287206-61-5
基本信息
4-Fluoro-N-methyl-L-phenylalanyl-N-methyl-L-valyl-3-(1,1-dimethylethyl)-N-ethyl-L-tyrosinamide
物理化学性质
| 沸点 | 765.1±60.0 °C(Predicted) |
| 密度 | 1.128±0.06 g/cm3(Predicted) |
| 储存条件 | -20°C储存 |
| 溶解度 | Soluble to 20 mM in 1eq. HCl and to 100 mM in DMSO |
| 酸度系数(pKa) | 11.24±0.20(Predicted) |
| 形态 | 粉末 |
| 颜色 | White to off-white |
MA-2029价格(试剂级)
| 报价日期 | 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 |
| 2023/03/20 | HY-107642 | MA-2029 MA-2029 | 287206-61-5 | 10mg | 9800元 |
常见问题列表
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. |