GSK1016790A

製品コードS8107 バッチS810704

印刷

化学情報

Chemical Structure Synonyms GSK101 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C28H32Cl2N4O6S2
分子量 655.61 CAS No. 942206-85-1
Solubility (25°C)* 体外 DMSO 100 mg/mL (152.52 mM)
Ethanol 50 mg/mL (76.26 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 GSK1016790A (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34nM in choroid plexus epithelial cells.
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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Choroid plexus epithelial cells
濃度 10 nM
反応時間 20 min
実験の流れ 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.
動物実験 動物モデル Adult male Sprague-Dawley rats
投薬量 2, 4, 6, 8, 10, and 12 μg/kg
投与方法 Intravenous injection

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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