MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Linaclotide

CAS No. : 851199-59-2

MCE 站：Linaclotide

产品活性：Linaclotide 是一种有效和选择性的鸟苷酸环化酶 C (guanylate cyclase C) 激动剂；开发用于研究便秘型肠易激综合症 (IBS-C) 和慢性便秘。

研究领域：GPCR/G Protein

作用靶点：Guanylate Cyclase

In Vitro: Linaclotide inhibits in vitro [¹²⁵I]-STa binding to intestinal mucosal membranes from wt mice in a concentration-dependent manner. In contrast, [¹²⁵I]-STa binding to these membranes from GC-C null mice is significantly decreased. After incubation in vitro in jejunal fluid for 30 min, linaclotide is completely degraded. Linaclotide acts on guanylate cyclase-C receptors on the luminal membrane to increase chloride ａnd bicarbonate secretions into the intestine ａnd inhibit the absorption of sodium ions, thus increasing the secretion of water into the lumen ａnd improving defecation; the drug is minimally absorbed into the systemic circulation.

In Vivo: Pharmacokinetic analysis shows very low oral bioavailability (0.10%). In intestinal secretion ａnd transit models, linaclotide exhibits significant pharmacological effects in wt, but not in GC-C null mice: induction of increased fluid secretion into surgically ligated jejunal loops is accompanied by the secretion of elevated levels of cyclic guanosine-3＇,5-monophosphate ａnd accelerated gastrointestinal transit. Linaclotide significantly increases weekly spontaneous bowel movements ａnd complete spontaneous bowel movements (CSBMs) while reducing abdominal pain in patients with chronic constipation.

相关产品：Covalent Screening Library Plus  |  Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  FDA-Approved Drug Library  |  Peptidomimetic Library  |  Drug Repurposing Compound Library  |  Covalent Screening Library  |  Macrocyclic Compound Library  |  Orally Active Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Vericiguat  |  Lificiguat  |  Methylene Blue  |  Riociguat  |  Cinaciguat  |  BAY 41-2272  |  NS-2028  |  Nelociguat  |  ODQ  |  Praliciguat  |  Olinciguat  |  Plecanatide  |  Guanylin(human) TFA  |  Guanylate cyclase-IN-1  |  (Rac)-BI 703704  |  (Rac)-MGV354  |  Ataciguat  |  BAY 41-8543  |  BAY 60-2770  |  MM 419447  |  (4-Acetamidocyclohexyl) nitrate  |  Runcaciguat

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。