA UNII | Z80293URPV |
Код УВД | L04AA38 |
рисовальное письмо(GHS)
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рисовальное письмо(GHS)
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сигнальный язык
опасность
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вредная бумага
H372:Поражает органы в результате многократного или продолжительного воздействия.
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оператор предупредительных мер
P260:Не вдыхать газ/ пары/ пыль/ аэрозоли/ дым/ туман.
P264:После работы тщательно вымыть кожу.
P270:При использовании продукции не курить, не пить, не принимать пищу.
P314:В случае плохого самочувствия обратиться к врачу.
P501:Удалить содержимое/ контейнер на утвержденных станциях утилизации отходов.
Озанимод химические свойства, назначение, производство
Описание
Ozanimod is a sphingosine-1-phosphate receptor 1 (S1P1) and S1P5 agonist. It induces GTPγS binding in cell membranes expressing human S1P1 or S1P5 (EC50s = 0.41 and 11 nM, respectively) but not cell membranes expressing S1P2 or S1P3 receptors (EC50s = >10,000 nM for both). Ozanimod (0.2 mg/kg) reduces the number of peripheral lymphocytes in rats. It reduces disease severity and the number of circulating lymphocytes in a mouse model of experimental autoimmune encephalomyelitis (EAE). Ozanimod (0.3 and 1 mg/kg) reduces disease severity and body weight loss in a mouse model of TNBS-induced colitis. Formulations containing ozanimod have been used in the treatment of relapsing multiple sclerosis and ulcerative colitis.Использование
Ozanimod is an agonist that binds to S1P1 and S1P5 receptors. Experiments on rodents revealed that Ozanimod is effective against autoimmune diseases.Ферментативный ингибитор
This orally available S1PR1 modulator (FW = 404.46 g/mol; CAS 1306760- 87-1; Solubility: 81 mg/mL DMSO; < 1 mg/mL H2O), also named RPC1063 and 5-[3-[(1S)-2,3-dihydro-1-[(2-hydroxyethyl)amino]-1H-inden- 4-yl]-1,2,4-oxadiazol-5-yl]-2-(1-methylethoxy)benzonitrile, selectively targets sphingosine 1-Phosphate (S1P) receptors, which mediate multiple processes, including lymphocyte trafficking, cardiac function, and endothelial barrier integrity. Ozanimod is specific for S1P1R (IC50 = 0.4 nM) and S1P5R, inducing S1P1R internalization and reversibly reducing the number of circulating B and CCR7+ T lymphocytes in vivo. It shows high oral bioavailability and volume of distribution, and a circulatory half-life that supports once daily dosing. Oral ozanimod reduced inflammation and disease parameters in three autoimmune disease models, commending its use in the treatment of relapsing multiple sclerosis (RMS) and inflammatory bowel disease (IBD). Indeed, the safety and efficacy of this modulator ozanimod in relapsing multiple sclerosis is indicated on the basis of a randomized, placebo-controlled, Phase 2 trial. Other SIPR1-directed immunomodulators include laquinimod, ponesimod, and siponimod.Озанимод поставщик
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