Cimetropium-Bromide-DA-3177-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECimetropium BromideCat. No.: HY-U00106CAS No.: 51598-60-8Synonyms: DA-3177分式: CHBrNO分量: 438.36作靶點: mAChR作通路: GPCR/G Protein; Neuronal Signaling儲存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 H2O : 50 mg/mL

2、(114.06 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.2812 mL 11.4062 mL 22.8123 mL5 mM 0.4562 mL 2.2812 mL 4.5625 mL10 mM 0.2281 mL 1.1406 mL 2.2812 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。BIOLOGICAL ACTIVITY物活性 Cimetropium Bromide (DA-3177)種毒蕈堿受體拮抗劑，于長期治療腸易激綜合征。IC5

3、0 & Target mAChR 1體外研究Cimetropium Bromide behaves as a competitive antagonist of muscarinic-mediated contractions in isolatedcolonic preparations from both species, with affinity values (pA2) ranging between 7.41 and 7.82 1.Cimetropium has potent antimuscarinic effect in inhibition of contraction of

4、 longitudinal muscle preparations.1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEIn the superfusion experiments of the preparation which has been preloaded with labelled choline,Cimetropium decreases the labelled ACh release induced by electrical field stimulation under the muscarinicautoinhibitio

5、n blocked-condition 2.體內(nèi)研究 When administered intravenously to conscious dogs provided with a colonic Thiry fistula, Cimetropium is apotent inhibitor of large bowel motility evoked by both exogenous and endogenous stimuli. CimetropiumBromide (10-100 g/kg) counteracts colonic motor response to neostig

6、mine administration with an ID50 of27.9 g/kg; both tonic and phasic components of contractile response are affected. In a comparable range ofdoses (3-100g/kg), the drug inhibits motor activity elicited by intraluminal distension 1.REFERENCES1. Identification of orally administered cimetropium bromid

7、e in the colon of the rat and its possible local spasmolytic effect.2. Saitoh N, et al. Characterization of antimuscarinic effect of cimetropium bromide in guinea pig ileum. J Smooth Muscle Res. 1997Feb;33(1):1-9.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use o