GSK-1016790A, TRPV4 channel agonist (ab146191)

Overview

  • Product name

    GSK-1016790A, TRPV4 channel agonist
  • Description

    Novel, potent TRPV4 channel agonist
  • Alternative names

    • GSK1016790A
  • Biological description

    Novel, potent TRPV4 channel agonist. Induced Ca2+ influx in mouse and human TRPV4 expressing HEK cells (EC50 values of 18 and 2.1 nM respectively), and evoked a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM. 300-fold more potent than 4α-PDD.

  • CAS Number

    942206-85-1
  • Chemical structure

    Chemical Structure

Properties

  • Molecular weight

    655.61
  • Molecular formula

    C28H32Cl2N4O6S2
  • Storage instructions

    Store at Room Temperature. The product can be stored for up to 12 months.
  • Handling

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES

    Clc1ccc(c(Cl)c1)S(=O)(=O)N[C@@H](CO)C(=O)N2CCN(CC2)C(=O)[C@H](CC(C)C)NC(=O)c3cc4ccccc4s3
  • Source

    Synthetic

References

This product has been referenced in:

  • Thoppil RJ  et al. TRPV4 channel activation selectively inhibits tumor endothelial cell proliferation. Sci Rep 5:14257 (2015). Read more (PubMed: 26388427) »
  • Saxena A  et al. Angiotensin II induces membrane trafficking of natively expressed transient receptor potential vanilloid type 4 channels in hypothalamic 4B cells. Am J Physiol Regul Integr Comp Physiol 307:R945-55 (2014). Read more (PubMed: 25080500) »
  • Adapala RK  et al. PKCa mediates acetylcholine-induced activation of TRPV4-dependent calcium influx in endothelial cells. Am J Physiol Heart Circ Physiol 301:H757-65 (2011). Read more (PubMed: 21705673) »
  • Thorneloe KS  et al. N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a novel and potent transient receptor potential vanilloid 4 channel agonist induces urinary bladder contraction and hyperactivity: Part I. J Pharmacol Exp Ther 326:432-42 (2008). Read more (PubMed: 18499743) »
  • Willette RN  et al. Systemic activation of the transient receptor potential vanilloid subtype 4 channel causes endothelial failure and circulatory collapse: Part 2. J Pharmacol Exp Ther 326:443-52 (2008). Read more (PubMed: 18499744) »

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Please note: All products are "FOR RESEARCH USE ONLY. NOT FOR USE IN DIAGNOSTIC PROCEDURES, NOT FOR USE IN HUMANS"
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