1. GPCR/G Protein
  2. Motilin Receptor
  3. MA-2029

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。

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MA-2029 Chemical Structure

MA-2029 Chemical Structure

CAS No. : 287206-61-5

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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MA-2029 is a selective, orally active, and competitive motilin receptor antagonist (IC50=4.9 nM). MA-2029 is selective for the motilin receptor over various other receptors and ion channels. MA-2029 may be useful for gastrointestinal disorders associated with disturbed gastrointestinal motility[1].

IC50 & Target

IC50: 4.9 nM (motilin receptor)[1]

体外研究
(In Vitro)

MA-2029 (1 to 30 nM) competitively inhibits motilin-induced contractions in isolated rabbit duodenal longitudinal muscle strips, with a pA2 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 [125I]motilin to motilin receptors in a homogenate of rabbit colon smooth muscle tissue and membranes of HEK 293 cells expressing human motilin receptors. The pKi of MA-2029 is 8.58±0.04 in the rabbit colon homogenate and 8.39 in the HEK 293 cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

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[1].
MA-2029 (10 mg/kg; p.o.) treatment shows that the t1/2 is 2 hours[1].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Japanese-white rabbits (about 2-3 kg)[1]
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)[1]
Dosage: 10 mg/kg
Administration: Oral administration (Pharmacokinetic Analysis)
Result: The t1/2 is 2 hours.
分子量

556.71

Formula

C31H45FN4O4

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
纯度 & 产品资料
参考文献

MA-2029 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
MA-2029
目录号:
HY-107642
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