| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
In LPS- and MCP-1-stimulated macrophage cell lines, acetamidoamide (10, 30, 100 μM; 1 hour) decreases the expression level of IκB-α phosphorylation [1].
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|---|---|
| ln Vivo |
In a dose-dependent manner, acetazolamide (0.3, 1, 3 mg/kg; iv/3, 10, 30 mg/kg; po) raises the postprandial stomach motility index [2]. With an IC50 value of 1.79 μM, acotiamide (0.83 mg/kg; intravenous injection; once) inhibits AChE in the stomach of rats [3].
|
| Cell Assay |
Cell viability assay [1]
Cell Types: NR8383, macrophage Tested Concentrations: 10, 30, 100 μM Incubation Duration: 1 hour Experimental Results: The production of TNF-α and IL-6 in NR8383 cells stimulated by LPS/MCP-1 was significant reduce. |
| Animal Protocol |
Animal/Disease Models: Male mongrel dog (9-11 kg), male beagle dog (9.6-12.9 kg) [2]
Doses: 0.3, 1, 3, 10, 30 mg/kg Route of Administration: intravenous (iv) (iv)injection; primary Experimental Results: Gastric motility increases after meals. Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats (6-7 weeks old) [3] Doses: 0.83 mg/kg Route of Administration: intravenous (iv) (iv)injection; once. Experimental Results: Functional dyspepsia was effectively improved by inhibiting AChE in the stomach of rats. |
| References |
|
| Additional Infomation |
Acotiamide is a member of salicylamides.
Acotiamide has been used in trials studying the treatment of Dyspepsia and Functional Dyspepsia. Acotiamide is 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. Drug Indication Treatment of functional dyspepsia Treatment of functional dyspepsia |
| Molecular Formula |
C21H30N4O5S
|
|---|---|
| Exact Mass |
450.193
|
| CAS # |
185106-16-5
|
| Related CAS # |
Acotiamide monohydrochloride trihydrate;773092-05-0;Acotiamide hydrochloride;185104-11-4;Acotiamide-d6
|
| PubChem CID |
5282338
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.2±0.1 g/cm3
|
| Index of Refraction |
1.592
|
| LogP |
3.56
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
10
|
| Heavy Atom Count |
31
|
| Complexity |
586
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(C1=CSC(NC(C2=CC(OC)=C(OC)C=C2O)=O)=N1)NCCN(C(C)C)C(C)C
|
| InChi Key |
TWHZNAUBXFZMCA-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C21H30N4O5S/c1-12(2)25(13(3)4)8-7-22-20(28)15-11-31-21(23-15)24-19(27)14-9-17(29-5)18(30-6)10-16(14)26/h9-13,26H,7-8H2,1-6H3,(H,22,28)(H,23,24,27)
|
| Chemical Name |
N-[2-[di(propan-2-yl)amino]ethyl]-2-[(2-hydroxy-4,5-dimethoxybenzoyl)amino]-1,3-thiazole-4-carboxamide
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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