Mosapride citrate dihydrate | Gasmotin | AS-4370 | CAS#636582-62-2 | CAS#112885-41-3 | 5-HT4 Receptor Agonist

MedKoo Cat#: 328511 | Name: Mosapride citrate dihydrate

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Mosapride Citrate (also known as Gasmotin, AS-4370, GR-107719-B, and TAK-370) is a 5-HT4 receptor agonist used to stimulate gastrointestinal motility via acetylcholine. Mosapride Citrate facilitates acetylcholine release from the enteric cholinergic neurons.

Chemical Structure

Mosapride citrate dihydrate

CAS#636582-62-2 (citrate hydrate)

Theoretical Analysis

MedKoo Cat#: 328511

Name: Mosapride citrate dihydrate

CAS#: 636582-62-2 (citrate hydrate)

Chemical Formula: C27H37ClFN3O12

Exact Mass:

Molecular Weight: 650.05

Elemental Analysis: C, 49.89; H, 5.74; Cl, 5.45; F, 2.92; N, 6.46; O, 29.53

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 350.00	2 Weeks
50mg	USD 1,050.00	2 Weeks

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Related CAS #

636582-62-2 (citrate hydrate) 112885-41-3 (free base) 112885-42-4 (citrate)

Synonym

Mosapride Citrate; AS-4370; GR-107719-B; TAK-370; AS 4370; GR 107719 B; TAK 370; AS4370; GR107719B; TAK370; Gasmotin

IUPAC/Chemical Name

4-amino-5-chloro-2-ethoxy-N-((4-(4-fluorobenzyl)morpholin-2-yl)methyl)benzamide 2-hydroxypropane-1,2,3-tricarboxylate dihydrate

InChi Key

KVKIQHMTGSGTFO-UHFFFAOYSA-N

InChi Code

InChI=1S/C21H25ClFN3O3.C6H8O7.2H2O/c1-2-28-20-10-19(24)18(22)9-17(20)21(27)25-11-16-13-26(7-8-29-16)12-14-3-5-15(23)6-4-14;7-3(8)1-6(13,5(11)12)2-4(9)10;;/h3-6,9-10,16H,2,7-8,11-13,24H2,1H3,(H,25,27);13H,1-2H2,(H,7,8)(H,9,10)(H,11,12);2*1H2

SMILES Code

O=C(NCC1CN(CC2=CC=C(F)C=C2)CCO1)C3=CC(Cl)=C(N)C=C3OCC.O=C(CC(C(O)=O)(O)CC(O)=O)O.[H]O[H].[H]O[H]

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Related CAS# 112885-41-3 (Mosapride) 636582-62-2 (Mosapride Citrate)

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Mosapride (TAK-370) citrate dehydrate is a gastroprokinetic agent with 5-hydroxytryptamine4 receptor agonist activity and potently inhibits Kv4.3.

In vitro activity:

This study tested the effect of mosapride on 5-hydroxytryptamine type 3 (5-HT3) receptor currents because the 5-HT3 receptors are also known to be expressed in the GI system and have an important role in the regulation of GI functions. The 5-HT3 receptor current amplitudes were inhibited by mosapride in a concentration-dependent manner. Mosapride blocked the peak currents evoked by the application of 5-HT in a competitive manner because the EC50 shifted to the right without changing the maximal effect. Reference: Korean J Physiol Pharmacol. 2019 Sep;23(5):419-426. https://pubmed.ncbi.nlm.nih.gov/31496879/

In vivo activity:

Forty-five healthy male Sprague-Dawley rats that were pathogen-free (weight 200-220 g) were randomly divided into a control group (n = 15), model group (n = 15) and mosapride group (n = 15). There was a significant decline in the rate of gut microbiota translocation in the mosapride group compared with the model group. There were intestinal microbiota changes in the mosapride group compared with that of the model group, including Bacteroidetes, Prevotellaceae, Alloprevotella, Ruminiclostridium, Negativicutes, Selenomonadales, Veillonellaceae, Anaerovibrio, Campylobacterales, Epsilonbacteraeota, Helicobacter, Oscillibacter, Verrucomicrobiales, Akkermansia, Intestinimonas, Eubacterium, Clostridiaceae, Clostridium, Bacteroides, Tyzzerella, Actinobacteria, and Bifidobacteriales. Among these bacteria, Alloprevotella showed a strong correlation with the other bacteria. Reference: Adv Clin Exp Med. 2022 Jun;31(6):623-633. https://pubmed.ncbi.nlm.nih.gov/35275452/

Preparing Stock Solutions

The following data is based on the product molecular weight 650.05 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Park YS, Sung KW. Gastroprokinetic agent, mosapride inhibits 5-HT3 receptor currents in NCB-20 cells. Korean J Physiol Pharmacol. 2019 Sep;23(5):419-426. doi: 10.4196/kjpp.2019.23.5.419. Epub 2019 Aug 26. PMID: 31496879; PMCID: PMC6717790. 2. Mine Y, Yoshikawa T, Oku S, Nagai R, Yoshida N, Hosoki K. Comparison of effect of mosapride citrate and existing 5-HT4 receptor agonists on gastrointestinal motility in vivo and in vitro. J Pharmacol Exp Ther. 1997 Dec;283(3):1000-8. PMID: 9399969. 3. Chen D, Xiong J, Feng H, Liu Y, Xu J, Xu H. The influence of mosapride on gut microbiota of carbon tetrachloride-induced cirrhosis rats based on 16S rRNA gene sequencing. Adv Clin Exp Med. 2022 Jun;31(6):623-633. doi: 10.17219/acem/146320. PMID: 35275452. 4. Krishna V, Bairy KL, Patil N, Sunny SV. Evaluation of the antianxiety and antidepressant activities of mosapride in Wistar albino rats. J Basic Clin Physiol Pharmacol. 2019 Jul 18;30(4). doi: 10.1515/jbcpp-2018-0089. PMID: 31318691.

In vitro protocol:

In vivo protocol:

1. Chen D, Xiong J, Feng H, Liu Y, Xu J, Xu H. The influence of mosapride on gut microbiota of carbon tetrachloride-induced cirrhosis rats based on 16S rRNA gene sequencing. Adv Clin Exp Med. 2022 Jun;31(6):623-633. doi: 10.17219/acem/146320. PMID: 35275452. 2. Krishna V, Bairy KL, Patil N, Sunny SV. Evaluation of the antianxiety and antidepressant activities of mosapride in Wistar albino rats. J Basic Clin Physiol Pharmacol. 2019 Jul 18;30(4). doi: 10.1515/jbcpp-2018-0089. PMID: 31318691.

1: Maruoka D, Arai M, Tanaka T, Okimoto K, Oyamada A, Minemura S, Tsuboi M, Matsumura T, Nakagawa T, Kanda T, Katsuno T, Imazeki F, Yokosuka O. Mosapride citrate increases postprandial glucagon-like peptide-1, insulin, and gene expression of sweet taste receptors. Dig Dis Sci. 2015 Feb;60(2):345-53. doi: 10.1007/s10620-014-3271-7. Epub 2014 Jul 10. PubMed PMID: 25008428. 2: Kim YH, Bae YJ, Kim HS, Cha HJ, Yun JS, Shin JS, Seong WK, Lee YM, Han KM. Measurement of Human Cytochrome P450 Enzyme Induction Based on Mesalazine and Mosapride Citrate Treatments Using a Luminescent Assay. Biomol Ther (Seoul). 2015 Sep;23(5):486-92. doi: 10.4062/biomolther.2015.041. Epub 2015 Sep 1. PubMed PMID: 26336590; PubMed Central PMCID: PMC4556210. 3: Okubo H, Nakatsu Y, Sakoda H, Kushiyama A, Fujishiro M, Fukushima T, Matsunaga Y, Ohno H, Yoneda M, Kamata H, Shinjo T, Iwashita M, Nishimura F, Asano T. Mosapride citrate improves nonalcoholic steatohepatitis with increased fecal lactic acid bacteria and plasma glucagon-like peptide-1 level in a rodent model. Am J Physiol Gastrointest Liver Physiol. 2015 Jan 15;308(2):G151-8. doi: 10.1152/ajpgi.00198.2014. Epub 2014 Nov 26. PubMed PMID: 25428903. 4: Aoki K, Kamiyama H, Masuda K, Togashi Y, Terauchi Y. Mosapride citrate, a 5-HT₄ receptor agonist, increased the plasma active and total glucagon-like peptide-1 levels in non-diabetic men. Endocr J. 2013;60(4):493-9. Epub 2012 Dec 18. PubMed PMID: 23257734. 5: Takatori K, Yoshida R, Horai A, Satake S, Ose T, Kitajima N, Yoneda S, Adachi K, Amano Y, Kinoshita Y. Therapeutic effects of mosapride citrate and lansoprazole for prevention of aspiration pneumonia in patients receiving gastrostomy feeding. J Gastroenterol. 2013 Oct;48(10):1105-10. doi: 10.1007/s00535-012-0725-6. Epub 2012 Dec 13. PubMed PMID: 23238778. 6: Lee JW, Sung KW, Lee OY, Lee SE, Sohn CI. The effects of 5-HT4 receptor agonist, mosapride citrate, on visceral hypersensitivity in a rat model. Dig Dis Sci. 2012 Jun;57(6):1517-24. doi: 10.1007/s10620-012-2101-z. Epub 2012 Mar 17. PubMed PMID: 22427128. 7: Tajika M, Niwa Y, Bhatia V, Kondo S, Tanaka T, Mizuno N, Hara K, Hijioka S, Imaoka H, Komori K, Yamao K. Can mosapride citrate reduce the volume of lavage solution for colonoscopy preparation? World J Gastroenterol. 2013 Feb 7;19(5):727-35. doi: 10.3748/wjg.v19.i5.727. PubMed PMID: 23430381; PubMed Central PMCID: PMC3574599. 8: Ida Y, Hosoe N, Imaeda H, Bessho R, Ichikawa R, Naganuma M, Kanai T, Hibi T, Ogata H. Effects of the oral administration of mosapride citrate on capsule endoscopy completion rate. Gut Liver. 2012 Jul;6(3):339-43. doi: 10.5009/gnl.2012.6.3.339. Epub 2012 Jul 12. PubMed PMID: 22844562; PubMed Central PMCID: PMC3404171. 9: Amano T, Ariga H, Kurematsu A, Yamato S, Morioka S, Masaka A, Kanazawa M, Fukudo S. Effect of 5-hydroxytryptamine receptor 4 agonist mosapride on human gastric accommodation. Neurogastroenterol Motil. 2015 Sep;27(9):1303-9. doi: 10.1111/nmo.12623. PubMed PMID: 26303048. 10: Ali AA, Sayed OM. Preparation and characterization of mosapride citrate inclusion complexes with natural and synthetic cyclodextrins. Pharm Dev Technol. 2013 Sep-Oct;18(5):1042-50. doi: 10.3109/10837450.2011.646425. Epub 2011 Dec 30. PubMed PMID: 22206481.