NIBR0213 - CAS:1233332-14-3

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NIBR0213

目录号 : KCM10757 CAS No. : 1233332-14-3 纯度 : ≥98%

Data Sheet SDS 产品使用指南

NIBR0213 is an orally bioavailable, potent, and selective antagonist of sphingosine-1-phosphate receptor-1 (S1P) with IC values of 2.5 and 2.0 nM for the hS1P in a Ca mobilization assay and GTPγS assay, respectively. It is inactive at S1P, S1P, and S1P receptors (ICs = >20, >10, and >10 µM, respectively in a Ca mobilization assay). S1P plays a key role in the immune system, regulating lymphocyte egress from lymphoid tissues into the circulation. In rats, NIBR0213 (30 mg/kg) reduces peripheral blood lymphocytes by 75-85% for up to 24 hours. In a mouse model of experimental autoimmune encephalitis (EAE), it significantly reduces disease severity up to 26 days, when administered at 30 mg/kg twice per day for three days, then 60 mg/kg twice per day. However, in a rat model of adjuvant-induced arthritis, chronic administration of 30 mg/kg induces pulmonary damage and chronic lung inflammation.

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
25mg	询价	In-stock
10 mM * 1 mL in DMSO		In-stock

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生物活性

NIBR0213 is a potent, orally active and selective S1P1 antagonist with efficacy in experimental autoimmune encephalomyelitis. NIBR0213 displays potent and comparable potency on human and rat S1P1 (IC50 of 2.0 nM and 2.3 nM, respectively) in GTPγ35S assays[1].

体外研究

NIBR0213 exhibits inhibitory activity against hS1P1 with an IC50 of 2.5 nM, while it shows no activity against S1P2, S1P3, and S1P4 in Ca2+mobilization assays (IC50>10 μM) [1].

NIBR0213 showed strong and comparable efficacy against human and large S1P1 (IC50 of 2.0 nM and 2.3 nM, respectively) in the GTP γ 35S assay, while the IC50 against small S1P1 was 8.5 nM [1].

NIBR0213 exhibits approximately 3000 fold selectivity in GTP γ 35S assay for human S1P5 [1].

NIBR0213 is a competitive S1P1 antagonist with a calculated Kd of 0.37 ± 0.031 nM [1].

体内研究

NIBR0213 (oral administration of 30 mg/kg) can reduce peripheral lymphocyte (PBL) count by 75% -85% within 14 hours, and this effect can last for 24 hours after treatment [1].
NIBR0213 (30 mg/kg and 60 mg/kg) is effective in treating small experimental autoimmune encephalomyelitis (EAE) models.
The PK characteristics of NIBR0213 show that it has a moderate clearance rate (26 mL/min/kg) and high oral bioavailability (69%), and can produce significant exposure after oral administration [1].

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[1]
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.

分子式

C₂₇H₂₉ClN₂O₃

分子量

465

CAS号

1233332-14-3

中文名称

(S)-2-({3'-[(R)-1-(4-Chloro-3-methyl-phenyl)-ethylamino]-3,5-dimethyl-biphenyl-4-carbonyl}-amino)-propionic acid

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO: 100 mg/mL (215.06 mM; Need ultrasonic)

Ethanol : ≥ 25 mg/mL (53.77 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1506 mL	10.7532 mL	21.5063 mL
5 mM	0.4301 mL	2.1506 mL	4.3013 mL
10 mM	0.2151 mL	1.0753 mL	2.1506 mL

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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

纯度： ≥98%