A2764-dihydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEA2764 dihydrochlorideCat. No.: HY-135809CAS No.: 861038-72-4分式: CHClNO分量: 351.7作靶點(diǎn): Potassium Channel作通路: Membrane Transporter/Ion Channel儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 41.

2、67 mg/mL (118.48 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.8433 mL 14.2167 mL 28.4333 mL5 mM 0.5687 mL 2.8433 mL 5.6867 mL10 mM 0.2843 mL 1.4217 mL 2.8433 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液

3、，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.91 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (5.91 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Mol

4、ecules 您邊的抑制劑師www.MedChemE物活性 A2764 dihydrochlorideTRESK (K2P18.1) 的選擇性抑制劑，對(duì) TREK-1 和 TALK-1 有定的抑制作。A2764 dihydrochloride 相底 mTRESK 電流，對(duì)激活渠道更敏感 (IC50= 6.8 M)。A2764dihydrochloride 可導(dǎo)致細(xì)胞去極化，增加細(xì)胞的興奮性，具有探索 TRESK 通道在偏頭痛和痛覺(jué)中的作的潛。IC50 & Target IC50: 6.8 M (activated mTRESK channel) 1體外研究 A2764 (100 M) inhi

5、bits the background K+ current by 42.811.5% when it applies to the oocytes expressingmTRESK 1.A2764 (100 M) shows an improved inhibitory potency for activated channel with an IC50 ofactivated channel in ionomycin-activated mTRESK current.The subsequent application of A2764 stronglyinhibits the curre

6、nt (77.83.5%) 1.A2764 (100 M) inhibits the current of TRESK under resting conditionsand in the activated state by 42.811.5% and 77.83.5%, respectively 1.REFERENCES1. Lengyel M, et al. Chemically Modified Derivatives of the Activator Compound Cloxyquin Exert Inhibitory Effect on TRESK (K2P18.1)Background Potassium Channel.Mol Pharmacol. 2019 Jun;95(6):652-660.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: