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GSK205

CAS No. 1263068-83-2

GSK205( —— )

Catalog No. M32950 CAS No. 1263068-83-2

GSK205 is a selective TRPV4 antagonist that blocks Ca(2+) signaling and may be used to reduce inflammation and pain.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    GSK205
  • Note
    Research use only, not for human use.
  • Brief Description
    GSK205 is a selective TRPV4 antagonist that blocks Ca(2+) signaling and may be used to reduce inflammation and pain.
  • Description
    GSK205 is a potent, selective TRPV4 antagonist with an IC50 of 4.19? μM for inhibiting TRPV4-mediated Ca2+ influx.
  • In Vitro
    RT-PCR Cell Line:T3-F442A adipocytes Concentration:5 μM Incubation Time:4 days Result:Resulted in increased expression of thermogenic genes and is also accompanied by a decrease in the proinflammatory gene program.
  • In Vivo
    Animal Model:Male C57BL/6J mice with high-fat dietDosage:10 mg/kg Administration:Intraperitoneal injection; twice daily; for 7 days Result:Caused a reduced expression of the proinflammatory chemokines, macrophage marker and Tnfa in the EPI fat. Significantly improved glucose tolerance in diet-induced obese (DIO) mice.
  • Synonyms
    ——
  • Pathway
    GPCR/G Protein
  • Target
    Calcium Channel
  • Recptor
    Calcium Channel | TRP/TRPV Channel
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1263068-83-2
  • Formula Weight
    481.45
  • Molecular Formula
    C24H25BrN4S
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 250 mg/mL (519.26 mM; Ultrasonic )
  • SMILES
    Br.CN(CCc1ccc(Nc2ncc(s2)-c2cccnc2)cc1)Cc1ccccc1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Ye L, et al. TRPV4 is a regulator of adipose oxidative metabolism, inflammation, and energy homeostasis. Cell. 2012 Sep 28;151(1):96-110.?
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