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 Vitro Acoramidis (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 Vivo Animal 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 animals Form:Solid
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Acoramidis hydrochloride
CAS number：2242751-53-5 molecular formula：C15H18ClFN2O3
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| Chinese alias | 盐酸阿考拉米迪斯 | ||
| English alias | Acoramidis hydrochloride [USAN] | UNII-VY9C88C2NV | Acoramidis (hydrochloride) | Alxn2060 hydrochloride | Alxn-2060 hydrochloride | AKOS040757458 | AG10 hydrochloride | AG-10 hydrochloride | 3-(3-(3,5-Dimethyl-1H-pyrazol-4-yl)propoxy)-4-fluorobenzoic acid | ||
| CAS number | 2242751-53-5 | molecular formula | C15H18ClFN2O3 |
| molecular weight | 328.77 g/mol | Exact mass | ≥98% |
| PSA | 75.200 Ų | logp | - |
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