GSK205 (hydrobromide) |
Katalog-Nr.GC91768
One-Click Copy Product Info
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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).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: N/A
Sample solution is provided at 25 µL, 10mM.
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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 | |
| Formula | C24H24N4S•XHBr | M.Wt | 400.5 |
| Löslichkeit | DMSO: Slightly soluble: 0.1-1 mg/ml | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4969 mL | 12.4844 mL | 24.9688 mL |
| 5 mM | 499.4 μL | 2.4969 mL | 4.9938 mL |
| 10 mM | 249.7 μL | 1.2484 mL | 2.4969 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >95.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)