Acoramidis hydrochloride_product_DataBase

Bioactivity	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[1][2].
Invitro	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]. Western Blot Analysis[1]. Cell Line:
In Vivo	Animal Model:
Name	Acoramidis hydrochloride
CAS	2242751-53-5
Formula	C15H18ClFN2O3
Molar Mass	328.77
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	-20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[1]. Sravan C Penchala, et al. AG10 inhibits amyloidogenesis and cellular toxicity of the familial amyloid cardiomyopathy-associated V122I transthyretin. Proc Natl Acad Sci U S A. 2013 Jun 11;110(24):9992-7. [2]. Jonathan C Fox, et al. First-in-Human Study of AG10, a Novel, Oral, Specific, Selective, and Potent Transthyretin Stabilizer for the Treatment of Transthyretin Amyloidosis: A Phase 1 Safety, Tolerability, Pharmacokinetic, and Pharmacodynamic Study in Healthy Adult Volunteers. Clin Pharmacol Drug Dev. 2020 Jan;9(1):115-129. [3]. Stephen P Soltoff, et al. Evidence that tyrphostins AG10 and AG18 are mitochondrial uncouplers that alter phosphorylation-dependent cell signaling. J Biol Chem. 2004 Mar 19;279(12):10910-8.

PeptideDB

Acoramidis hydrochloride

CAS: 2242751-53-5 F: C15H18ClFN2O3 W: 328.77