5.30533

GSK1016790A

≥98% (HPLC), powder, TRPV4 channel agonist, Calbiochem

• 別名: TRPV4 Agonist, GSK1016790A, GSK101, Transient Receptor Potential Vanilloid 4 Channel Agonist
• 実験式（ヒル表記法）: C₂₈H₃₂Cl₂N₄O₆S₂
• CAS番号: 942206-85-1
• 分子量: 655.61
• UNSPSCコード: 12352200
• PubChem Substance ID: 23630211
• NACRES: NA.77

特性

• product name: TRPV4 Agonist, GSK1016790A,
• アッセイ: ≥98% (HPLC)
• 品質水準: 100
• 形状: powder
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: white
• 溶解性: DMSO: 50 mg/mL
• 保管温度: −20°C
• SMILES記法: CC(C)CC(C(=O)N1CCN(CC1)C(=O)C(CO)NS(=O)(=O)C2=C(C=C(C=C2)Cl)Cl)NC(=O)C3=CC4=CC=CC=C4S3

詳細

詳細

A cell-permeable piperazine amide derivative that acts as a potent and selective agonist of Transient Receptor Potential Vanilloid 4 Channel (TRPV4) and enhances Ca2+ flux in a variety of human and mouse cells (EC₅₀ = 2.1 nM and 18 nM in human and mouse TRPV4 expressed in HEK293 cells, respectively). Generates greater [Ca2+]i transients in chrondocytes than hypoosmotic treatments. Shown to be about 300-fold more potent that 4-α-PDD in activating TRPV4 channels. Suggested to act by recruiting previously inactive channels, rather than through increasing elevation of basal activity. Does not affect TRPM8 and TRPA1 channels even at high concentrations (~20 µM).

A cell-permeable piperazine amide derivative that acts as a potent and selective agonist of Transient Receptor Potential Vanilloid 4 Channel (TRPV4) and enhances Ca2+ flux in a variety of human and mouse cells (EC₅₀ = 2.1 nM and 18 nM in human and mouse TRPV4 expressed in HEK293 cells, respectively). Generates greater [Ca2+]i transients in chrondocytes than hypoosmotic treatments. Shown to be about 300-fold more potent that 4-α-PDD in activating TRPV4 channels. Suggested to act by recruiting previously inactive channels, rather than through increasing elevation of basal activity. Does not affect TRPM8 and TRPA1 channels even at high concentrations (~20 µM).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

生物化学的／生理学的作用

Primary Target
TRPV4

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

その他情報

OʹConor, C.J., 2014. PNAS.111, 1316.
Sullivan, M.N., et al. 2012. Mol. Pharmacol.82, 464.
Jun, M., et al. 2011. PLoS One.6, e16713.
Thorneloe, K. S., et al. 2008. J. Pharm. Exp. Ther.326,432.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 1
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable