MA-2029
|
|
|
- CAS号:
- 287206-61-5
- 英文名:
- MA 2029
- 英文别名:
- MA 2029;MA 2029,MA2029;4-Fluoro-N-methyl-L-phenylalanyl-N-methyl-L-valyl-3-(1,1-dimethylethyl)-N-ethyl-L-tyrosinamide;L-Tyrosinamide, 4-fluoro-N-methyl-L-phenylalanyl-N-methyl-L-valyl-3-(1,1-dimethylethyl)-N-ethyl-
- 中文名:
- MA-2029
- 中文别名:
- 化合物 T15946
- CBNumber:
- CB94731552
- 分子式:
- C31H45FN4O4
- 分子量:
- 556.71
- MOL File:
- 287206-61-5.mol
|
|
|
MA-2029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:
-
Store at -20°C
-
|
-
溶解度:
-
Soluble to 20 mM in 1eq. HCl and to 100 mM in DMSO
-
|
-
形态:
-
Powder
-
|
-
酸度系数(pKa):
-
11.24±0.20(Predicted)
-
|
MA-2029性质、用途与生产工艺
MA-2029 是一种选择性、口服活性和竞争性的胃动素受体 (motilin receptor) 拮抗剂 (IC50=4.9 nM)。MA-2029 对胃动素受体的选择性高于其他受体和离子通道。MA-2029 可用于与胃肠动力紊乱相关的胃肠道疾病。
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.
|
MA-2029
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 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 |
287206-61-5, MA-2029 相关搜索:
- C31H45FN4O4
- 化合物 T15946
- 287206-61-5
- L-Tyrosinamide, 4-fluoro-N-methyl-L-phenylalanyl-N-methyl-L-valyl-3-(1,1-dimethylethyl)-N-ethyl-
- MA 2029,MA2029
- 4-Fluoro-N-methyl-L-phenylalanyl-N-methyl-L-valyl-3-(1,1-dimethylethyl)-N-ethyl-L-tyrosinamide
- MA 2029