MA-2029 | CAS#287206-61-5 | Motilin Receptor Antagonist |MedKoo

MedKoo Cat#: 532174 | Name: MA-2029

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Description:

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

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

Chemical Structure

MA-2029

CAS#287206-61-5

Theoretical Analysis

MedKoo Cat#: 532174

Name: MA-2029

CAS#: 287206-61-5

Chemical Formula: C31H46ClFN4O4

Exact Mass: 592.3192

Molecular Weight: 593.18

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 350.00	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

Product Data

Instruction

View handling instruction

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/

	Solvent	mg/mL	mM
Solubility
	DMSO	43.3	73.05

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.

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:

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.

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.