Ozanimod hydrochloride RPC-1063 hydrochloride|cas:1618636-37-5|西域试剂

Ozanimod hydrochloride RPC-1063 hydrochloride,99.19%

产品编号：Bellancom-12288A| CAS NO：1618636-37-5| 分子式：C₂₃H₂₅ClN₄O₃| 分子量：440.92

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货号	价格	库存与货期
Bellancom-12288A	￥1200.00	杭州北京（现货）
Bellancom-12288A	￥1800.00	杭州北京（现货）
Bellancom-12288A	￥3700.00	杭州北京（现货）
Bellancom-12288A	￥5800.00	杭州北京（现货）
Bellancom-12288A	￥8500.00	杭州北京（现货）

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Ozanimod hydrochloride RPC-1063 hydrochloride

产品介绍

Ozanimod (RPC-1063) hydrochloride 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 hydrochloride 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 hydrochloride 可用于复发性多发性硬化 (MS) 的研究。

生物活性

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

体外研究

Ozanimod (RPC-1063) hydrochloride 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.
Ozanimod hydrochloride 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 hydrochloride 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 hydrochloride has saturation binding of [³H]-ozanimod to hS1P₅, and mS1P₅_A120T with K_D values of 6.56 nM, 7.35 nM, respectively and also has saturation binding for [³H]-A971432 to S1P₅D value of 8.75 nM.

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

体内研究

Ozanimod (RPC-1063) hydrochloride (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 hydrochloride (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 hydrochloride (oral, 1 or 5 mg/kg, for 7 days) has good pharmacokinetics in mice.

西域 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:

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**

体内研究

西域 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:

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**

性状

Solid

溶解性数据

In Vitro:

DMSO : 200 mg/mL (453.60 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2680 mL	11.3399 mL	22.6798 mL
5 mM	0.4536 mL	2.2680 mL	4.5360 mL
10 mM	0.2268 mL	1.1340 mL	2.2680 mL

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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

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

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 5 mg/mL (11.34 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (11.34 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 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 ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 5 mg/mL (11.34 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (11.34 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 5 mg/mL (11.34 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (11.34 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 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。