SB 205384
目录号 : GC16356
positive GABAA receptor modulator
Cas No.:160296-13-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
SB-205384 is a selective and positive GABAA receptor modulator with EC50 values of 280, 695 and 730 nM on α6, α3 and α5-subunit-containing receptors, respectively [1].
g-Aminobutyric acid (GABA) acting on the GABAA receptor can inhibit synaptic transmission in the mammalian central nervous system [1]. Ligands that modulate the function of g-aminobutyric acid A (GABAA) receptor gated chloride channels have hypnotic, anaesthetic, anxiolytic, anticonvulsant and sedative actions [2].
SB-205384 can slow the decay rate on GABAA currents in oocytes expressing human GABAA subunits, which is also seen on native GABA-activated currents in rat neurons [3]. The isoforms containing the a3, a5, and a6 subunits show significantly greater enhancement of the current by SB-205384 and the receptors with the a6-subunit had the greatest sensitivity to SB-205384 [1]. In rat cerebellum granule cells, SB-205384 dramatically pro-longed the half-life for decay of the GABA response in a concentration-dependent manner. The half-life of decay was increased about 10 fold compared with control responses at the highest concentration of SB-205384 used. Also, SB-205384 did not increase the maximum current evoked by 100 mM GABA but the half-life decay was dramatically increased, as saw at the lower dose of 1 mM GABA [2].
References:
[1]. Heidelberg LS, Warren JW, Fisher JL. SB-205384 is a positive allosteric modulator of recombinant GABAA receptors containing rat α3, α5, or α6 subunit subtypes coexpressed with β3 and γ2 Subunits. J Pharmacol Exp Ther, 2013, 347(1): 235-241.
[2]. Meadows HJ, Harries MH, Thompson M, et al. Effect of SB-205384 on the decay of GABA-activated chloride currents in granule cells cultured from rat cerebellum. Br J Pharmacol, 1997, 121(7): 1334-1338.
[3]. Meadows HJ, Kumar CS, Pritchett DB, et al. SB-205384: a GABAA receptor modulator with novel mechanism of action that shows subunit selectivity. Br J Pharmacol, 1998, 123(6): 1253-1259.
| Cas No. | 160296-13-9 | SDF | |
| 化学名 | (S)-but-2-yn-1-yl 4-amino-7-hydroxy-2-methyl-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-b]pyridine-3-carboxylate | ||
| Canonical SMILES | O[C@H](C1)CCC2=C1SC3=NC(C)=C(C(OCC#CC)=O)C(N)=C23 | ||
| 分子式 | C17H18N2O3S | 分子量 | 330.4 |
| 溶解度 | <33.04mg/ml in 1eq. HCl; <16.52mg/ml in DMSO | 储存条件 | Desiccate at RT |
| 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 | 3.0266 mL | 15.1332 mL | 30.2663 mL |
| 5 mM | 0.6053 mL | 3.0266 mL | 6.0533 mL |
| 10 mM | 0.3027 mL | 1.5133 mL | 3.0266 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。