Acotiamide monohydrochloride trihydrate |
| Katalog-Nr.GC38732 |
Acotiamid-Monohydrochlorid-Trihydrat ist ein oral wirksamer, selektiver und reversibler Acetylcholinesterase (AChE)-Hemmer mit einem IC50-Wert von 1,79 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 773092-05-0
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Acotiamide monohydrochloride trihydrate is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia. Acotiamide monohydrochloride trihydrate enhances acetylcholine released by enteric neurons through muscarinic receptor antagonism and acetylcholinesterase (AChE) inhibition, thereby enhancing gastric emptying and gastric accommodation[1][2].
In in vitro studies, Acotiamide inhibits acetylcholine-induced activation of muscarinic M1 and M2 receptors in transformed Xenopus oocytes, with IC50 values of 1.8 and 10.1 μM, respectively. Acotiamide shows no/limited affinity for serotonin 5HT2, 5HT3 or 5HT4 receptors and dopamine D2 receptors[1].Acotiamide inhibits AChE activity, inhibits both the slow (competitively) and fast (noncompetitively) inward currents induced by acetylcholine, enhances electrically stimulated contraction of gastric fundus and gastric body, facilitates acetylcholine release from enteric neurons and, using patch-clamp techniques, potentiates L-type voltagedependent Ca2+ current and inhibits GABA-induced current in area postrema neurons[1].
In in vivo animal models, Acotiamide stimulates postprandial gastroduodenal and/or colonic motor activity, and improves delayed but not normal gastric emptying. For example, Acotiamide significantly improves delayed gastric emptying and feeding inhibition in a restraintstress-induced rat model, but does not affect normal gastric emptying or feeding in intact rats[1].
[1]. Nowlan ML, et al. Acotiamide: first global approval. Drugs. 2013 Aug;73(12):1377-83. [2]. Attia KAM, et al. Spectrofluorimetric determination of acotiamide hydrochloride trihydrate in the presence of its oxidative degradation product. Luminescence. 2018 Jun;33(4):806-811.
| Cas No. | 773092-05-0 | SDF | |
| Canonical SMILES | O=C(C1=CSC(NC(C2=CC(OC)=C(OC)C=C2O)=O)=N1)NCCN(C(C)C)C(C)C.[H]Cl.O.O.O | ||
| Formula | C21H37ClN4O8S | M.Wt | 541.06 |
| Löslichkeit | DMSO: 125 mg/mL (231.03 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.8482 mL | 9.2411 mL | 18.4822 mL |
| 5 mM | 0.3696 mL | 1.8482 mL | 3.6964 mL |
| 10 mM | 0.1848 mL | 0.9241 mL | 1.8482 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *