MA-2029
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MedKoo CAT#: 532174

CAS#: 287206-61-5

Description: MA-2029 is a novel selective and competitive motilin receptor antagonist. It inhibits motilin-induced intestinal contractions and visceral pain in rabbits.


Chemical Structure

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MA-2029
CAS# 287206-61-5

Theoretical Analysis

MedKoo Cat#: 532174
Name: MA-2029
CAS#: 287206-61-5
Chemical Formula: C31H46ClFN4O4
Exact Mass: 592.32
Molecular Weight: 593.181
Elemental Analysis: C, 62.77; H, 7.82; Cl, 5.98; F, 3.20; N, 9.45; O, 10.79

Price and Availability

Size Price Availability Quantity
1mg USD 350 2 Weeks
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Synonym: MA-2029; MA 2029; MA2029.

IUPAC/Chemical Name: (2S)-N-[(2S)-3-(3-tert-butyl-4-hydroxyphenyl)-1-(ethylamino)-1-oxopropan-2-yl]-2-[[(2S)-3-(4-fluorophenyl)-2-(methylamino)propanoyl]-methylamino]-3-methylbutanamide;hydrochloride

InChi Key: AMSDRHOIAWZBTJ-PBQYMGKRSA-N

InChi Code: InChI=1S/C31H45FN4O4.ClH/c1-9-34-28(38)24(18-21-12-15-26(37)23(16-21)31(4,5)6)35-29(39)27(19(2)3)36(8)30(40)25(33-7)17-20-10-13-22(32)14-11-20;/h10-16,19,24-25,27,33,37H,9,17-18H2,1-8H3,(H,34,38)(H,35,39);1H/t24-,25-,27-;/m0./s1

SMILES Code: CC(C)[C@H](N(C([C@@H](NC)CC1=CC=C(F)C=C1)=O)C)C(N[C@@H](CC2=CC=C(O)C(C(C)(C)C)=C2)C(NCC)=O)=O.[H]Cl

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:

Product Data:
Biological target: MA-2029 is a selective, orally active, and competitive motilin receptor antagonist (IC50=4.9 nM).
In vitro activity: MA-2029 at 100 microg/ml also decreased the maximum rising velocity and action potential amplitude in the action potential study, indicating that MA-2029 has Na(+) channel blocking potential. Reference: J Toxicol Sci. 2008 Dec;33(5):631-9. https://pubmed.ncbi.nlm.nih.gov/19043284/
In vivo activity: This study determined the coordinated action of motilin and ghrelin on gastric motility during fasted and postprandial contractions by using house musk shrew (Suncus murinus; order: Insectivora, suncus named as the laboratory strain). Administration of the motilin receptor antagonist MA-2029 (0.1 mg/kg) and/or (D-Lys(3))-GHRP-6 (0.6 mg/kg) at the peak of phase III abolished the spontaneous gastric phase III contractions in vivo. Reference: Endocrinology. 2015 Dec;156(12):4437-47. https://pubmed.ncbi.nlm.nih.gov/26441238/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 43.3 73.05

Preparing Stock Solutions

The following data is based on the product molecular weight 593.18 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.

Recalculate based on batch purity %
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. Tabo M, Komatsu R, Honda M, Itoh M, Kimura K. Cardiovascular safety profile of MA-2029, a novel motilin receptor antagonist. J Toxicol Sci. 2008 Dec;33(5):631-9. doi: 10.2131/jts.33.631. PMID: 19043284. 2. Kuroda K, Hequing H, Mondal A, Yoshimura M, Ito K, Mikami T, Takemi S, Jogahara T, Sakata I, Sakai T. Ghrelin Is an Essential Factor for Motilin-Induced Gastric Contraction in Suncus murinus. Endocrinology. 2015 Dec;156(12):4437-47. doi: 10.1210/en.2015-1561. Epub 2015 Oct 6. PMID: 26441238. 3. Ozaki K, Onoma M, Muramatsu H, Sudo H, Yoshida S, Shiokawa R, Yogo K, Kamei K, Cynshi O, Kuromaru O, Peeters TL, Takanashi H. An orally active motilin receptor antagonist, MA-2029, inhibits motilin-induced gastrointestinal motility, increase in fundic tone, and diarrhea in conscious dogs without affecting gastric emptying. Eur J Pharmacol. 2009 Aug 1;615(1-3):185-92. doi: 10.1016/j.ejphar.2009.04.059. Epub 2009 May 13. PMID: 19445919.
In vitro protocol: 1. Tabo M, Komatsu R, Honda M, Itoh M, Kimura K. Cardiovascular safety profile of MA-2029, a novel motilin receptor antagonist. J Toxicol Sci. 2008 Dec;33(5):631-9. doi: 10.2131/jts.33.631. PMID: 19043284.
In vivo protocol: 1. Kuroda K, Hequing H, Mondal A, Yoshimura M, Ito K, Mikami T, Takemi S, Jogahara T, Sakata I, Sakai T. Ghrelin Is an Essential Factor for Motilin-Induced Gastric Contraction in Suncus murinus. Endocrinology. 2015 Dec;156(12):4437-47. doi: 10.1210/en.2015-1561. Epub 2015 Oct 6. PMID: 26441238. 2. Ozaki K, Onoma M, Muramatsu H, Sudo H, Yoshida S, Shiokawa R, Yogo K, Kamei K, Cynshi O, Kuromaru O, Peeters TL, Takanashi H. An orally active motilin receptor antagonist, MA-2029, inhibits motilin-induced gastrointestinal motility, increase in fundic tone, and diarrhea in conscious dogs without affecting gastric emptying. Eur J Pharmacol. 2009 Aug 1;615(1-3):185-92. doi: 10.1016/j.ejphar.2009.04.059. Epub 2009 May 13. PMID: 19445919.

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1: Mondal A, Koyama K, Mikami T, Horita T, Takemi S, Tsuda S, Sakata I, Sakai T. Underlying mechanism of the cyclic migrating motor complex in Suncus murinus: a change in gastrointestinal pH is the key regulator. Physiol Rep. 2017 Jan;5(1). pii: e13105. doi: 10.14814/phy2.13105. PubMed PMID: 28082431; PubMed Central PMCID: PMC5256163.

2: Kuroda K, Hequing H, Mondal A, Yoshimura M, Ito K, Mikami T, Takemi S, Jogahara T, Sakata I, Sakai T. Ghrelin Is an Essential Factor for Motilin-Induced Gastric Contraction in Suncus murinus. Endocrinology. 2015 Dec;156(12):4437-47. doi: 10.1210/en.2015-1561. PubMed PMID: 26441238.

3: Mondal A, Xie Z, Miyano Y, Tsutsui C, Sakata I, Kawamoto Y, Aizawa S, Tanaka T, Oda S, Sakai T. Coordination of motilin and ghrelin regulates the migrating motor complex of gastrointestinal motility in Suncus murinus. Am J Physiol Gastrointest Liver Physiol. 2012 May 15;302(10):G1207-15. doi: 10.1152/ajpgi.00379.2011. PubMed PMID: 22383491.

4: Ozaki K, Onoma M, Muramatsu H, Sudo H, Yoshida S, Shiokawa R, Yogo K, Kamei K, Cynshi O, Kuromaru O, Peeters TL, Takanashi H. An orally active motilin receptor antagonist, MA-2029, inhibits motilin-induced gastrointestinal motility, increase in fundic tone, and diarrhea in conscious dogs without affecting gastric emptying. Eur J Pharmacol. 2009 Aug 1;615(1-3):185-92. doi: 10.1016/j.ejphar.2009.04.059. PubMed PMID: 19445919.

5: Tabo M, Komatsu R, Honda M, Itoh M, Kimura K. Cardiovascular safety profile of MA-2029, a novel motilin receptor antagonist. J Toxicol Sci. 2008 Dec;33(5):631-9. PubMed PMID: 19043284.

6: Sudo H, Yoshida S, Ozaki K, Muramatsu H, Onoma M, Yogo K, Kamei K, Cynshi O, Kuromaru O, Peeters TL, Takanashi H. Oral administration of MA-2029, a novel selective and competitive motilin receptor antagonist, inhibits motilin-induced intestinal contractions and visceral pain in rabbits. Eur J Pharmacol. 2008 Mar 10;581(3):296-305. doi: 10.1016/j.ejphar.2007.11.049. PubMed PMID: 18164286.

7: Mitselos A, Depoortere I, Peeters TL. Delineation of the motilin domain involved in desensitization and internalization of the motilin receptor by using full and partial antagonists. Biochem Pharmacol. 2007 Jan 1;73(1):115-24. PubMed PMID: 17074305.