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Acoramidis (Synonyms: AG10)

Cat. No.: HY-109165
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Acoramidis (AG10) is an orally active and selective kinetic stabilizer of WT and V122I-TTR (transthyretin). Acoramidis (AG10) is used in the study for transthyretin amyloidosis.

For research use only. We do not sell to patients.

Acoramidis Chemical Structure

Acoramidis Chemical Structure

CAS No. : 1446711-81-4

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Description

Acoramidis (AG10) is an orally active and selective kinetic stabilizer of WT and V122I-TTR (transthyretin). Acoramidis (AG10) is used in the study for transthyretin amyloidosis[1][2].

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[1].
Acoramidis (AG10) stimulates the mitochondrial QO2 in a concentration-dependent manner between 10 and 100 μM[3].
Acoramidis (AG10) has very 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1].

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[1].
Dosage: 50 mg/kg/d (Toxicity Analysis).
Administration: Oral gavage, daily for 28 d.
Result: Showed the plasma Cmax 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
Molecular Weight

292.31

Formula

C₁₅H₁₇FN₂O₃

CAS No.

1446711-81-4

SMILES

O=C(O)C1=CC=C(F)C(OCCCC2=C(C)NN=C2C)=C1

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

AcoramidisAG10AG 10AG-10OthersInhibitorinhibitorinhibit

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Acoramidis
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