ASP7663-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEASP7663Cat. No.: HY-101907CAS No.: 1190217-35-6分式: CHFNO分量: 263.26作靶点: TRP Channel作通路: Membrane Transporter/Ion Channel; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 25

2、0 mg/mL (949.63 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液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请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，

3、建议您现现配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (7.90 mM); Clear solution2. 请依序添加每种溶剂： 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 您边的抑制剂师www.MedChemE物活性 ASP7663具有服活性的、选择性的 TRPA1 激动剂。ASP7663 具有抗便秘和抗腹痛的活性。体外研究 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.体内研究 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