2. GPCR/G Protein
  3. Motilin Receptor
  4. 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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规格 价格 是否有货 数量
1 mg ￥1600
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5 mg ￥5000
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50 mg   询价  

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MA-2029 相关抗体

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 至 30 nM) 竞争性抑制离体兔十二指肠纵向肌条中胃动素诱导的收缩，pA2 值为 9.17±0.01。即使在 1 μM 的 MA-2029 下，对乙酰胆碱和 P 物质的收缩反应也不受影响。MA-2029 浓度依赖性地抑制[125I]胃动素与兔结肠平滑肌组织和表达人胃动素受体的 HEK 293 细胞膜匀浆中的胃动素受体的结合。MA-2029 在兔结肠匀浆中的 pKi 为 8.58±0.04，在 HEK 293 细胞中为 8.39[1]。

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

MA-2029 相关抗体:
体内研究
(In Vivo)

MA-2029 (0.3-3 mg/kg；口服) 剂量依赖性地抑制在相同条件下诱发的腹肌收缩次数，并在 3 mg/kg 时引起显著抑制[1]。
MA-2029 (10 mg/kg；口服) 处理显示 t1/2 为 2 小时[1]。
3 mg/kg 或以上给药后 30 分钟和 10 mg/kg 或以上（MA-2029）给药后 4 小时抑制显著，因此 10 mg/kg 或以上给药会在给药后 30 分钟或更短时间内至至少 4 小时内引起抑制作用[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

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

MA-2029287206-61-5MA2029MA 2029Motilin ReceptorMLNRcontractionsgastrointestinalmotilityvisceralHEK 293cellsirritablebowelsyndromepKiselectiveInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-107642
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