产品
编 号：F084588
分子式：C27H29ClN2O3
分子量：464.98
分子式：C27H29ClN2O3
分子量：464.98
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 1233332-14-3
产品详情
生物活性：
NIBR-0213 is a potent, orally active and selective S1P1?antagonist with efficacy in experimental autoimmune encephalomyelitis. NIBR-0213 displays potent and comparable potency on human and rat S1P1?(IC50?of 2.0?nM and 2.3?nM, respectively) in GTPγ35S assays.
体内研究：
NIBR-0213 (given orally at 30?mg/kg to rats) reduces the peripheral blood lymphocyte?(PBL) counts by 75%-85% within 14?hr and maintained this effect up to 24?hr posttreatment.NIBR-0213 (30?mg/kg and 60?mg/kg) is efficacious when given therapeutically in a mouse experimental autoimmune encephalomyelitis (EAE) model.The PK properties of NIBR-0213 shows a moderate clearance (26?mL/min/kg) and a high oral bioavailability (69%), leading to significant exposure after oral dosing.Animal Model:Lewis or Wistar rats (220-250 g, males)
Dosage:30?mg/kg
Administration:Orally
Result:Reduced the PBL counts by 75%-85% within 14?hr and maintained this effect up to 24?hr posttreatment.
Animal Model:C57BL/6 mice bearing EAE model
Dosage:30?mg/kg and 60?mg/kg
Administration:30?mg/kg twice per day (BID) for 3?days and then increased to 60?mg/kg BID until the remainder of the experiment. In total, the treatment lasted 26?days
Result:Resulted in a gradual reduction in disease-scores, with a divergence from vehicle controls that became significant after 5?days.
体外研究：
NIBR-0213 displays an inhibitory activity on hS1P1?with an IC50?of 2.5?nM whereas it is inactive (IC50?>10?μM) on S1P2, S1P3, and S1P4?in Ca2+?mobilization assays.NIBR-0213 displays potent and comparable potency on human and rat S1P1?(IC50?of 2.0?nM and 2.3?nM, respectively) in GTPγ35S assays, whereas on mouse S1P1?with an IC50?of 8.5?nM.NIBR-0213 shows an ～3,000-fold selectivity against human S1P5?in the GTPγ35S assay. NIBR-0213 is a competitive S1P1?antagonist with a calculated Kd?of 0.37±0.031?nM.
NIBR-0213 is a potent, orally active and selective S1P1?antagonist with efficacy in experimental autoimmune encephalomyelitis. NIBR-0213 displays potent and comparable potency on human and rat S1P1?(IC50?of 2.0?nM and 2.3?nM, respectively) in GTPγ35S assays.
体内研究：
NIBR-0213 (given orally at 30?mg/kg to rats) reduces the peripheral blood lymphocyte?(PBL) counts by 75%-85% within 14?hr and maintained this effect up to 24?hr posttreatment.NIBR-0213 (30?mg/kg and 60?mg/kg) is efficacious when given therapeutically in a mouse experimental autoimmune encephalomyelitis (EAE) model.The PK properties of NIBR-0213 shows a moderate clearance (26?mL/min/kg) and a high oral bioavailability (69%), leading to significant exposure after oral dosing.Animal Model:Lewis or Wistar rats (220-250 g, males)
Dosage:30?mg/kg
Administration:Orally
Result:Reduced the PBL counts by 75%-85% within 14?hr and maintained this effect up to 24?hr posttreatment.
Animal Model:C57BL/6 mice bearing EAE model
Dosage:30?mg/kg and 60?mg/kg
Administration:30?mg/kg twice per day (BID) for 3?days and then increased to 60?mg/kg BID until the remainder of the experiment. In total, the treatment lasted 26?days
Result:Resulted in a gradual reduction in disease-scores, with a divergence from vehicle controls that became significant after 5?days.
体外研究：
NIBR-0213 displays an inhibitory activity on hS1P1?with an IC50?of 2.5?nM whereas it is inactive (IC50?>10?μM) on S1P2, S1P3, and S1P4?in Ca2+?mobilization assays.NIBR-0213 displays potent and comparable potency on human and rat S1P1?(IC50?of 2.0?nM and 2.3?nM, respectively) in GTPγ35S assays, whereas on mouse S1P1?with an IC50?of 8.5?nM.NIBR-0213 shows an ～3,000-fold selectivity against human S1P5?in the GTPγ35S assay. NIBR-0213 is a competitive S1P1?antagonist with a calculated Kd?of 0.37±0.031?nM.
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