Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Prucalopride (R-93877) is a selective, high-affinity 5-HT4A/4B receptor agonist (Ki: 2.5/8 nM). It has >290-fold selectivity for 5-HT4A/4B receptor than other 5-HT receptor subtypes.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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サンプルについてお問い合わせ | |||||
5 mg | 在庫あり | ¥ 7,500 | |||
10 mg | 在庫あり | ¥ 12,000 | |||
25 mg | 在庫あり | ¥ 16,000 | |||
50 mg | 在庫あり | ¥ 18,500 | |||
100 mg | 在庫あり | ¥ 32,500 | |||
200 mg | お問い合わせ | ¥ 45,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 11,500 |
説明 | Prucalopride (R-93877) is a selective, high-affinity 5-HT4A/4B receptor agonist (Ki: 2.5/8 nM). It has >290-fold selectivity for 5-HT4A/4B receptor than other 5-HT receptor subtypes. |
ターゲット&IC50 | 5-HT4B:8 nM(Ki), 5-HT4A:2.5 nM(Ki) |
In vitro | Administration of prucalopride at dosages of 2/4 mg resulted in complete spontaneous bowel movements per week at rates of 30.9% and 28.4%, respectively, compared to 12.0% in the placebo group. Patients treated with 2 mg of prucalopride (47.3%) and those receiving 4 mg (46.6%) experienced an increase in the frequency of spontaneous bowel movements, with an average of one or more complete bowel movements per week, versus 25.8% in the placebo group. Prucalopride (2/4 mg) significantly enhanced other secondary efficacy endpoints, including patient satisfaction with their bowel functions and treatment, as well as their perception of the severity of constipation symptoms. At a dosage of 4 mg/day, prucalopride accelerated overall gastric emptying and small intestinal transit without causing intestinal evacuation disorders. It also sped up overall colonic transit and increased the colonic emptying rate. |
In vivo | Prucalopride (1 mM) significantly amplifies the rebound contraction of the guinea pig's proximal colon following electrical stimulation. It induces contractions in a concentration-dependent manner (pEC50: 7.5). Additionally, Prucalopride induces relaxation in the muscularis mucosae of the rat esophagus (pEC50: 7.8), demonstrating a monophasic concentration-response curve. |
別名 | R-93877 |
分子量 | 367.87 |
分子式 | C18H26ClN3O3 |
CAS No. | 179474-81-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 36 mg/mL (97.9 mM)
DMSO: 56 mg/mL (152.2 mM)
You can also refer to dose conversion for different animals. 詳細
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Prucalopride 179474-81-8 GPCR/G Protein Neuroscience 5-HT Receptor R-93877 Serotonin Receptor A549 5-hydroxytryptamine Receptor chronic constipation pseudo-intestinal obstruction inhibit R 93877 A427 Inhibitor R93877 Lung cancer inhibitor