[CAS NO. 185106-16-5] Acotiamide

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [185106-16-5]

Catalog

SLK-S5075

Brand

Selleck

CAS

185106-16-5

DESCRIPTION [185106-16-5]

Overview

MDL	MFCD00953661
Molecular Weight	450.55
Molecular Formula	C21H30N4O5S
SMILES	C(NC1=NC(C(NCCN(C(C)C)C(C)C)=O)=CS1)(=O)C2=CC(OC)=C(OC)C=C2O

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.2195 mL	11.0975 mL	22.1951 mL
5 mM	0.4439 mL	2.2195 mL	4.4390 mL
10 mM	0.2220 mL	1.1098 mL	2.2195 mL
50 mM	0.0444 mL	0.2220 mL	0.4439 mL

Description

Acotiamide (Acofide, Z388) is a novel inhibitor with fundus-relaxing and gastroprokinetic properties.

Targets

AChE ^[2]

3 μM

In vitro

Acotiamide inhibited recombinant human and canine stomach-derived acetylcholinesterase (AChE) activity in vitro. The mode of the AChE inhibitory action of acotiamide was selective and reversible. It shows a mixed-type inhibition toward recombinant human AChE activity. Ki1 (competitive inhibition) and Ki2 values (noncompetitive inhibition) of acotiamide were 610 nM and 2.7 μM, respectively. IC50 values for AChE of acotiamide is 3 μM. IC50 value for BuChE of acotiamide is >1.0 × 10 M. Acotiamide inhibited AChE selectively, and the ratio of the IC50 value for BuChE to AChE was more than 330. Acotiamide has no affinity for α2-adrenoceptor, dopamine D2S receptor, or serotonin 5-HT4 receptors, including 5-HT4c, 5-HT4d, or 5-HT4e receptors. In in vitro studies, acotiamide enhanced acetylcholine- but not carbachol-induced contractile responses of guinea pig gastric antrum strips.

In vivo

Acotiamide stimulates gastric motility and improves gastric motility dysfunction in rats by inhibiting AChE activity. It improves stress-induced delayed gastric emptying in rats. Acotiamide also enhances gastric motility by inhibiting AChE activity without affecting QT interval in dogs.

References

[1] Kawachi M, et al. Eur J Pharmacol. 2011, 666(1-3):218-25.
[2] Matsunaga Y, et al. J Pharmacol Exp Ther. 2011, 336(3):791-800.

Synonyms

4-Thiazolecarboxamide, N-[2-[bis(1-methylethyl)amino]ethyl]-2-[(2-hydroxy-4,5-dimethoxybenzoyl)amino]-

N-[2-[Bis(1-methylethyl)amino]ethyl]-2-[(2-hydroxy-4,5-dimethoxybenzoyl)amino]-4-thiazolecarboxamide

Acotiamide