产品说明书

Acoramidis HCl

Print
Chemical Structure| 2242751-53-5 同义名 : AG10 hydrochloride;Acoramidis hydrochloride
CAS号 : 2242751-53-5
货号 : A1544116
分子式 : C15H18ClFN2O3
纯度 : 99%+
分子量 : 328.766
MDL号 : -
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(182.5 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Acoramidis HCl is an orally active, selective kinetic stabiliser of wild-type and V122I mutant TTR (transthyretin).Acoramidis HCl is used in the study of transthyretin amyloidosis[1][2].Acoramidis HCl stabilises V122I-TTR and WT-TTR reasonably well at concentrations of 0.1-10 µM (TTR ∼5 µM), and is also effective in stabilising wild-type and mutant TTRs in whole serum[1].Acoramidis HCl stimulates mitochondrial QO2 in a concentration-dependent manner at concentrations ranging from 10 to 100 µM[3].Acoramidis HCl showed minimal inhibition of two common non-targets in drug discovery, the potassium channel hERG (IC50 > 100 µM) and multiple cytochrome P450 isozymes (IC50 > 50 µM) (low toxicity)[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.04mL

0.61mL

0.30mL

15.21mL

3.04mL

1.52mL

30.42mL

6.08mL

3.04mL
参考文献

[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.