Pilocarpine-Hydrochloride - mAChR Agonist - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPilocarpine HydrochlorideCat. No.: HY-B0726CAS No.: 54-71-7分式: CHClNO分量: 244.72作靶點: mAChR作通路: GPCR/G Protein; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 years* 該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)現(xiàn)配，即刻使。溶解性數(shù)據(jù)體外實驗 H2O : 37 mg/mL (151.19 mM)DMSO

2、: 6.8 mg/mL (27.79 mM; Need ultrasonic and warming)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 4.0863 mL 20.4315 mL 40.8630 mL5 mM 0.8173 mL 4.0863 mL 8.1726 mL10 mM 0.4086 mL 2.0432 mL 4.0863 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；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)現(xiàn)配，即刻使。體內(nèi)實驗 P

3、ilocarpine hydrochloride is prepared in 0.9% NaCl saline4.BIOLOGICAL ACTIVITY物活性 Pilocarpine Hydrochloride種選擇性的 M3 型毒蕈堿酰膽堿受體 (M3 muscarinic receptor) 激動劑。IC50 & Target M3 muscarinic receptor 11/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE體外研究 To evaluate the cytotoxicity of Pilocarpine, the morph

4、ology and viability of human corneal stromal (HCS) cellsare examined by light microscopy and MTT assay, respectively. Morphological observations show that HCScells exposed to Pilocarpine at a concentration from 0.625 to 20 g/L exhibit dose- and time-dependentproliferation retardation and morphologic

5、al abnormality such as cellular shrinkage, cytoplasmic vacuolation,detachment from culture matrix, and eventually death, while no obvious difference is observed betweenthose exposed to Pilocarpine below the concentration of 0.625 g/L and controls. Results of MTT assay revealthat the cell viability o

6、f HCS cells decrease with time and concentration after exposing to Pilocarpine abovethe concentration of 0.625 g/L (P 2. The partial muscarinic agonist, Pilocarpine, evokes concentration-dependent relaxation with an EC50 of 2.4 mM in isolated segments of rat tail artery that were constricted withPen

7、ylephrine (10 to 200 nM) 3.體內(nèi)研究 The Pilocarpine-induced saliva secretion of the control rats (CN) and exercised (EX) rats is examined. Asignificantly greater amount of saliva is induced by Pilocarpine in the EX rats than in the CN rats (P+concentration in the saliva of the EX rats is significantly l

8、ower than that of the CN rats (P 1.PROTOCOLCell Assay 2 Cell viability is determined by MTT assay. Briefly, HCS cells are inoculated into a 96-well culture plate (Nunc)at a density of 1104 cells/100 L/well, and are cultured and treated. At a 4h interval, the Pilocarpine (0.625to 20 g/L)-containing m

9、edium is replaced entirely with 100 L serum-free DMEM/F12 medium containing 1.0g/L MTT, and the cells are incubated at 37C in the dark for 4h. After the MTT-containing medium isdiscarded with caution, 150 L DMSO is added to dissolve the produced formazan crystals at 37C in thedark for 15 min, and th

10、e absorbance at 490 nm is measured with a Multiskan GO microplate reader 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats 1Administration 1 Male, 10-week-old Wistar rats are assigned to one of two groups, exercise (EX, n=6) and control (CN,

11、 n=6).The EX rats are kept for 40 days in cages with a running wheel (SN-451), allowing them to undertakevoluntary exercise, while the CN rats are kept in cages with the running wheel locked. On the 40th day,Pilocarpine-induced saliva is measured as follows. Briefly, the rats are anesthetized, prewe

12、ighed cotton wasplaced in their mouths sublingually, and Pilocarpine (0.5 mg/kg) is intraperitoneally injected to induce salivasecretion. Each cotton ball is then changed every 10 min for 1 h. The collected cotton balls are weighedagain, and the mass of saliva secreted is calculated by subtracting t

13、he initial from the final weight.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Neuropharmacology. 2017 May 1;117:238-248. Epilepsy Res. 2018 May;142:45-52.See more customer validations on HYPERLINK / www.MedChemEREFERENCES2/3 Master of Sma

14、ll Molecules 您邊的抑制劑師www.MedChemE1. Matsuzaki K, et al. Daily voluntary exercise enhances pilocarpine-induced saliva secretion and aquaporin 1 expression in ratsubmandibular glands. FEBS Open Bio. 2017 Dec 7;8(1):85-93.2. Yuan XL, et al. Cytotoxicity of pilocarpine to human corneal stromal cells and

15、its underlying cytotoxic mechanisms. Int J Ophthalmol.2016 Apr 18;9(4):505-11.3. Tonta MA, et al. Pilocarpine-induced relaxation of rat tail artery by a non-cholinergic mechanism and in the absence of an intactendothelium. Br J Pharmacol. 1994 Jun;112(2):525-32.4. Wang RF, et al. Post-treatment with the GLP-1 analogue liraglutide alleviate chronic inflammation and mitochondrial stress induced byStatus epilepticus. Epil