MGL-3196

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

MGL-3196 (VIA-3196, Resmetirom) 是一种有效且高度选择性的 THR-β（甲状腺激素受体 β）激动剂，EC50 为 0.21 uM

MGL-3196 (VIA-3196, Resmetirom) is a potent and highly selective agonist of THR-β (Thyroid Hormone Receptor β) with EC50 of 0.21 uM; shows 28-fold selectivity for THR-β over THR-α in a functional assay; exhibits an excellent safety profile and orally bioactive.Steatohepatitis,Phase 2 Clinical(In Vitro):Resmetirom (MGL-3196) is 28-fold selective for THR-β (EC50=0.21 μM) over THR-α (EC50=3.74 μM ) in a functional assay. Resmetirom (MGL-3196) shows an IC20 of roughly 30 μM for blockage of the hERG channel. The IC50 for CYP3A4/5 and for CYP2C19 is >50 μM, and there is only weak inhibition (roughly 22 μM) of CYP2C9.(In Vivo):Resmetirom (MGL-3196) exhibits good exposures and reasonable oral bioavailability in rats. The volume of distribution and clearance are both low. Dose proportional increases in exposure are observed for a suspension of Resmetirom (MGL-3196) given orally to DIO mice.In animals treated with Resmetirom (MGL-3196) there is a reduction in cholesterol and in liver size, which is secondary to reduction of liver TG. There is no effect on bone mineral density (BMD) or heart or kidney size in Resmetirom (MGL-3196) treated animals.

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Resmetirom | VIA-3196 | MGL3196 | MGL 3196 | VIA3196 | VIA 3196

Endocrinology/Hormones

THR

THR-β

Other Indications

Steatohepatitis

920509-32-6

435.221

C17H12Cl2N6O4

>98% (HPLC)

DMSO: ≥ 31 mg/mL

N#CC1=NN(C2=CC(Cl)=C(OC(C=C3C(C)C)=NNC3=O)C(Cl)=C2)C(NC1=O)=O

1,2,4-Triazine-6-carbonitrile, 2-[3,5-dichloro-4-[[1,6-dihydro-5-(1-methylethyl)-6-oxo-3-pyridazinyl]oxy]phenyl]-2,3,4,5-tetrahydro-3,5-dioxo-

(-20℃)

With Ice Pack

≥ 2 years