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Chemical Structure| 1263068-83-2 Chemical Structure| 1263068-83-2

Structure of GSK205
CAS No.: 1263068-83-2

Chemical Structure| 1263068-83-2

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GSK205 is a potent and selective TRPV4 antagonist with an IC50 value of 4.19 μM, inhibiting TRPV4-mediated Ca2+ influx.

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Product Details of GSK205

CAS No. :1263068-83-2
Formula : C24H25BrN4S
M.W : 481.45
SMILES Code : CN(CCC1=CC=C(NC2=NC=C(C3=CC=CN=C3)S2)C=C1)CC4=CC=CC=C4.[H]Br
MDL No. :MFCD28160554
InChI Key :LQGOJHGNGSOUKL-UHFFFAOYSA-N
Pubchem ID :72736243

Safety of GSK205

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Astrocytes 5 nM Evaluate the inhibitory effect of GSK205 derivatives in primary cells expressing TRPV4. Compound 16-8 was significantly more effective than the parent molecule GSK205. Sci Rep. 2016 Jun 1;6:26894
Articular chondrocytes 5 nM Evaluate the inhibitory effect of GSK205 derivatives in primary cells expressing TRPV4. Compound 16-8 was significantly more effective than the parent molecule GSK205. Sci Rep. 2016 Jun 1;6:26894
human periodontal ligament cells (hPDLCs) 30 µM 8 hours To investigate the inhibitory effect of GSK205 on the TrPV4 channel and its impact on mechanotransduction in hPDLCs. Results showed that GSK205 treatment reduced intracellular calcium concentration and suppressed the increased expression of COX2, RANKL, and OPG induced by mechanical loading. Mol Med Rep. 2020 May;21(5):2113-2122
N2a cells 5 μM 5 minutes Evaluate the inhibitory effect of GSK205 derivatives on TRPV4-mediated Ca++ influx. Compounds 16-8 and 16-19 showed the strongest inhibitory effects, almost completely eliminating Ca++ influx. Sci Rep. 2016 Jun 1;6:26894

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Functional spine unit (FSU) culture model Added to the culture medium 10 μM 24 hours of sustained loading TRPV4 inhibition mitigated the changes in inflammatory cytokines, protected against IVD degeneration, but could not prevent ECM disorganization due to mechanical damage in the annulus fibrosus. FASEB J. 2023 Feb;37(2):e22714
Mice Trigeminal irritant pain model Intraperitoneal injection 10 mg/kg Single dose, observed for 45 minutes Evaluate the effect of GSK205 derivatives in the trigeminal irritant pain model. Compounds 16-8 and 16-19 significantly reduced pain behavior in the delayed phase, while GSK205 was ineffective. Sci Rep. 2016 Jun 1;6:26894

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.08mL

0.42mL

0.21mL

10.39mL

2.08mL

1.04mL

20.77mL

4.15mL

2.08mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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