GSK1016790A

Catalog No.S8107 Batch:S810701

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Technical Data

Formula

C28H32Cl2N4O6S2
Molecular Weight 655.61 CAS No. 942206-85-1
Solubility (25°C)* In vitro DMSO 100 mg/mL (152.52 mM)
Ethanol 100 mg/mL (152.52 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description GSK1016790A (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34nM in choroid plexus epithelial cells.
Targets
hTRPV4 [1]
(In HEK cells)		 mTRPV4 [1]
(In HEK cells)
2.1 nM 18 nM
In vitro GSK1016790A elicits Ca2+ influx in mouse and human TRPV4 expressing HEK cells (EC50 values of 18 and 2.1 nM, respectively), and evokes a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM[1]. It stimulates TRPV4 in multiple cell types including endothelial cells, urinary smooth muscle cells, urothelial cells and HEK-293 cells over-expressing TRPV4. GSK1016790A specifically activates TRPV4 channels, leading to a rapid partial desensitization and downregulation of the channel expression on the plasma membrane[2].
In vivo GSK1016790A can produce marked decreases in systemic vascular resistance and pulmonary vascular resistance under high pulmonary vascular tone conditions[3]. The activation of TRPV4 by GSK1016780A leads to vasodilation, vascular leakage, and tissue hemorrhage[4].

Protocol (from reference)

Cell Assay:[4]
  • Cell lines

    Choroid plexus epithelial cells

  • Concentrations

    10 nM

  • Incubation Time

    20 min

  • Method

    CPECs are treated for 20 minutes with vehicle(DMSO), 10 nM GSK, or 10 nM GSK following the pretreatment with 1 mM HC. Then the cells are fixed and stained with Coomassie Brilliant Blue.
Animal Study:[3]
  • Animal Models

    Adult male Sprague-Dawley rats

  • Dosages

    2, 4, 6, 8, 10, and 12 μg/kg

  • Administration

    Intravenous injection

Selleck's GSK1016790A has been cited by 9 publications

Fatty acid metabolism promotes TRPV4 activity in lung microvascular endothelial cells in pulmonary arterial hypertension [ Am J Physiol Lung Cell Mol Physiol, 2024, 326(3):L252-L265] PubMed: 38226418
Heat promotes melanogenesis by increasing the paracrine effects in keratinocytes via the TRPV3/Ca2+/Hh signaling pathway [ iScience, 2023, 26(5):106749] PubMed: 37216091
Dental Pulp Stem Cell-Derived Exosomes Alleviate Mice Knee Osteoarthritis by Inhibiting TRPV4-Mediated Osteoclast Activation [ Int J Mol Sci, 2023, 24(5)4926] PubMed: 36902356
Piezo1-mediated mechanosensation in bone marrow macrophages promotes vascular niche regeneration after irradiation injury [ Theranostics, 2022, 12(4): 1621-1638] PubMed: N/A
Piezo1-mediated mechanosensation in bone marrow macrophages promotes vascular niche regeneration after irradiation injury [ Theranostics, 2022, 12(4):1621-1638] PubMed: 35198061
Resident cardiac macrophages mediate adaptive myocardial remodeling [ Immunity, 2021, S1074-7613(21)00289-2] PubMed: 34320366
Calcium and TRPV4 promote metastasis by regulating cytoskeleton through the RhoA/ROCK1 pathway in endometrial cancer [ Cell Death Dis, 2020, 11(11):1009] PubMed: 33230171
Mechanical force modulates periodontal ligament stem cell characteristics during bone remodelling via TRPV4 [ Cell Prolif, 2020, 53(10):e12912] PubMed: 32964544
Effect of cGMP-activated aquaporin 1 on TRPV4 in rats with allodynia induced by chronic compression of the dorsal root ganglion. [ Neurosci Lett, 2019, 10.1016/j.neulet.2019.134630] PubMed: 31790718

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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