CAS1306760-87-1 High Quality Ozanimod an Agonist That Binds to S1p1 and S1p5 Receptors

Model NO.
1306760-87-1
Standard
USP/Ep/Bp/Cp/IP/Jp/Who/in-House
Capacity
1000kg/Mon
Transport Package
25kg/Drum/1000g/Bag/10g/Bag
Specification
100% raw material
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Widely
Origin
China
Production Capacity
1000kg/Mon
Reference Price
$ 27.00 - 45.00
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Product Description

CAS1306760-87-1 High Quality Ozanimod an Agonist That Binds to S1p1 and S1p5 Receptors  
Uses Ozanimod is an agonist that binds to S1P1 and S1P5 receptors. Experiments on rodents revealed that Ozanimod is effective against autoimmune diseases.
Description Ozanimod is a sphingosine-1-phosphate receptor 1 (S1P 1 ) and S1P 5  agonist. It induces GTPγS binding in cell membranes expressing human S1P 1  or S1P 5  (EC 50 s = 0.41 and 11 nM, respectively) but not cell membranes expressing S1P 2  or S1P 3  receptors (EC 50 s = >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.
Uses Ozanimod is an agonist that binds to S1P1 and S1P5 receptors. Experiments on rodents revealed that Ozanimod is effective against autoimmune diseases.
in vitro ozanimod(rpc1063) was a specific agonist for s1p1 and s1p5 receptors. the ec50values were 160 ± 60 pm and 410 ± 160 pm for s1p1 receptors in the inhibition of camp generation and[35s]-gtpγs binding. the 83% emax value of ozanimod against s1p5 receptor was 11 ± 4.3 nm. rpc1063 dose-dependently decreased s1p1 receptor re-expression on the cell surface and resulted in near complete and sustained loss of cell surface receptor expression at concentrations above 10 nm in s1p1 receptor-hek293t cells after 1 h incubation [1].
in vivo the t1/2 of ozanimod was 4.7 h and 5.1 h in mice and rats after p.o. administration, respectively. about 81-82% decrease in circulating t lymphocyte was observed after dosing administration for 6 h, with a maximal blood concentration of 45 nm and 159 nm in rats and mice respectively. oral gavage of ozanimod dose-dependently reduced the disease score of mice in both doses (0.2 or 0.6 mg/kg/day) [1].
Enzyme inhibitor 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.
 
CAS1306760-87-1 High Quality Ozanimod an Agonist That Binds to S1p1 and S1p5 Receptors
CAS1306760-87-1 High Quality Ozanimod an Agonist That Binds to S1p1 and S1p5 Receptors
Hubei weideli Chemical Reagent Co., Ltd., located in Wuhan East Lake New Technology Development Zone, is a manufacturing supplier focusing on reagent products for scientific research, and its business scope includes the manufacturing of special chemical products; Disinfectant production; Sales of special chemical products; Disinfectant sales; Research and development of biological feed; Research and development of bio based materials technology; Research and development of biochemical products technology; Technical services, technical development, technical consultation, technical exchange, technology transfer and technology promotion; Sales of instruments and meters; Sales of daily glass products; Sales of technical glass products; Sales of electronic special materials; Technology import and export; Import and export of goods; Veterinary drug management; Production of disinfection products for the prevention and treatment of infectious diseases.

The company has gradually established extensive cooperation with scientific research institutions in Colleges and universities and powerful enterprises to lay a solid foundation for technological production; At the same time, we will recruit talents all over the country and keep them fresh and energetic; With more than ten years of experience and accumulation in the industry, the company further improves its market competitiveness and strengthens its support to customers.

With the help of modern ERP system, the company provides customers with accurate quotation and inventory information in time. It has a warehouse base and Laboratory of more than 1000 square meters in Jiangxia District, Wuhan. The system inventory products can be ordered on the same day, and the order number is given on the same day of delivery. The information can be queried online, followed up in real time, and customer service provides after-sales support services.

Hubei weideli Chemical Reagent Co., Ltd. is committed to scientific research.


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