产品
编 号：F306206
分子式：C31H45FN4O4
分子量：556.71
分子式：C31H45FN4O4
分子量：556.71
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 287206-61-5
产品详情
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.
体内研究：
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 t1/2 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 t1/2 is 2 hours.
体外研究：
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.
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.
体内研究：
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 t1/2 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 t1/2 is 2 hours.
体外研究：
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.
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