[CAS NO. 51598-60-8] Cimetropium Bromide
PRODUCTS SPECIFICATIONS [51598-60-8]
DESCRIPTION [51598-60-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 438.36 |
| Molecular Formula | C21H28BrNO4 |
| SMILES | C[N+]1([C@H]2[C@@H](O3)[C@@H]3[C@@H]1C[C@H](OC([C@@H](C4=CC=CC=C4)CO)=O)C2)CC5CC5.[Br-] |
Summary
Cimetropium Bromide (DA-3177) is a mAChR antagonist for long-term treatment of irritable bowel syndrome.
IC50 & Target
mAChR [1]
In Vitro
Cimetropium Bromide behaves as a competitive antagonist of muscarinic-mediated contractions in isolated colonic 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 longitudinal muscle preparations. In 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 muscarinic autoinhibition blocked-condition [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
When administered intravenously to conscious dogs provided with a colonic Thiry fistula, Cimetropium is a potent inhibitor of large bowel motility evoked by both exogenous and endogenous stimuli. Cimetropium Bromide (10-100 μg/kg) counteracts colonic motor response to neostigmine administration with an ID 50 of 27.9 μg/kg; both tonic and phasic components of contractile response are affected. In a comparable range of doses (3-100μg/kg), the drug inhibits motor activity elicited by intraluminal distension [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01842932 | Ajou University School of Medicine |
Colonoscopy
|
December 2009 | Phase 4 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 50 mg/mL ( 114.06 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2812 mL | 11.4062 mL | 22.8123 mL |
| 5 mM | 0.4562 mL | 2.2812 mL | 4.5625 mL |
| 10 mM | 0.2281 mL | 1.1406 mL | 2.2812 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (228.12 mM); Clear solution; Need ultrasonic
References
Synonyms