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CAS No.: 1306760-87-1

Ozanimod/奥扎莫德 Catalog No. CSN16206

Synonyms: RPC-1063;奥扎莫德

Ozanimod is an oral, once daily, selective sphingosine 1-phosphate 1 and 5 receptor modulator in development for autoimmune indications including relapsing multiple sclerosis (RMS) and ulcerative colitis (UC).

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Ozanimod is a specific modulator of S1P1 and S1P5 receptors. It can inhibit the generation of cAMP induced by forskolin, and GTP-binding with EC50 values of 0.16 nM and 0.41 nM, respectively. The induction of S1P1 receptor sustained internalization and degradation could be observed post one-hour treatment with 1 μM Ozanimod in transfected HEK293T cells expressing S1P1 receptors. Oral dose of 1 mg/kg Ozanimod in mice, or 0.5 mg/kg in rat, induced dose-dependent, selective lymphopenia and rapid lymphocyte repopulation kinetics, with reduction of CD4⁺CCR7⁺, and CD8⁺CCR7⁺ T cells. Administration of 0.6 mg/kg Ozanimod for 14 days reduced ongoing disease symptoms in EAE model induced by immunization with MOG_35–55 peptide. Also, a significant reduction of disease activity in TNBS-induced colitis could be achieved in rats dosed 0.3 or 1 mg/kg Ozanimod. Histological disease severity and inflammatory cytokine expression were both reduced in a naïve T-cell adoptive transfer model of colitis after therapeutic administration^[1].

动物研究

剂量

Mice^[1] (p.o.): min = 0.2 mg/kg, max = 3 mg/kg

给药途径

p.o.

动物药代数据

Animal	Mice^[1]	Rats^[1]
Dose	1 mg/kg	0.5 mg/kg
Administration	p.o.	p.o.
C_max	0.16 ± 0.03 μM	0.06 ± 0.003 μM
T_1/2	4.7 h	5.1 h
Brain: blood	10	16
AUC Norm_0-inf	1.50 ± 0.15 μM·h
CL	28 ml/min/kg	30 ml/min/kg
AUC_0-inf		0.70 ± 0.07 μM·h
T_max	3 h	3 h
V_d	10 L/kg	13 L/kg

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01647516	Ulcerative Colitis	Phase 2	Active, not recruiting	July 1, 2019	-
NCT01628393	Relapsing Multiple Sclerosis	Phase 2 Phase 3	Completed	-	-
NCT02294058	Multiple Sclerosis	Phase 3	Completed	-	-

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参考文献

[1] Scott FL, Clemons B, et al. Ozanimod (RPC1063) is a potent sphingosine-1-phosphate receptor-1 (S1P1 ) and receptor-5 (S1P5 ) agonist with autoimmune disease-modifying activity. Br J Pharmacol. 2016 Jun;173(11):1778-92.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4724 mL
- 12.3621 mL
- 24.7242 mL
- 5 mM
- 0.4945 mL
- 2.4724 mL
- 4.9448 mL
- 10 mM
- 0.2472 mL
- 1.2362 mL
- 2.4724 mL

技术信息

CAS号

1306760-87-1

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H24N4O3

运输

蓝冰

分子量

404.46

别名

RPC-1063;奥扎莫德

溶解度

DMSO	250.0 mg/mL (618.1 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	5 mg/mL	clear
PO	0.5% CMC-Na	38 mg/mL	suspension

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01647516	Ulcerative Colitis	Phase 2	Active, not recruiting	July 1, 2019	-
NCT01628393	Relapsing Multiple Sclerosis	Phase 2 Phase 3	Completed	-	-
NCT02294058	Multiple Sclerosis	Phase 3	Completed	-	-
NCT02435992	Ulcerative Colitis	Phase 3	Recruiting	July 29, 2020	-
NCT02047734	Relapsing Multiple Sclerosis	Phase 2 Phase 3	Completed	-	-
NCT02994381	Healthy Volunteers	Phase 1	Completed	-	United Kingdom ... more >> Quotient Clinical Nottingham, United Kingdom, NG11 6JS Collapse <<
NCT02531126	Ulcerative Colitis	Phase 3	Recruiting	March 31, 2022	-
NCT03694119	Healthy Volunteer	Phase 1	Recruiting	January 8, 2019	United States, Texas ... more >> PPD Phase 1 Clinic Recruiting Austin, Texas, United States, 78744 Collapse <<
NCT03665610	-	-	Recruiting	May 21, 2019	United States, Texas ... more >> PPD Phase 1 Clinic Not yet recruiting Austin, Texas, United States, 78744 PPD Phase 1 Clinic Recruiting Austin, Texas, United States, 78744 ICON Early Phase Services, LLC Not yet recruiting San Antonio, Texas, United States, 78209 ICON Early Phase Services, LLC Recruiting San Antonio, Texas, United States, 78209 Collapse <<
NCT03624959	Healthy Volunteer	Phase 1	Recruiting	April 15, 2019	United States, Texas ... more >> PPD Phase 1 Clinic Recruiting Austin, Texas, United States, 78744 Collapse <<
NCT02531113	Crohn's Disease	Phase 2	Active, not recruiting	October 12, 2019	-
NCT02797015	Multiple Sclerosis	Phase 1	Completed	-	United States, California ... more >> Breastlink Medical Group, Inc. Long Beach, California, United States, 90806 Multiple Sclerosis Center at UCSF San Francisco, California, United States, 94158 United States, North Carolina Raleigh Neurology Associates PA Raleigh, North Carolina, United States, 27607 United States, Ohio Neurology and Neuroscience Associates Inc. Akron, Ohio, United States, 44320 United States, Tennessee Hope Neurology MS Center Knoxville, Tennessee, United States, 37922 United States, Texas Central Texas Neurology Consultants PA Round Rock, Texas, United States, 78681 Collapse <<
NCT03440372	Crohn Disease	Phase 3	Recruiting	August 31, 2020	-
NCT03440385	Crohn Disease	Phase 3	Recruiting	August 30, 2020	-
NCT03644576	Healthy Volunteers	Phase 1	Recruiting	February 12, 2019	United States, Texas ... more >> ICON Early Phase Services, LLC Recruiting San Antonio, Texas, United States, 78209 Collapse <<
NCT03464097	Crohn Disease	Phase 3	Recruiting	May 31, 2021	-
NCT02576717	Multiple Sclerosis	Phase 3	Enrolling by invitation	June 30, 2020	-
NCT03467958	Crohn Disease	Phase 3	Recruiting	December 30, 2022	-

Ozanimod/奥扎莫德 Catalog No. CSN16206

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