|1-(6,8-二氟-2-甲基喹啉-4-基)-3-(4-(二甲基氨基)苯基)脲|CsnPharm

CAS No.: 288150-92-5

SB-408124 Catalog No. CSN16521

Synonyms: SB-408124

SB-408124 is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively, and exhibits 50-fold selectivity over OX2 receptor.

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生物活性

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技术信息

生物活性

描述Orexins (A and B) are hypothalamic peptides that interact with OX1 and OX2 receptors and are involved in the sleep/wake cycle. OX1 receptors are highly expressed in colon cancer tumours and colonic cancer cell lines where orexins induce apoptosis and inhibit tumour growth in preclinical animal models^[3]. Injection of exogenous orexin-A specifically improved the inflammatory symptoms in the two colitis murine models. Conversely, injection of inactive orexin-A analog, OxB7-28 or OX1R specific antagonist SB-408124 did not have anti-inflammatory effect. Moreover, treatment with orexin-A in DSS-colitis induced OX1R-/- knockout mice did not have any protective effect. The orexin-A anti-inflammatory effect was due to the decreased expression of pro-inflammatory cytokines in immune cells and specifically in T-cells isolated from colonic mucosa^[4].SB-408124 is a non-peptide OX1 receptor antagonist with Kis of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 exhibits 50-fold selectivity over OX2 receptor^[5]. SB-408124 (30 μg/10 μl; i.c.v.; male Wistar rats) decreases Orexin-A induced water intake in Wistar rats^[6].In isolated rat cardiomyocytes, only orexin-B (OR-B) caused an increase in contractile shortening, independent of diastolic or systolic calcium levels. A specific orexin receptor-2 (OX2R) agonist ([Ala11, d-Leu15]-Orexin B) exerted similar effects as OR-B, whereas a specific orexin receptor-1 (OX1R) antagonist (SB-408124) did not alter the responsiveness of OR-B^[7].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8061 mL
- 14.0304 mL
- 28.0608 mL
- 5 mM
- 0.5612 mL
- 2.8061 mL
- 5.6122 mL
- 10 mM
- 0.2806 mL
- 1.4030 mL
- 2.8061 mL

技术信息

CAS号

288150-92-5

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H18F2N4O

运输

蓝冰

分子量

356.37

别名

SB-408124

溶解度

DMSO	36.0 mg/mL (101.0 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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