Prucalopride succinate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Prucalopride succinate (R-108512) 是一种有效的选择性 5-HT4 受体激动剂。

Prucalopride succinate (R-108512) is a potent, selective 5-HT4 receptor agonist with pKi of 8.6 and 8.1 for 5-HT4a and 5-HT4b, >290-fold higher affinity for 5-HT4 receptors than for other receptors; targets the impaired motility associated with chronic constipation, thus normalizing bowel movements; induces contractions (pEC50=7.48) in the guinea-pig colon, demonstrates anti-cholinergic, anticholinesterase or nonspecific inhibitory activity and does not antagonise 5-HT2A, 5-HT2B and 5-HT3 receptors or motilin, CCK1 receptors.

Cell Proliferation Assay Cell Line:A549 cells Concentration:10 μM Incubation Time:24, 48, 72 h Result:Repressed lung cancer cells proliferation.

Animal Model:Diabetes mellitus (DM) rat modelsDosage:5 μg/kg, 10 μg/kg Administration:Oral gavage, single daily for 2 weeks.Result:Accelerated colonic movement and shortened the colonic transit time, and markedly increased the expression levels of Ki67 .Increased expression of SOX10 in the columnar epithelial nuclei and enteraden (when at 5 μg/kg), and in the columnar epithelial cells, the nuclei of lamina propria cells and enteraden (when at 10 μg/kg). Significantly increased Nestin expression, which concentrated in columnar epithelial cells and the mesenchyme. (Nestin:a marker of enteric neural stem cells in the ENS).

R-108512 | R108512

Endocrinology/Hormones

5-HT Receptor

5-HT4A |5-HT4B

Other Indications

——

179474-85-2

485.9584

C22H32ClN3O7

>98% (HPLC)

DMSO: ≥ 36 mg/mL

COCCCN1CCC(CC1)NC(=O)C2=CC(=C(C3=C2OCC3)N)Cl.C(CC(=O)O)C(=O)O

Butanedioic acid, compd. with 4-amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl)-4-piperidinyl]-7-benzofurancarboxamide (1:1)

(-20℃)

With Ice Pack

≥ 2 years