产品
编 号：F114483
分子式：C23H24N4O3
分子量：404.46
分子式：C23H24N4O3
分子量：404.46
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规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1306760-87-1
产品详情
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).
体内研究：
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.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.Ozanimod (oral, 1 or 5 mg/kg, for 7 days) has good pharmacokinetics in mice.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:DoseTerminal body weight % versus day 1Spinal cord inflammation Foci per 20 cellsSpinal cord demyelination Score 0–5Spinal cord apoptotic cells Count per sectionPlasma NfL pg/ml
Vehicle (5% DMSO, 5%Tween 20, 90% water)86.4 ± 3.28.50 ± 1.212.00 ± 0.152.25 ± 0.534.37 ± 0.89
Ozanimod (0.05 mg/kg)85.8 ± 2.75.00 ± 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**
体外研究：
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.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 Ki values of 2.0 nM, 59.9 nM and 5.6 nM forhS1P5, mS1P5 and mS1P5 _A120T, respectively.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 S1P5Ozanimod 相关抗体:
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).
体内研究：
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.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.Ozanimod (oral, 1 or 5 mg/kg, for 7 days) has good pharmacokinetics in mice.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:DoseTerminal body weight % versus day 1Spinal cord inflammation Foci per 20 cellsSpinal cord demyelination Score 0–5Spinal cord apoptotic cells Count per sectionPlasma NfL pg/ml
Vehicle (5% DMSO, 5%Tween 20, 90% water)86.4 ± 3.28.50 ± 1.212.00 ± 0.152.25 ± 0.534.37 ± 0.89
Ozanimod (0.05 mg/kg)85.8 ± 2.75.00 ± 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**
体外研究：
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.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 Ki values of 2.0 nM, 59.9 nM and 5.6 nM forhS1P5, mS1P5 and mS1P5 _A120T, respectively.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 S1P5Ozanimod 相关抗体:
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