TAK-071 - M1R Agonist - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETAK-071Cat. No.: HY-122190CAS No.: 1820812-16-5分式: CHFNO分量: 421.46作靶點: mAChR作通路: GPCR/G Protein; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 135 mg/mL (320.32 mM; Need

2、 ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.3727 mL 11.8635 mL 23.7270 mL5 mM 0.4745 mL 2.3727 mL 4.7454 mL10 mM 0.2373 mL 1.1864 mL 2.3727 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存

3、條件，適當保存；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. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.25 mg/mL (5.34 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.25 mg/mL (5.34 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.25 mg/mL (5.34

4、mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 TAK-071種新型, 效，選擇性的毒蕈堿酰膽堿受體1 (M1R)正變構(gòu)調(diào)節(jié)劑。 TAK-071激活M1R的EC50為520nM。IC50 & Target EC50: 520 nM (M1R) 1體內(nèi)研究 TAK-071 increase hippocampal inositol monophosphate production through M1R activation and improvedDB00747

5、-induced cognitive deficits in rats at 0.3 mg/kg 1.TAK-071 also induce diarrhea at 10 mg/kg in rats 1.Combining sub-effective doses of TAK-071 (3 mg/kg) with an acetylcholinesterase inhibitor significantlyameliorates DB00747-induced cognitive deficits in rats 1.REFERENCES1. Sako Y, et al. TAK-071, a

6、 novel M1 positive allosteric modulator with low cooperativity, improves cognitive function in rodents with fewcholinergic side effects. Neuropsychopharmacology. 2018 Aug 1. doi: 10.1038/s41386-018-0168-8.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820