Uses
ChemicalBook > CAS DataBase List > Ozanimod

Ozanimod

Uses
Product Name
Ozanimod
CAS No.
1306760-87-1
Chemical Name
Ozanimod
Synonyms
(S)-5-(3-(1-((2-hydroxyethyl)amino)-2,3-dihydro-1H-inden-4-yl)-1,2,4-oxadiazol-5-yl)-2-isopropoxybenzonitrile;RPC1063;Ozanimod (RPC1063);Ozamud;CS-2386;Ozanimod;Ozanimod-d6;RPC1063 Ozanimod;oxanimod(RPC1063);Ozanimod USP/EP/BP
CBNumber
CB42716147
Molecular Formula
C23H24N4O3
Formula Weight
404.46
MOL File
1306760-87-1.mol
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Ozanimod Property

Melting point:
134-137°C
Boiling point:
648.3±65.0 °C(Predicted)
Density 
1.30±0.1 g/cm3(Predicted)
storage temp. 
-20°C Freezer
solubility 
DMSO (Slightly), Methanol (Slightly)
form 
Solid
pka
14.73±0.10(Predicted)
color 
White to Off-White
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H372Causes damage to organs through prolonged or repeated exposure

Precautionary statements

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P314Get medical advice/attention if you feel unwell.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
19922
Product name
Ozanimod
Purity
≥98%
Packaging
1mg
Price
$44
Updated
2024/03/01
Cayman Chemical
Product number
19922
Product name
Ozanimod
Purity
≥98%
Packaging
5mg
Price
$193
Updated
2024/03/01
Cayman Chemical
Product number
19922
Product name
Ozanimod
Purity
≥98%
Packaging
10mg
Price
$341
Updated
2024/03/01
Cayman Chemical
Product number
19922
Product name
Ozanimod
Purity
≥98%
Packaging
25mg
Price
$796
Updated
2024/03/01
TRC
Product number
O880000
Product name
Ozanimod
Packaging
1mg
Price
$40
Updated
2021/12/16
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Ozanimod Chemical Properties,Usage,Production

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 (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.

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.

storage

Store at -20°C

References

scott f l, clemons b, brooks j, et al. ozanimod (rpc1063) is a potent sphingosine‐1‐phosphate receptor‐1 (s1p1) and receptor‐5 (s1p5) agonist with autoimmune disease‐modifying activity[j]. british journal of pharmacology, 2016.sandborn wj, feagan bg1, et al. ozanimod induction and maintenance treatment for ulcerative colitis. n engl j med. 2016, 374(18):1754-1762.

Ozanimod Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Ozanimod manufacturers

Shaanxi Dideu Medichem Co. Ltd
Product
Ozanimod 1306760-87-1
Price
US $1.00-1.00/KG
Min. Order
1g
Purity
99%
Supply Ability
50tons
Release date
2020-05-06
Wuhan Nutra Biotechnology Co.,Ltd
Product
Ozanimod 1306760-87-1
Price
US $600.00-0.00/g
Min. Order
1g
Purity
98%+
Supply Ability
100kgs
Release date
2021-05-23
Dideu Industries Group Limited
Product
Ozanimod 1306760-87-1
Price
US $1.10/g
Min. Order
1g
Purity
0.999
Supply Ability
100 Tons min
Release date
2021-08-03

1306760-87-1, OzanimodRelated Search:


  • Benzonitrile, 5-[3-[(1S)-2,3-dihydro-1-[(2-hydroxyethyl)aMino]-1H-inden-4-yl]-1,2,4-oxadiazol-5-yl]-2-(1-Methylethoxy)- (free base)
  • Ozanimod (RPC1063)
  • Ozanimod
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  • Benzonitrile, 5-[3-[(1S)-2,3-dihydro-1-[(2-hydroxyethyl)amino]-1H-inden-4-yl]-1,2,4-oxadiazol-5-yl]-2-(1-methylethoxy)-
  • 5-[3-[(1S)-2,3-Dihydro-1-[(2-hydroxyethyl)amino]-1H-inden-4-yl]-1,2,4-oxadiazol-5-yl]-2-(1-methylethoxy)benzonitrile
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