GSK205 (hydrobromide)
目录号 : GC91768GSK205 is an inhibitor of transient receptor potential vanilloid 4 (TRPV4) and transient receptor potential ankyrin 1 (TRPA1; IC50s = 4.19 and 5.56 µM, respectively, for the rat channels).
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
GSK205 is an inhibitor of transient receptor potential vanilloid 4 (TRPV4) and transient receptor potential ankyrin 1 (TRPA1; IC50s = 4.19 and 5.56 µM, respectively, for the rat channels).[1] It inhibits calcium influx induced by the TRPV4 agonist GSK101 (GSK1016790A; ) in whole-cell patch-clamp assays using Neuro2a neuroblastoma cells expressing TRPV4 when used at a concentration of 5 µM. GSK205 (10 µM) prevents compression-induced increases in NF-κB transcriptional activity and secreted levels of IL-6 and VEGFA, as well as inhibits compression-induced fractures, abnormal cell morphology, and fissures in the intervertebral space, in primary mouse lumbar spines when used at a concentration of 10 µM.[2]
References:
[1].Kanju, P., Chen, Y., Lee, W., et al.Small molecule dual-inhibitors of TRPV4 and TRPA1 for attenuation of inflammation and painSci. Rep.626894(2016).
[2].Easson, G.W.D., Savadipour, A., Anandarajah, A., et al.Modulation of TRPV4 protects against degeneration induced by sustained loading and promotes matrix synthesis in the intervertebral discFASEB J.37(2)e22714(2023).
| Cas No. | N/A | SDF | Download SDF |
| 分子式 | C24H24N4S•XHBr | 分子量 | 400.5 |
| 溶解度 | DMSO: Slightly soluble: 0.1-1 mg/ml | 储存条件 | -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 | 2.4969 mL | 12.4844 mL | 24.9688 mL |
| 5 mM | 0.4994 mL | 2.4969 mL | 4.9938 mL |
| 10 mM | 0.2497 mL | 1.2484 mL | 2.4969 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。