눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.
NFPA 704
0
2
0
오베티콜산 C화학적 특성, 용도, 생산
개요
Obeticholic acid is a potent
and selective farnesoid X receptor agonist that promotes the
flow of bile in the liver. The drug was approved by the
USFDA for the treatment of the rare chronic liver disease
primary biliary cholangitis (PBC) in combination with
ursodeoxycholic acid (UDCA) in adults with inadequate
response to UDCA or as a single agent therapy in adults
unable to tolerate UDCA. Obeticholic acid was discovered at
the Università de Perugia and developed by Intercept
Pharmaceuticals. Obeticholic acid has also been granted orphan
drug designation for the treatment of primary sclerosing
cholangitis and primary biliary cirrhosis and has received
breakthrough therapy designation for the treatment of patients
with nonalcohol steatohepatitis (NASH) with liver fibrosis.
용도
6-Ethylchenodeoxycholic Acid is a derivative of the bile acid Chenodeoxycholic Acid (C291900). 6-Ethylchenodeoxycholic Acid is a potent activator of the farnesoid X nuclear receptor which reduces liver fat and fibrosis in animal models of fatty liver disease.
정의
ChEBI: A dihydroxy-5beta-cholanic acid that is chenodeoxycholic acid carrying an additional ethyl substituent at the 6alpha-position. A semi-synthetic bile acid which acts as a farnesoid X receptor agonist and is used for treatme
t of primary biliary cholangitis.
효소 저해제
This semisynthetic bile acid analogue (FW = 420.63 g/mol; CAS 459789- 99-2), also named INT-747, 6α-ethyl-chenodeoxycholate, and (3α,5β,6α, 7α)-6-ethyl-3,7-dihydroxycholan-24-oic acid, is an analogue of the naturally occurring bile acid (FW = 392.57 g/mol; CAS 474-25-9). The latter is synthesized in the liver, where it conjugated to form taurochenodeoxycholate and glycol-chenodeoxycholate, reducing its pKa and increasing retention in the gastrointestinal tract, until reabsorption by the ileum. Chenodeoxycholate is the most active physiological ligand known for the farnesoid X receptor, or FXR (encoded by the NR1H4 gene in humans) that translocates to the nucleus, dimerizes, and binds to hormone response elements. Obeticholic acid reduces bacterial translocation and invasion in cirrhotic rats by restoring intestinal barrier integrity (through increased expression of tight junction proteins) and by inhibiting inflammation. Obeticholate likewise up-regulated expression of the FXR-associated gene small heterodimer partner (SHP).