MA-2029
| 中文名称 | MA-2029 |
|---|---|
| 中文同义词 | 化合物 T15946 |
| 英文名称 | MA 2029 |
| 英文同义词 | MA 2029;4-Fluoro-N-methyl-L-phenylalanyl-N-methyl-L-valyl-3-(1,1-dimethylethyl)-N-ethyl-L-tyrosinamide;MA 2029,MA2029;L-Tyrosinamide, 4-fluoro-N-methyl-L-phenylalanyl-N-methyl-L-valyl-3-(1,1-dimethylethyl)-N-ethyl- |
| CAS号 | 287206-61-5 |
| 分子式 | C31H45FN4O4 |
| 分子量 | 556.71 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 287206-61-5.mol |
| 结构式 |  |
MA-2029 性质
| 沸点 | 765.1±60.0 °C(Predicted) |
|---|---|
| 密度 | 1.128±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 1eq 中可溶解至 20 mM。 HCl 和 DMSO 中浓度为 100 mM |
| 形态 | 粉末 |
| 酸度系数(pKa) | 11.24±0.20(Predicted) |
| 颜色 | 白色至米白色 |
IC50: 4.9 nM (motilin receptor)
MA-2029 (1 to 30 nM) competitively inhibits motilin-induced contractions in isolated rabbit duodenal longitudinal muscle strips, with a pA 2 value of 9.17±0.01. Contractile responses to acetylcholine and substance P are unaffected even at 1 μM of MA-2029. MA-2029 concentration-dependently inhibits the binding of [ 125 I]motilin to motilin receptors in a homogenate of rabbit colon smooth muscle tissue and membranes of HEK 293 cells expressing human motilin receptors. The pK i of MA-2029 is 8.58±0.04 in the rabbit colon homogenate and 8.39 in the HEK 293 cells.
MA-2029 (0.3-3 mg/kg; p.o.) dose-dependently inhibits the number of abdominal muscle contractions induced under the same conditions and causes significant inhibition at 3 mg/kg.
MA-2029 (10 mg/kg; p.o.) treatment shows that the t
1/2
is 2 hours.
The inhibition is significant at 30 min after administration of 3 mg/kg or more and at 4 h after administration of 10 mg/kg or more (MA-2029), so administration of 10 mg/kg or more causes inhibitory effects from 30 min or less to at least 4 h after administration.
| Animal Model: | Male Japanese-white rabbits (about 2-3 kg) |
| Dosage: | 0.3, 1, 3 mg/kg |
| Administration: | Oral administration |
| Result: | Dose-dependently inhibited the number of abdominal muscle contractions induced under the same conditions. Caused significant inhibition at 3 mg/kg. |
| Animal Model: | Male Japanese-white rabbits (about 2-3 kg) |
| Dosage: | 10 mg/kg |
| Administration: | Oral administration (Pharmacokinetic Analysis) |
| Result: | The t 1/2 is 2 hours. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-107642 | MA-2029 MA-2029 | 287206-61-5 | 1mg | 1600元 |
| 2024/04/30 | HY-107642 | MA-2029 MA-2029 | 287206-61-5 | 5mg | 5000元 |