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Chemical Structure : MA-2029
CAS No.: 287206-61-5
Catalog No.: PC-22029Not For Human Use, Lab Use Only.
MA-2029 (MA2029) is a potent, selective and competitive motilin receptor antagonist with pA2 value of 9.17, displas [125I]motilin with IC50 of 2.74 nM.
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MA-2029 (MA2029) is a potent, selective and competitive motilin receptor antagonist with pA2 value of 9.17, displas [125I]motilin with IC50 of 2.74 nM.
MA-2029 (1 µM) has no effects on resting tone or spontaneous contractions and no significant effect on the contractile response to acetylcholine or substance P.
MA-2029 also displaces [125I] motilin bound to cell membranes of HEK 293 cells expressing human motilin receptors with IC50 and pKi values of 4.9 nM and 8.39, respectively.
MA-2029 shows either very low or no affinity for any of the 24 receptors and 7 ion channels.
MA-2029 (3 to 30 mg/kg, oral) dose-dependently inhibited colonic contractions induced by motilin (3 μg/kg, i.v.) in conscious rabbits.
MA-2029 (0.3 to 3 mg/kg) also inhibited abdominal muscle contractions (an index of the visceral pain) induced by intravenous infusion of motilin (3 μg/kg/h) during colorectal distension in conscious rabbits.
| M.Wt | 538.73 | |
| Formula | C31H46N4O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(S)-N-[(S)-2-(3-tert-Butyl-4-hydroxy-phenyl)-1-ethylcarbamoyl-ethyl]-3-methyl-2-[methyl-((S)-2-methylamino-3-phenyl-propionyl)-amino]-butyramide |
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1. Sudo H, et al. Eur J Pharmacol. 2008 Mar 10;581(3):296-305.
2. Ozaki K, et al. Eur J Pharmacol. 2009 Aug 1;615(1-3):185-92.
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