Ozanimod hydrochloride
(Synonyms: RPC-1063 hydrochloride) 目录号 : GC69645Ozanimod (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。
Cas No.:1618636-37-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ozanimod (RPC-1063) drochloride, a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod drochloride has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod drochloride can be used for the research of relapsing multiple sclerosis (MS) [1].
Ozanimod (RPC-1063) drochloride 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 drochloride 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 drochloride 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 drochloride 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].
Ozanimod (RPC-1063) drochloride (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[1].
Ozanimod drochloride (oral gavage; 5 mg/kg; once-daily) prevented axonal degradation and myelin loss during toxin challenge but did not facilitate enhanced remyelination after intoxication[1].
Ozanimod drochloride (oral, 1 or 5 mg/kg, for 7 days) has good pharmacokinetics in mice[1].
| 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: | Animal ModelC57BL/6J mice[1] | ||||||||||||||||||||||||||||||
| Dosage: | 1 or 5 mg/kg | ||||||||||||||||||||||||||||||
| Administration: | oral, 1 or 5 mg/kg, for 7 days | ||||||||||||||||||||||||||||||
| Result: |
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[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
| Cas No. | 1618636-37-5 | SDF | Download SDF |
| 别名 | RPC-1063 hydrochloride | ||
| 分子式 | C23H25ClN4O3 | 分子量 | 440.92 |
| 溶解度 | DMSO : 200 mg/mL (453.60 mM; Need ultrasonic) | 储存条件 | 4°C, away from moisture |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.268 mL | 11.3399 mL | 22.6799 mL |
| 5 mM | 0.4536 mL | 2.268 mL | 4.536 mL |
| 10 mM | 0.2268 mL | 1.134 mL | 2.268 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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