MA-2029 | Motilin receptor antagonist | Probechem Biochemicals

Chemical Structure : MA-2029

CAS No.: 287206-61-5

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MA-2029 (MA2029)

货号: PC-22029Not For Human Use, Lab Use Only.

MA-2029 (MA2029) is a potent, selective and competitive motilin receptor (GPR38) antagonist with pA2 value of 9.17, displays [125I]motilin with IC50 of 2.74 nM.

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生物&药学活性

MA-2029 (MA2029) is a potent, selective and competitive motilin receptor (GPR38) antagonist with pA2 value of 9.17, displays [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.

物理化学性质&存储条件

分子量	538.73
分子式	C31H46N4O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
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

参考文献

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.

MA-2029 (MA2029)

生物&药学活性

物理化学性质&存储条件

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MA-2029 (MA2029)

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物理化学性质&存储条件

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