MA-2029

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 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

MA-2029 用途与合成方法

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.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/04/30HY-107642MA-2029
MA-2029
287206-61-51mg1600元
2024/04/30HY-107642MA-2029
MA-2029
287206-61-55mg5000元

MA-2029 上下游产品信息

"MA-2029"相关产品信息
主页 | 企业会员服务 | 广告业务 | 联系我们 | 旧版入口 | 中文MSDS | CAS Index | 常用化学品CAS列表 | 化工产品目录 | 新产品列表 | 评选活动 | HS海关编码 | MSDS查询 | 化工站点

Copyright © 2016-2023 ChemicalBook 版权所有  京ICP备07040585号  京公海网安备11010802032676号  

互联网增值电信业务经营许可证:京ICP证150597号  互联网药品信息服务资格证编号(京)-非经营性-2015-0073  信息系统安全等级保护备案证明(三级)  营业执照公示

根据相关法律法规和本站规定,单位或个人购买相关危险物品应取得有效的资质、资格条件。
参考《应急管理部等多部门关于加强互联网销售危险化学品安全管理的通知 (应急〔2022〕119号)》《互联网危险物品信息发布管理规定》