NIBR0213|cas:1233332-14-3|西域试剂

NIBR0213

产品编号：Bellancom-18166| CAS NO：1233332-14-3| 分子式：C₂₇H₂₉ClN₂O₃| 分子量：464.98

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货号	价格	库存与货期
Bellancom-18166	￥3300.00	杭州北京（现货）
Bellancom-18166	￥5300.00	杭州北京（现货）
Bellancom-18166	￥11200.00	杭州北京（现货）

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NIBR0213

产品介绍

NIBR-0213 是一种有效的选择性 S1P1 拮抗剂，对实验性自身免疫性脑脊髓炎有效。在 GTPγ³⁵S 试验中，NIBR-0213 有效作用于人和大鼠 S1P1，IC₅₀ 分别为 2.0 nM 和 2.3 nM。

生物活性

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 (IC₅₀ of 2.0 nM and 2.3 nM, respectively) in GTPγ³⁵S assays.

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 K_d of 0.37±0.031 nM.

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

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.

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

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.

体内研究

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

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.