Acoramidis (AG10) hydrochloride is an orally active and selective kinetic stabilizer of WT and V122I- TTR (transthyretin). Acoramidis (AG10) hydrochloride is used in the study for transthyretin amyloidosis.In VitroAcoramidis (AG10, 0.1-10 μM for TTR ∼5 µM) stabilizes V122I- and WT-TTR equally well and also exceeds their efficacy to stabilize WT and mutant TTR in whole serum. Acoramidis (AG10) stimulates the mitochondrial QO2 in a concentration-dependent manner between 10 and 100 μM. Acoramidis (AG10) has very minimal inhibition of two common off-targets in drug discovery, the potassium ion channel hERG (IC 50 > 100 µM) and a number of cytochrome P450 isozymes (IC 50 > 50 µM) (low toxicity). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot Analysis. Cell Line: Human serum (TTR ∼5 µM). Concentration: 0.1 and 10 μM. Incubation Time: 72 h. Result: Was significantly more effective than tafamidis in stabilizing TTR. The concentration of AG10 to 10 µM resulted in stabilization of almost all of TTR in serum.In VivoAnimal Model: Wistar rats . Dosage: 50 mg/kg/d (Toxicity Analysis). Administration: Oral gavage, daily for 28 d. Result: Showed the plasma C max of ∼40 µM and histopathological evaluation of liver, kidney, heart, spleen, thymus, and lung showed no signs of pathologic processes in the AG10-treated animalsForm:Solid. Specification: 0.98 Molecular Formula: C15H18ClFN2O3 Molecular Weight: 328.77 PubChem CID: 135307127 Isomeric SMILES: CC1=C(C(=NN1)C)CCCOC2=C(C=CC(=C2)C(=O)O)F.Cl
- UPC:
- 12142207
- Condition:
- New
- Availability:
- 8-12 weeks
- Weight:
- 1.06 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- A646727-10mg
- CAS:
- 2242751-53-5
- Product Size:
- 10mg
