NIBR-0213 is a potent and selective S1P1 antagonist with efficacy in experimental autoimmune encephalomyelitis. NIBR-0213 displays potent and comparable potency on human and rat S1P1 (IC 50 of 2.0 nM and 2.3 nM, respectively) in GTPγS assays.
体外研究(In Vitro)
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 Ca 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 GTPγS 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 GTPγS assay. NIBR-0213 is a competitive S1P1 antagonist with a calculated Kd of 0.37±0.031 nM. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Jean Quancard, et al. A potent and selective S1P(1) antagonist with efficacy in experimental autoimmune encephalomyelitis. Chem Biol. 2012 Sep 21;19(9):1142-51.