ASP7663-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEASP7663Cat. No.: HY-101907CAS No.: 1190217-35-6分式: CHFNO分量: 263.26作靶點(diǎn): TRP Channel作通路: Membrane Transporter/Ion Channel; Neuronal Signaling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 : 25

2、0 mg/mL (949.63 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.7985 mL 18.9926 mL 37.9853 mL5 mM 0.7597 mL 3.7985 mL 7.5971 mL10 mM 0.3799 mL 1.8993 mL 3.7985 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 (7.90 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 (7.90 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Mole

4、cules 您邊的抑制劑師www.MedChemE物活性 ASP7663具有服活性的、選擇性的 TRPA1 激動(dòng)劑。ASP7663 具有抗便秘和抗腹痛的活性。體外研究 ASP7663 concentration dependently increases intracellular Ca2+ concentration in human, rat, and mouseTRPA1 expressed in HEK293 cells in a similar manner, with respective EC50 values (95% confidenceinterval CI) of 0.5

5、1 (0.400.66), 0.54 (0.410.72), and 0.50 (0.410.63) mol/L 1.ASP7663 concentration-dependently stimulates 5-HT release from QGP-1 cells, a lineage of TRPA1-expressing EC cells, with an EC50 value of 72.5 (52.699.9) mol/L 1.體內(nèi)研究 ASP7663 significantly improves the loperamide-induced delay in colonic tra

6、nsit in mice 1.ASP7663 (orally, 0.3 and 1 mg/kg) significantly shortens the prolonged bead expulsion time caused byloperamide 1.ASP7663 (orally, 1 and 3 mg/kg) exhibits inhibitory effects on colorectal distension in rat 1.Animal Model: CRD model (colorectal distension in rat) 1.Dosage: 1 and 3 mg/kg

7、.Administration: Orally.Result: Significantly reduced the number of abdominal contractions evoked during CRD atpressures of 30, 45, and 60 mmHg. ASP7663 also reduced the number of abdominalcontractions by intravenous treatment.REFERENCES1. Ryosuke Kojima, et al. Effects of Novel TRPA1 Receptor Agoni

8、st ASP7663 in Models of Drug-Induced Constipation and Visceral Pain.Eur J Pharmacol. 2014 Jan 15;723:288-93.2. Yao Lu, et al. Transient Receptor Potential Ankyrin 1 Activation Within the Cardiac Myocyte Limits Ischemia-reperfusion Injury inRodents. Anesthesiology. 2016 Dec;125(6):1171-1180.McePdfHeightCaution: Product has not been fully validated for medical applications