非酒精性脂肪性肝病(nonalcoholic fatty liver disease, NAFLD)是目前最常见的慢性肝病之一,指除酒精和其他对肝脏有明确损害因素所引起的,肝脏内脂质过度沉积的疾病,包括单纯性脂肪肝(nonalcoholic fatty liver, NAFL)、非酒精性脂肪性肝炎(nonalcoholic steatohepatitis, NASH)及相关肝硬化。其中,NASH是NAFLD恶化的关键...
NONALCOHOLIC STEATOHEPATITISPATHOGENESISREGULATORResmetirom, a liver-directed, orally active agonist of THR-beta, could play a favorable role in treating NASH... X Wang,L Wang,NYB Geng - 《International Journal of Molecular Sciences》 被引量: 0发表: 2023年 Understanding the Relationship between Non...
佐治亚大学 化学博士 Resmetirom(MGL-3196) | Resmetirom (MGL-3196) is an orally active thyroid hormone receptor-beta (THR-beta) agonist with high specific uptake in liver. Selectivity for THR-beta may provide metabolic benefits of thyroid hormones in managing MASH. ...
T3 nebulization significantly improved PQ-induced pulmonary fibrosis in mice, possibly by activating thyroid hormone receptor beta (THRβ). T3 and sobetirome, a specific THRβ agonist significantly upregulated peroxlsome proliferator-activated receptor-γ coactlvator-1α (PGC1α) expression, and NH...
R&D and commercialization of new drugs in the field of nonalcoholic steatohepatitis (NASH), announces the positive clinical results in overweight and obese subjects for ASC41, a liver-targeted prodrug. The active metabolite of ASC41 is a selective thyroi...
表2:本发明化合物对甲状腺素受体beta的激动活性如下: 结论:本发明化合物能够激活甲状腺激素受体beta下游信号。 测试实施例5:药代动力学评价: 以大鼠为受试动物,测试了大鼠灌胃给予实施例4、实施例9化合物后不同时刻血浆中药物浓度。研究本发明化合物在大鼠体内药物代谢动力学行为,评价其药物代谢特征。每组实施例选用3只...
P2X2[T339S] receptors were 10-fold more sensitive than wild type to exogenous ATP, and alphabeta meATP also increased channel opening. Two conserved ectodomain lysine residues (Lys69 and Lys308) are critical for function and have been proposed to contribute to the ATP binding site of P2X ...
Keywords: Autism Spectrum Disorder, Polymorphism, Resistance to Thyroid Hormone, Thyroid Hormone, Thyroid Hormone Receptor Beta Abstract Thyroid hormone receptor β (THRβ) binds to thyroid hormones to execute various cellular and physiological processes as a ligand-inducible transcriptional factor. THRs, ...
MB-07811 (VK-2809) is an orally active HepDirect prodrug of MB07344 with cholesterol and triglycerides lowering activity. MB-07811 is an agonist of liver-targeted THR-β. 体外活性 MB-07811 has a low affinity for thyroid hormone receptors with a Ki of 14.6 μM for TRβ and a Ki of 12....
Pancreatic Polypeptide, rat is an agonist of NPY receptor, with high affinity at NPYR4. Pancreatic Polypeptide (1 μM) does not alter proliferation in BRIN BD11 or 1.1B4 beta-cells, but reverses the decreased cell viability in BRIN BD11 cells induced by streptozotocin. Pancreatic Polypeptide (...