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GSK 1016790A

Catalog #: 6433
3 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
6433/50
6433/10
GSK 1016790A | CAS No. 942206-85-1 | TRPV Agonists
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Description: Potent TRPV4 agonist; active in vivo

Chemical Name: N-[(1S)-1-[[4-[(2S)-2-[[(2,4-Dichlorophenyl)sulfonyl]amino]-3-hydroxy-1-oxopropyl]-1-piperazinyl]carbonyl]-3-methylbutyl]benzo[b]thiophene-2-carboxamide

Purity: ≥97%

Product Details
Citations (3)
Reviews
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Biological Activity

GSK 1016790A is a potent TRPV4 agonist; elicits Ca2+ influx in human and mouse TRPV4-expressing HEK cells (EC50 values of 2.1 and 18 nM, respectively). Enhances insulin mRNA expression. Increases ERK1/2 phosphorylation and NO production. Exhibits no activity at TRPM8 and TRPA1 (20 μM) channels. Induces bladder overactivity in TRPV4+/+ mice.

Technical Data

M.Wt:
655.61
Formula:
C28H32Cl2N4O6S2
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥97%
Storage:
Store at -20°C
CAS No:
942206-85-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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Citations for GSK 1016790A

The citations listed below are publications that use Tocris products. Selected citations for GSK 1016790A include:

3 Citations: Showing 1 - 3

  1. TRPV4-Rho GTPase complex structures reveal mechanisms of gating and disease.
    Authors: Kwon Et al.
    Nat Commun  2023;14:3732
  2. Endothelial pannexin 1-TRPV4 channel signaling lowers pulmonary arterial pressure in mice.
    Authors: Brant E Et al.
    Elife  2021;10
  3. The Effects of the Anti-aging Protein Klotho on Mucociliary Clearance.
    Authors: Stefanie Et al.
    Front Med (Lausanne)  2020;6:339

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