SB408124
目录号 : GC15317
A potent orexin 1 receptor antagonist
Cas No.:288150-92-5
Sample solution is provided at 25 µL, 10mM.
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SB408124 is a potent and novel nonpeptide antagonist of orexin-1 (OX(1)) receptor with Ki values of 27 nM and 57 nM in membrane formats and in whole cell, respectively. SB408124 was 50-fold selective over the human OX2 receptor [1].
Pre-treated with SB408124 before orexin A in primary astrocyte cultures from the rat cerebral cortex remarkably decreased the orexin A stimulatory activity on forskolin and basal-induced cAMP production [2].
In rats, SB408124 at dose of 30 μg/10 μl together with orexin-A after histamine (HA) or hypertonic saline injection could prevent the orexin-A-induced reduction in vasopressin (VP) concentration increase [3].
References:
[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.
| Cas No. | 288150-92-5 | SDF | |
| 化学名 | 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 | ||
| 分子式 | C19H18F2N4O | 分子量 | 356.38 |
| 溶解度 | ≥ 35.4 mg/mL in DMSO with gentle warming, ≥ 1.76 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.806 mL | 14.03 mL | 28.0599 mL |
| 5 mM | 0.5612 mL | 2.806 mL | 5.612 mL |
| 10 mM | 0.2806 mL | 1.403 mL | 2.806 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet