| CAS NO: | 288150-92-5 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 100mg | 电议 |
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 356.38 |
| Cas No. | 288150-92-5 |
| Formula | C19H18F2N4O |
| Solubility | insoluble in H2O; ≥1.76 mg/mL in EtOH with gentle warming and ultrasonic; ≥35.4 mg/mL in DMSO with gentle warming |
| Chemical Name | 1-(6,8-difluoro-2-methylquinolin-4-yl)-3-[4-(dimethylamino)phenyl]urea |
| Canonical SMILES | CC1=NC2=C(C=C(C=C2C(=C1)NC(=O)NC3=CC=C(C=C3)N(C)C)F)F |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
SB408124是一种新型有效的非肽类食欲素-1(OX(1))受体拮抗剂,在细胞膜和全细胞中的Ki值分别为27 nM和57 nM.SB408124对OX1受体的选择性比人OX2受体高50倍[1].
在从大鼠大脑皮层中获得的原代星形细胞培养物中,使用食欲素A之前用SB408124预处理可显著降低食欲素A对毛喉素和基底诱导的cAMP生成的刺激活性[2].
在大鼠中,注射组胺(HA)或高盐水后,SB408124(30 μg/10 μl)与食欲素A共同给药可防止食欲素A诱导的对加压素(VP)浓度提高的减少[3].
参考文献：
[1] Langmead CJ1, Jerman JC, Brough SJ, Scott C, Porter RA, Herdon HJ. Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. Br J Pharmacol. 2004 Jan;141(2):340-6.
[2] Woldan-Tambor A1, Biegańska K, Wiktorowska-Owczarek A, Zawilska JB. Activation of orexin/hypocretin type 1 receptors stimulates cAMP synthesis in primary cultures of rat astrocytes. Pharmacol Rep. 2011;63(3):717-23.
[3] Kis GK1, Molnár AH, Daruka L, Gardi J, Rákosi K, László F, László FA, Varga C. The osmotically and histamine-induced enhancement of the plasma vasopressin level is diminished by intracerebroventricularly administered orexin in rats. Pflugers Arch. 2012 Apr;463(4):531-6.
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