GSK1016790A

製品コードS8107 バッチS810704

印刷

化学情報

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

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (7.63mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.800mg/ml (1.22mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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）は、脈絡叢上皮細胞においてEC50が34nMの、TRPV4（一過性受容体電位バニロイド4）の新規強力活性化因子です。
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. It stimulates TRPV4 in multiple cell types including endothelial cells, urinary smooth muscle cells, urothelial cells and HEK-293 cells over-expressing TRPV4. This compound specifically activates TRPV4 channels, leading to a rapid partial desensitization and downregulation of the channel expression on the plasma membrane.
in vivo	GSK1016790A can produce marked decreases in systemic vascular resistance and pulmonary vascular resistance under high pulmonary vascular tone conditions. The activation of TRPV4 by this compound leads to vasodilation, vascular leakage, and tissue hemorrhage.

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 GSK1016790A, or 10 nM this compound 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

参考

http://www.ncbi.nlm.nih.gov/pubmed/?term=GSK1016790A%2C+a+Novel+and+Potent+TRPV4+Channel+Agonist+Induces+Urinary+Bladder+Contraction+and+Hyperactivity%3A+Part+I
https://pubmed.ncbi.nlm.nih.gov/21339821/
https://pubmed.ncbi.nlm.nih.gov/24186096/

https://pubmed.ncbi.nlm.nih.gov/25681460/

+ 展开

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：

Magnetogenetics inspired by animal Magnetoreception: ΔTRPV4MagR as a novel magnetogenetic actuator enabling remote neuromodulation of brain circuits [ Brain Stimul, 2025, 18(5):1455-1469]	PubMed: 40769384
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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。