MA-2029

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

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.


Price and Availability

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MA-2029 is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

No image available

Theoretical Analysis

MedKoo Cat#: 532174
Name: MA-2029
CAS#: 287206-61-5
Chemical Formula: C31H46ClFN4O4
Exact Mass:
Molecular Weight: 593.1814
Elemental Analysis: C, 62.77; H, 7.82; Cl, 5.98; F, 3.20; N, 9.45; O, 10.79


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


Technical Data

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).

Harmonized System Code:
293490


References

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.