Ozanimod (RPC1063)|1306760-87-1|(奥扎莫德; RPC-1063)-陌孚医药/Medlife

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Ozanimod (RPC1063) (Synonyms: 奥扎莫德; RPC-1063)

目录号: PC11044 纯度: ≥98%

CAS No. :1306760-87-1

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中文名称

Ozanimod (RPC1063)

中文别名

奥扎莫德

英文名称

Ozanimod (RPC1063)

英文别名

ozanimod;RPC1063;RPC-1063;5-[3-[(1S)-2,3-Dihydro-1-[(2-hydroxyethyl)amino]-1H-inden-4-yl]-1,2,4-oxadiazol-5-yl]-2-(1-methylethoxy)benzonitrile

Cas No.

1306760-87-1

分子式

C₂₃H₂₄N₄O₃

分子量

404.46

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Ozanimod (RPC-1063), a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod has modulate effect for hS1P₁ and hS1P₅ receptor with EC₅₀s of 1.03 nM and 8.6 nM, respectively. Ozanimod can be used for the research of relapsing multiple sclerosis (MS).

性状

Solid

IC50 & Target[1][2]

S1PR1

1.03 nM (EC₅₀)

S1PR5

8.6 nM (EC₅₀)

体外研究(In Vitro)

Ozanimod (RPC-1063) has potency and intrinsic activity of S1P receptor modulators for S1P5 across species with [S]-GTPgS binding, and the EC₅₀ values of 1.03 nM, 1.29 nM, 0.90 nM, 1.02 nM and 0.61 nM for Human S1P₁, Cynomolgus monkey S1P₁, Mouse S1P₁, Rat S1P1 and Canine S1P₁, respectively; and the EC₅₀ values of 8.6 nM, 15.9 nM, 957.5 nM, 2032.7 nM and 1662.0 nM for Human S1P₅, Cynomolgus monkey S1P₅, Mouse S1P₅, Rat S1P₅ and Canine S1P₅, respectively.
Ozanimod restores the potency with EC₅₀ from 958 nM for mS1P₅ to 6.7 nM for mS1P₅_A120T to closely mirror the EC₅₀ for hS1P₅ of 8.6 nM by mutating the alanine in the mouse sequence.
Ozanimod has binding affinity with K_i values of 2.0 nM, 59.9 nM and 5.6 nM for hS1P₅, mS1P₅ and mS1P₅ _A120T, respectively.
Ozanimod has saturation binding of [H]-ozanimod to hS1P₅, and mS1P₅_A120T with K_D values of 6.56 nM, 7.35 nM, respectively and also has saturation binding for [H]-A971432 to S1P₅D value of 8.75 nM.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Ozanimod (RPC-1063) (oral gavage; 0.05, 0.2, or 1 mg/kg; once daily; for 14 consecutive days) exposures sufficient to engage S1P₁, but not S1P₅, resulted in reduced circulating lymphocytes, disease scores, and body weight loss; reduced inflammation, demyelination, and apoptotic cell counts in the spinal cord; and reduced circulating levels of the neuronal degeneration marker, neurofilament light.
Ozanimod (oral gavage; 5 mg/kg; once-daily) prevented axonal degradation and myelin loss during toxin challenge but did not facilitate enhanced remyelination after intoxication.
Ozanimod (oral, 1 or 5 mg/kg, for 7 days) has good pharmacokinetics in mice.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Experimental Autoimmune Encephalomyelitis Model
Dosage:	0.05, 0.2, or 1 mg/kg
Administration:	oral gavage; 0.05, 0.2, or 1 mg/kg; once daily; for 14 consecutive days
Result:	Attenuated body weight loss, terminal disease scores were significantly attenuated with the 0.2 and 1 mg/kg doses and ALCs were significantly reduced in all dose groups. Reduced spinal cord inflammation and demyelination, as well as attenuated the number of spinal cord apoptotic cells, and significantly reduced the levels of circulating neurofilament light at the top dose of 1 mg/kg.

Animal Model:	Cuprizone/Rapamycin Demyelination Model
Dosage:	5 mg/kg
Administration:	oral gavage; 5 mg/kg; once-daily
Result:	Protected neuronal axons, preventing breakage and ovoid formation in the corpus callosum of CPZ/Rapa treated mice. Significantly attenuated the extent to which the corpus callosum demonstrated reduced myelin content as visualized by MRI. Did not result in enhanced myelin content.

Animal Model:

C57BL/6J mice

Dosage:

1 or 5 mg/kg

Administration:

oral, 1 or 5 mg/kg, for 7 days

Result:

Dose	Terminal body weight % versus day 1	Spinal cord inflammation Foci per 20 cells	Spinal cord demyelination Score 0–5	Spinal cord apoptotic cells Count per section	Plasma NfL pg/ml
Vehicle (5% DMSO, 5%Tween 20, 90% water)	86.4 ± 3.2	8.50 ± 1.21	2.00 ± 0.15	2.25 ± 0.53	4.37 ± 0.89
Ozanimod (0.05 mg/kg)	85.8 ± 2.7	5.00 ± 1.03*	0.91 ± 0.21***	1.08 ± 0.23*	3.53 ± 0.46
Ozanimod (0.2 mg/kg)	95.7 ± 3.1*	3.54 ± 0.49***	0.73 ± 0.14 ***	0.91 ± 0.28*	2.62 ± 0.46
Ozanimod (1 mg/kg)	102.8 ± 1.8*	2.67 ± 0.56***	0.33 ± 0.14 ***	0.60 ± 0.19**	1.91 ± 0.34**

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Julie V Selkirk, et al. Deconstructing the Pharmacological Contribution of Sphingosine-1 Phosphate Receptors to Mouse Models of Multiple Sclerosis Using the Species Selectivity of Ozanimod, a Dual Modulator of Human Sphingosine 1-Phosphate Receptor Subtyp [Information]

溶解度数据

体外研究:

DMSO : ≥ 29 mg/mL (71.70 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4724 mL	12.3622 mL	24.7243 mL
5 mM	0.4945 mL	2.4724 mL	4.9449 mL
10 mM	0.2472 mL	1.2362 mL	2.4724 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.18 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.18 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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