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AG-10 (Acoramidis) is an orally active and selective kinetic stabilizer of TTR (transthyretin). AG-10 exhibits activity for WT and V122I-TTR. AG-10 is used in the study of transthyretin amyloidosis.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $100 | In Stock | |
5 mg | $247 | In Stock | |
10 mg | $396 | In Stock | |
25 mg | $787 | In Stock | |
50 mg | $1,180 | In Stock | |
100 mg | $1,860 | In Stock | |
1 mL x 10 mM (in DMSO) | $419 | In Stock |
Description | AG-10 (Acoramidis) is an orally active and selective kinetic stabilizer of TTR (transthyretin). AG-10 exhibits activity for WT and V122I-TTR. AG-10 is used in the study of transthyretin amyloidosis. |
In vitro | AG-10 (0.1-10 μM for TTR ∼5 µM) stabilizes WT- and V122I-TTR equally well and also exceeds their efficacy to stabilize WT and mutant TTR in whole serum. AG-10 exhibits minimal inhibition of two common off-targets in drug discovery, the potassium ion channel hERG (IC50 > 100 µM) and a number of cytochrome P450 isozymes (IC50 > 50 µM) (low toxicity)[1]. AG-10 (10-100 μM) stimulates the mitochondrial QO2 in a concentration-dependent manner[2]. |
In vivo | AG-10 (Oral gavage; 50 mg/kg/d; daily for 28 d) exhibited the plasma Cmax of ∼40 µM and histopathological evaluation of liver, thymus, kidney, spleen, heart, and lung showed no signs of pathologic processes in the AG10-treated Wistar rats[1]. |
Alias | Acoramidis |
Molecular Weight | 292.31 |
Formula | C15H17FN2O3 |
Cas No. | 1446711-81-4 |
Smiles | O(CCCC=1C(C)=NNC1C)C2=CC(C(O)=O)=CC=C2F |
Relative Density. | 1.282 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 4.8 mg/mL (16.42 mM) | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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