Structure of Resmetirom
CAS No.: 920509-32-6
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
MGL-3196 is a selective thyroid hormone receptor β agonist with EC50s of 0.21 and 3.74 µM for TRβ and TRα respectively.
Synonyms: MGL-3196; VIA-3196
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CAS No. : | 920509-32-6 |
Formula : | C17H12Cl2N6O4 |
M.W : | 435.22 |
SMILES Code : | N#CC1=NN(C2=CC(Cl)=C(OC(C=C3C(C)C)=NNC3=O)C(Cl)=C2)C(NC1=O)=O |
Synonyms : |
MGL-3196; VIA-3196
|
MDL No. : | MFCD26142653 |
InChI Key : | FDBYIYFVSAHJLY-UHFFFAOYSA-N |
Pubchem ID : | 15981237 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
HepG2 cells | 0.1 µM | 16 hours | Validate the effects of glucocorticoids and thyroid hormone on ACBP/DBI expression. Results showed that glucocorticoids induced ACBP/DBI release, while T3 downregulated ACBP/DBI mRNA levels. | PMC11659162 |
HEK-1B1 cells | 600 nM | 24 hours | To compare the induction of TH target genes by MGL-3196 and T3, finding stronger induction of KLF9 and PCK1 in TRβ-overexpressing cells. | PMC9691000 |
HEK293 cells | 10 nM–100 µM | 24 hours | To assess MGL-3196 action in HEK-1B1 and HEK-1B3 cells, finding OATP1B1 as the primary transporter for MGL-3196. | PMC9691000 |
HEK-1B1 cells | 6 µM | 48 hours | To measure the oxygen consumption rate, finding that MGL-3196 increases basal respiration, maximal respiration, ATP production, and proton leak, functionally mimicking T3. | PMC9691000 |
NCTC 1469 cells | 100 μM | 48 hours | To test the preventive effect of resmetirom on NASH cell model, results showed that resmetirom effectively eliminated lipid accumulation and decreased triglyceride (TG) levels. | PMC10058113 |
HepG2 cells | 100 μM | 48 hours | To test the preventive effect of resmetirom on NASH cell model, results showed that resmetirom effectively eliminated lipid accumulation and decreased triglyceride (TG) levels. | PMC10058113 |
H4 human neuroglioma cells | 5 µM | 6 or 24 hours | Evaluate the impact of 710 distinct agonists and antagonists of neurotransmitter and hormone receptors on ACBP/DBI expression. Results showed that glucocorticoids (e.g., hydrocortisone and dexamethasone) reduced ACBP/DBI expression, while thyroid hormone (T3) downregulated ACBP/DBI mRNA levels. | PMC11659162 |
Huh7 cells | 46.0 μM | overnight | To evaluate the effect of Resmetirom alone or in combination with ACCi on fatty acid oxidation. Res alone induced FAO 1.6-fold, and in combination with ACCi, the Emax of Res increased by 158%. | PMC9426400 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
C57BL/6J mice | Cushing’s syndrome model | Oral | 0.033 mg/ml | 5 weeks | Evaluate the effects of Resmetirom on metabolic symptoms of Cushing’s syndrome. Results showed that Resmetirom reduced ACBP/DBI mRNA levels in liver and adipose tissue and reversed corticosterone-induced metabolic abnormalities such as increased appetite, weight gain, adiposity, and insulin resistance. | PMC11659162 |
Rats | High-fat diet-induced dyslipidemic rat model | Oral | 1 mg/kg and 3 mg/kg | Once daily for 1 week | To evaluate the effect of Resmetirom alone or in combination with ACCi on liver TG and circulating TG. Res dose-dependently reduced liver TG (83% and 88%) and mitigated ACCi-induced hypertriglyceridemia. | PMC9426400 |
C57BL/6J mice | NASH Mice model | Oral | 3 mg/kg and 5 mg/kg | Daily administration for 48 days | To test the therapeutic effect of resmetirom on NASH Mice model, results showed that resmetirom significantly improved liver pathological features, reduced lipid accumulation and fibrosis, and inhibited the activation of STAT3 and NF-κB signaling pathways. | PMC10058113 |
C57BL/6 mice | High-fat diet-induced NAFLD model | Oral administration in drinking water | 9.35 mg/kg or 2.8 mg/kg | 2 or 3 weeks | To investigate the effect of TG68 on fatty liver accumulation and liver injury in mice fed a high-fat diet. Results showed that TG68 treatment led to a reduction in liver weight, hepatic steatosis, serum transaminases, and circulating triglycerides. | PMC8657920 |
Clinical Trial:
NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
NCT04951219 | Non-Alcoholic Fatty Liver Dise... More >>ase Less << | PHASE3 | RECRUITING | 2025-04-26 | Central Research Associates, B... More >>irmingham, Alabama, 35205, United States|Arizona Liver Health - Chandler, Chandler, Arizona, 85224, United States|East Valley Family Physicians, Chandler, Arizona, 85224, United States|The Institute For Liver Health - Glendale, Glendale, Arizona, 85306, United States|The Institute For Liver Health - Tucson, Tucson, Arizona, 85711, United States|Adobe Gastroenterology, Tucson, Arizona, 85712, United States|Arkansas Gastroenterology, North Little Rock, Arkansas, 72117, United States|Fresno Clinical Research Center, Fresno, California, 93720, United States|National Research Institute - Huntington Park, Huntington Park, California, 90255, United States|Ruane Clinical Research Group, Los Angeles, California, 90036, United States|Cedars-Sinai Medical Center, Los Angeles, California, 90048, United States|National Research Institute - Los Angeles, Los Angeles, California, 90057, United States|Catalina Research Institute, Montclair, California, 91763, United States|National Research Institute - Panorama City, Panorama City, California, 91402, United States|San Fernando Valley Health Institute, West Hills, California, 91307, United States|South Denver Gastroenterology - Swedish Medical Center Office, Englewood, Colorado, 80113, United States|Excel Medical Clinical Trials, Boca Raton, Florida, 33434, United States|Covenant Research, Fort Myers, Florida, 33912, United States|Velocity Clinical Research, Hallandale Beach (MD Clinical), Hallandale Beach, Florida, 33009, United States|Floridian Clinical Research, Hialeah, Florida, 33016, United States|Nature Coast Clinical Research - Inverness, Inverness, Florida, 34452, United States|Jacksonville Center for Clinical Research, Jacksonville, Florida, 32216, United States|Florida Research Institute, Lakewood Ranch, Florida, 34211, United States|Miami Dade Medical Research Institute, Miami, Florida, 33176, United States|Orlando Research Center, Orlando, Florida, 32806, United States|Progressive Medical Research, Port Orange, Florida, 32127, United States|Covenant Research, Sarasota, Florida, 34240, United States|The Villages Research Center, The Villages, Florida, 32162, United States|Gastrointestinal Specialists of Georgia, Marietta, Georgia, 30060, United States|East-West Medical Research Institute, Honolulu, Hawaii, 96814, United States|Chicago Research Center, Chicago, Illinois, 60602, United States|Northwestern Memorial Physicians Group, Chicago, Illinois, 60611, United States|Iowa Diabetes Research, West Des Moines, Iowa, 50265, United States|Kansas Medical Clinic - Gastroenterology, Topeka, Kansas, 66606, United States|L-MARC Research Center, Louisville, Kentucky, 40213, United States|Digestive Health Center of Louisiana, Baton Rouge, Louisiana, 70809, United States|Tandem Clinical Research - New Orleans Area Site, Marrero, Louisiana, 70072, United States|Clinical Trials of America, West Monroe, Louisiana, 71291, United States|Gastrointestinal Associates & Endoscopy Center - Flowood, Flowood, Mississippi, 39232, United States|Southern Therapy and Advanced Research, Jackson, Mississippi, 39216, United States|Kansas City Research Institute, Kansas City, Missouri, 64131, United States|Henderson Research Center, Henderson, Nevada, 89052, United States|Clarity Clinical Research, East Syracuse, New York, 13057, United States|Mount Sinai Health System, New York, New York, 10029, United States|Duke University Medical Center, Durham, North Carolina, 27710, United States|Cumberland Research Associates, Fayetteville, North Carolina, 28304, United States|Diabetes and Endocrinology Consultants, Morehead City, North Carolina, 28557, United States|Platinum - Sterling Research Group - Springdale, Cincinnati, Ohio, 45246, United States|Aventiv Research Columbus, Columbus, Ohio, 43213, United States|Awasty Research Network, Marion, Ohio, 43302, United States|Premier Medical Group - Clarksville - Dunlop Lane, Clarksville, Tennessee, 37040, United States|Gastro One - Germantown Office - Wolf Park Drive, Germantown, Tennessee, 38138, United States|Pinnacle Clinical Research - Austin, Austin, Texas, 78746, United States|The Liver Institute At Methodist Dallas, Dallas, Texas, 75203, United States|Dallas Research Center, Dallas, Texas, 75234, United States|Liver Center of Texas, Dallas, Texas, 75234, United States|South Texas Research Institute, Edinburg, Texas, 78539, United States|Texas Digestive Disease Consultants, Fort Worth, Texas, 76104, United States|Liver Associates of Texas, Houston, Texas, 77030, United States|Doctor's Hospital at Renaissance, McAllen, Texas, 78504, United States|Plano Research Center, Plano, Texas, 75093, United States|Texas Liver Institute/American Research Corporation, San Antonio, Texas, 78215, United States|Pinnacle Clinical Research - San Antonio, San Antonio, Texas, 78229, United States|San Antonio Research Center, San Antonio, Texas, 78229, United States|Texas Digestive Disease Consultants - San Marcos, San Marcos, Texas, 78666, United States|Impact Research Institute, Waco, Texas, 76710, United States|Texas Digestive Disease Consultants - Bay Area Houston Endoscopy Center, Webster, Texas, 77598, United States|Wasatch Peak Family Practice, Layton, Utah, 84041, United States|Salt Lake City Research Center, Murray, Utah, 84123, United States|Bon Secours Liver Institute of Richmond, Richmond, Virginia, 23226, United States|National Clinical Research - Richmond, Richmond, Virginia, 23294, United States|Virginia Commonwealth University School of Medicine, Richmond, Virginia, 23298, United States|Liver Institute Northwest, Seattle, Washington, 98105, United States|Fundacion de Investigacion de Diego, San Juan, Puerto Rico Less << |
Tags: Resmetirom | MGL-3196 | VIA-3196 | MGL3196 | MGL 3196 | VIA3196 | VIA 3196 | VIA-3196 | Thyroid Hormone Receptor | THR | 920509-32-6
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P304 + P341 | IF INHALED: If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing. |
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H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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