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Acoramidis hydrochloride

Catalog No. T39740 CAS 2242751-53-5

Synonyms: AG10 hydrochloride, Alxn2060 hydrochloride

Acoramidis hydrochloride (Alxn2060 hydrochloride) is an orally active and selective kinetic stabilizer of WT and V122I- TTR (transthyretin) . Acoramidis hydrochloride is used in the study for transthyretin amyloidosis.

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Acoramidis hydrochloride Chemical Structure

Acoramidis hydrochloride, CAS 2242751-53-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 97.00
5 mg	In stock	$ 247.00
10 mg	In stock	$ 397.00
25 mg	In stock	$ 663.00
50 mg	In stock	$ 945.00
100 mg	In stock	$ 1,280.00
500 mg	In stock	$ 2,570.00
1 mL * 10 mM (in DMSO)	In stock	$ 272.00

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Purity: 99.57%

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Storage & Solubility Information

Description	Acoramidis hydrochloride (Alxn2060 hydrochloride) is an orally active and selective kinetic stabilizer of WT and V122I- TTR (transthyretin) . Acoramidis 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 [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 (IC 50 > 100 μM) and a number of cytochrome P450 isozymes (IC 50 > 50 μM) (low toxicity) [1] . 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	In an animal model using Wistar rats [1], AG10 was administered orally via gavage at a dosage of 50 mg/kg/d for toxicity analysis over a 28-day period. Subsequent results indicated a plasma C max of approximately 40 μM. Histopathological evaluations of the liver, kidney, heart, spleen, thymus, and lung revealed no signs of pathological processes in the AG10-treated subjects.

Synonyms	AG10 hydrochloride, Alxn2060 hydrochloride
Molecular Weight	328.77
Formula	C15H18ClFN2O3
CAS No.	2242751-53-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 58.5 mg/mL (177.9 mM), Sonication is recommended.

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Clinical Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

Acoramidis hydrochloride 2242751-53-5 Others Alxn2060 Hydrochloride AG10 hydrochloride AG-10 Hydrochloride AG10 Hydrochloride Alxn2060 hydrochloride AG 10 Hydrochloride Acoramidis Hydrochloride inhibitor inhibit

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