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
InChIKey
XRVDGNKRPOAQTN-FQEVSTJZSA-N
SMILES
C(#N)C1=CC(C2ON=C(C3=CC=CC4=C3CC[C@@H]4NCCO)N=2)=CC=C1OC(C)C
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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.

Pharmacokinetics

Ozanimod is metabolised into two major active metabolites [ie, CC112273 and CC1084037] and several other minor active metabolites, all with similar selectivity for S1P1 and S1P5. Approximately 94% of the total circulating active drug is made up of ozanimod [6%], CC112273 [73%], and CC1084037 [15%]. The mean half-life of ozanimod is approximately 21 hours, and the mean half-life of CC112273 and CC1084037 is approximately 11 days. Given the relatively long half-life of the major active metabolites, some effects of ozanimod may continue after treatment discontinuation and a washout period of up to 3 months after discontinuing ozanimod is recommended in certain situations [eg, planning a pregnancy, planning to initiate an immunosuppressant or receipt of a live attenuated vaccine], and patients should be monitored for infections for up to 3 months after ozanimod is stopped[2].

Side effects

The most common ozanimod (Zeposia) side effects include colds, headaches, and chest and urinary tract infections. Compared to other disease-modifying therapies, the risk of side effects, especially serious ones, is in the middle and similar to those you get with fingolimod. That said, in trials, ozanimod had fewer side effects than fingolimod. When you take your first dose of the drug, it can cause your heartbeat to slow down (it soon goes back to normal). Because of this, your first dose will be smaller andl gradually increase over the first week. Ozanimod causes a short-lived rise in your liver enzymes. They generally go back to normal levels without you needing to stop taking it.

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

[1] 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.
[2] Bruce E Sands. “Clinician’s Guide to Using Ozanimod for the Treatment of Ulcerative Colitis.” Journal of Crohns & Colitis (2023): 2012–2025.

Ozanimod Preparation Products And Raw materials

Raw materials

Preparation Products

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Ozanimod Suppliers

Nanjing YakeLun Pharmaceutical Co., Ltd.
Tel
025-66096098 3165145969
Fax
QQ3165145969
Email
sales@accoronpharm.com
Country
China
ProdList
3924
Advantage
55
Wuhan HSN Pharmaresearch CO., LTD.
Tel
027-63499089 18086100502
Fax
027-86589137
Email
linwell@126.com
Country
China
ProdList
211
Advantage
50
Shanghai Chaolan Chemical Technology Center
Tel
021-QQ:65489617 15618227136
Fax
21-5161 9052
Email
Sales@ATKchemical.com
Country
China
ProdList
7296
Advantage
58
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
Nanjing Sunlida Biological Technology Co., Ltd.
Tel
025-57798810
Fax
025-57019371
Email
sales@sunlidabio.com
Country
China
ProdList
3239
Advantage
55
TargetMol Chemicals Inc.
Tel
021-021-33632979 15002134094
Fax
021-33632979
Email
marketing@targetmol.com
Country
China
ProdList
7783
Advantage
58
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185 18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3466
Advantage
58
Taizhou Tongxin Bio-Tech Co., Ltd
Tel
0523-18601685-898 18652728585
Email
sales@allyrise.com
Country
China
ProdList
2782
Advantage
60
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View Lastest Price from Ozanimod manufacturers

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
Longyan Tianhua Biological Technology Co., Ltd
Product
Ozanimod 1306760-87-1
Price
US $20.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
1000KG
Release date
2020-11-11
Career Henan Chemical Co
Product
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) 1306760-87-1
Price
US $2.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
100kg
Release date
2018-12-24

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
  • RPC1063
  • 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
  • (S)-5-(3-(1-((2-hydroxyethyl)amino)-2,3-dihydro-1H-inden-4-yl)-1,2,4-oxadiazol-5-yl)-2-isopropoxybenzonitrile
  • oxanimod(RPC1063)
  • RPC1063 Ozanimod
  • CS-2386
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  • Ozanimod-d6
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