A TRPV4 and TRPA1 inhibitor
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GSK205 (hydrobromide)

Item No. 40923

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[2-[methyl(phenylmethyl)amino]ethyl]phenyl]-5-(3-pyridinyl)-2-thiazolamine, hydrobromide
Molecular Formula
C24H24N4S • XHBr
Formula Weight
400.5
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
CN(CC1=CC=CC=C1)CCC(C=C2)=CC=C2NC3=NC=C(C4=CN=CC=C4)S3.Br
InChi Code
InChI=1S/C24H24N4S.BrH/c1-28(18-20-6-3-2-4-7-20)15-13-19-9-11-22(12-10-19)27-24-26-17-23(29-24)21-8-5-14-25-16-21;/h2-12,14,16-17H,13,15,18H2,1H3,(H,26,27);1H
InChi Key
LQGOJHGNGSOUKL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $32

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    10 mg

    $61

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    50 mg

    $272

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    100 mg

    $511

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    Product Description

    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; Item No. 17289) 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

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kanju, P., Chen, Y., Lee, W., et al. Small molecule dual-inhibitors of TRPV4 and TRPA1 for attenuation of inflammation and pain. Sci. Rep. 6, 26894 (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 disc. The FASEB Journal 37(2), e22714 (2023).