MGL-3196 free base · Synonyms: Resmetirom
Resmetirom is a highly selective thyroid hormone receptor β agonist.
For research use only. Not for human or veterinary use.
MGL-3196 structure
CAS No.: 920509-32-6
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 2 g | USD 598.00 | BP-02103-2g | In stock | Get quote |
| 5 g | USD 1,198.00 | BP-02103-5g | In stock | Get quote |
| 10 g | USD 1,988.00 | BP-02103-10g | In stock | Get quote |
| 20 g | Inquire | BP-02103-20g | In stock | Inquire |
| 50 g | Inquire | BP-02103-50g | In stock | Inquire |
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Description
Resmetirom (MGL-3196) is a highly selective thyroid hormone receptor β (THR-β) agonist with an EC50 value of 0.21 μM.
Biological activity
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[1].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.
Identifiers
- SMILES
-
CC(C)C1=CC(OC2=C(Cl)C=C(C=C2Cl)N2N=C(C#N)C(=O)NC2=O)=NNC1=O - InChIKey
-
FDBYIYFVSAHJLY-UHFFFAOYSA-N
Specifications
- MW (average)
- 435.2210
- Formula
- C17H12Cl2N6O4
- CAS No.
- 920509-32-6
- Physical state
- Solid
- Color
- White to yellow
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20℃ 2 years; In solvent -20℃ 1 month;
Solubility
Soluble in DMSO
- In vitro
- DMSO : 70 mg/mL