리나클로타이드

한글명:리나클로타이드

카스 번호851199-59-2

상품명:Linaclotide

CBNumberCB82498818

분자식C59H79N15O21S6

포뮬러 무게1526.74

MOL 파일851199-59-2.mol

동의어(한글)

리나클로타이드

화학적 성질

녹는점	231-235°C (dec.)
끓는 점	2045.0±65.0 °C(Predicted)
밀도	1.60
저장 조건	Hygroscopic, Refrigerator, under inert atmosphere
용해도	DMSO(약간, 가열), 메탄올((약간, 가열)), 물(약간, 가열)에 용해됨
산도 계수 (pKa)	3.05±0.10(Predicted)
물리적 상태	고체
물리적 상태	단단한 모양
색상	하얀색
안정성	흡습성
InChIKey	KXGCNMMJRFDFNR-VRMHCMCOSA-N

위험 및 안전 성명

유해 물질 데이터

851199-59-2(Hazardous Substances Data)

NFPA 704:

	0
3		0

그림문자(GHS)

리나클로타이드 화학적 특성, 용도, 생산

개요
In August 2012, the US FDA approved linaclotide (also referred to as MD-1100), a first-in-class, orally administered 14-amino acid peptide as a therapy for patients suffering from chronic idiopathic constipation (CIC) and irritable bowel syndrome with constipation (IBS-C). Linaclotide and its active metabolite MM-419447, which results from the cleavage of the C-terminal tyrosine residue by carboxypeptidase A, mimic the actions of the endogenous intestinal peptides guanylin (15 amino acids) and uroguanylin (16 amino acids) by activating guanylyl cyclase C (GC-C) on the intestinal epithelium. Activation of GC-C leads to increased intra- and extracellular levels of cGMP and activation of the CFTR ion channel, resulting in increased levels of HCO₃^-, Cl^-, and water in the intestinal lumen and accelerated gastrointestinal transit. Based on an in vitro assaymeasuring the accumulation of cGMP in T84 cell exposed to an agonist, the EC₅₀ of linaclotide at pH 7.0 was 99±17.5 nM. In preclinical studies in mice using the transit of activated charcoal as ameasure of efficacy, linaclotide at 100 μg/kg significantly accelerated transit compared to wild-type mice treated with charcoal only or GC-Cnullmice treatedwith and without linaclotide.118 Efficacy was also seen in rats treatedwith linaclotide atdoses of 5, 10, and 20 μg/kg. Linaclotide has been synthesized using conventional solid-phase peptide technology.
용도
Linaclotide is a guanylate cyclase-C agonist currently being studied in Phase 3 trials for the treatment of irritable bowel syndrome with constipation.
Biological Functions
Linaclotide works by increasing fluid in your intestines and helping speed up movement of food through the gut. Linaclotide may improve stool texture and lessen symptoms such as bloating, abdominal pain/discomfort, straining, and feelings of incomplete bowel movements.
부작용
Side effects include:Diarrhea, abdominal pain, flatulence, abdominal distension, viral gastroenteritis, headache, upper respiratory tract infection, sinusitis

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