2. GPCR/G Protein
  3. LPL Receptor
  4. Ozanimod

Ozanimod  (Synonyms: 奥扎莫德; RPC-1063)

目录号: HY-12288 纯度: 99.88%
COA 产品使用指南

摩尔计算器

Ozanimod (RPC-1063) 是一种鞘氨醇 1-磷酸 (S1P) 受体调节剂，可高亲和力地选择性结合 S1P 受体亚型 1 (S1P1) 和 S1P5 (S1P5)。Ozanimod 对 hS1P1和 hS1P5 受体具有调节作用，EC50 值分别为 1.03 nM 和 8.6 nM。Ozanimod 可用于复发性多发性硬化 (MS) 的研究。

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Ozanimod Chemical Structure

Ozanimod Chemical Structure

CAS No. : 1306760-87-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1320
In-stock
1 mg ￥545
In-stock
5 mg ￥1196
In-stock
10 mg ￥1800
In-stock
25 mg ￥3700
In-stock
50 mg ￥5688
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Ozanimod:

Ozanimod 相关抗体

Top Publications Citing Use of Products

查看 LPL Receptor 亚型特异性产品:

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LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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)[1].

IC50 & Target

S1PR1

1.03 nM (EC50)

S1PR5

8.6 nM (EC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO-K1 EC50
0.16 nM
Compound: RPC1063
Agonist activity at S1P1 (unknown origin) expressed in CHO-K1 cells using CC4-AM as substrate assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 4 hrs followed by substrate addition and measured after 2 hrs by FRET assay
Agonist activity at S1P1 (unknown origin) expressed in CHO-K1 cells using CC4-AM as substrate assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 4 hrs followed by substrate addition and measured after 2 hrs by FRET assay
[PMID: 31266686]
体外研究
(In Vitro)

Ozanimod (RPC-1063) has potency and intrinsic activity of S1P receptor modulators for S1P5 across species with [35S]-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[1].
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[1].
Ozanimod has binding affinity with Ki values of 2.0 nM, 59.9 nM and 5.6 nM for hS1P5, mS1P5 and mS1P5 _A120T, respectively[1].
Ozanimod has saturation binding of [3H]-ozanimod to hS1P5, and mS1P5_A120T with KD values of 6.56 nM, 7.35 nM, respectively and also has saturation binding for [3H]-A971432 to S1P5D value of 8.75 nM[1].

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

Ozanimod 相关抗体:
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, results in reduced circulating lymphocytes, disease scores, and body weight loss; reduces inflammation, demyelination, and apoptotic cell counts in the spinal cord; and reduces circulating levels of the neuronal degeneration marker, neurofilament light[1].
Ozanimod (oral gavage; 5 mg/kg; once-daily) prevents axonal degradation and myelin loss during toxin challenge but does not facilitate enhanced remyelination after intoxication[1].
Ozanimod (oral, 1 or 5 mg/kg, for 7 days) has good pharmacokinetics in mice[1].

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

Animal Model: Experimental Autoimmune Encephalomyelitis Model[1]
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[1]
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[1]
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**
Clinical Trial
分子量

404.46

Formula

C23H24N4O3
CAS 号
性状

固体

颜色

White to off-white

中文名称

奥扎莫德
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 50 mg/mL (123.62 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 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

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.18 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.18 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

    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。

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.88%

COA (197 KB) HNMR (268 KB) LCMS (93 KB)

产品使用指南 (1538 KB)
参考文献

Ozanimod 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4724 mL 12.3622 mL 24.7243 mL 61.8108 mL
5 mM 0.4945 mL 2.4724 mL 4.9449 mL 12.3622 mL
10 mM 0.2472 mL 1.2362 mL 2.4724 mL 6.1811 mL
15 mM 0.1648 mL 0.8241 mL 1.6483 mL 4.1207 mL
20 mM 0.1236 mL 0.6181 mL 1.2362 mL 3.0905 mL
25 mM 0.0989 mL 0.4945 mL 0.9890 mL 2.4724 mL
30 mM 0.0824 mL 0.4121 mL 0.8241 mL 2.0604 mL
40 mM 0.0618 mL 0.3091 mL 0.6181 mL 1.5453 mL
50 mM 0.0494 mL 0.2472 mL 0.4945 mL 1.2362 mL
60 mM 0.0412 mL 0.2060 mL 0.4121 mL 1.0302 mL
80 mM 0.0309 mL 0.1545 mL 0.3091 mL 0.7726 mL
100 mM 0.0247 mL 0.1236 mL 0.2472 mL 0.6181 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ozanimod1306760-87-1RPC-1063奥扎莫德RPC1063RPC 1063LPL ReceptorLysophospholipid Receptorsphingosine 1-phosphate (S1P)S1P receptor subtypes 1 (S1P1)S1P receptor subtypes 5 (S1P5)multiple sclerosis (MS)neurosurgeryInhibitorinhibitorinhibit

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