Acotiamide hydrochloride

SKU: orb1223055

Description

Acotiamide Hydrochloride is the hydrochloride salt form of acotiamide, a prokinetic agent with gastrointestinal (GI) motility-enhancing activity. Although the exact mechanism by which acotiamide exerts its effect has yet to be fully elucidated, this agent appears to inhibit acetylcholinesterase (AchE), an enzyme responsible for the breakdown of acetylcholine (Ach). Increased Ach concentrations lead to an improvement of gastric emptying and GI motility and eventually to a reduction of dyspepsia symptoms.(In Vivo):Acotiamide monohydrochloride trihydrate (0.3, 1, 3 mg/kg; i.v./3, 10, 30 mg/kg; p.o.) increases the postprandial gastric motility index in a dose-dependent manner.Acotiamide monohydrochloride trihydrate (0.83 mg/kg; i.v.; once) inhibits AChE in rat stomach with IC50 of 1.79 μM.

Key Properties

• CAS Number: 773092-05-0
• MW: 541.06
• Purity: >98% (HPLC)
• Formula: C₂₁H₃₇ClN₄O₈S
• SMILES: s1c(nc(c1)C(=O)NCCN(C(C)C)C(C)C)NC(=O)c1c(cc(c(c1)OC)OC)O.O.Cl.O.O
• Target: Melatonin Receptor
• Solubility: In Vitro: DMSO : 125 mg/mL (231.03 mM)

Bioactivity

• In Vivo:
  Acotiamide monohydrochloride trihydrate (0.3, 1, 3 mg/kg; i. v. /3, 10, 30 mg/kg; p.o.) increases the postprandial gastric motility index in a dose-dependent manner. Acotiamide monohydrochloride trihydrate (0.83 mg/kg; i. v. ; once) inhibits AChE in rat stomach with IC50 of 1.79 μM. Animal model: Male mongrel dogs (9-11 kg), Male beagle dogs (9.6-12.9 kg). Dosage: 0.3, 1, 3, 10, 30 mg/kg. Administration: Intravenous injection; once. Result: Increased the postprandial gastric motility. Animal model: Male Sprague-Dawley rats (aged 6-7 weeks). Dosage: 0.83 mg/kg. Administration: Intravenous injection; once. Result: Effectively improved functional dyspepsia by inhibiting AChE in rat stomach.
• In Vitro:
  Acotiamide monohydrochloride trihydrate (10, 30, 100 μM; 1 hour) reduces expression levels of IκB-α phosphorylation in LPS- and MCP-1-stimulated macrophage cell lines. Cell Viability Assay Cell line: NR8383, macrophage. Concentration: 10, 30, 100 μM. Incubation time: 1 hour. Result: Significantly reduced both TNF-α and IL-6 productions in LPS/MCP-1-stimulated NR8383 cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Melatonin Receptor