AG-10 1446711-81-4
- Product Name
- AG-10 1446711-81-4
- CAS No.
- 1446711-81-4
- Chemical Name
- AG-10 1446711-81-4
- Synonyms
- Acoramidis;AG10,AG 10;Acoramidis (AG-10);AG-10 1446711-81-4;AG-10, 10 mM in DMSO;3-(3-(3,5-dimethyl-1H-pyrazol-4-yl)propoxy)-4-fluorobenzoic acid;Benzoic acid, 3-[3-(3,5-dimethyl-1H-pyrazol-4-yl)propoxy]-4-fluoro-
- CBNumber
- CB34694530
- Molecular Formula
- C15H17FN2O3
- Formula Weight
- 292.31
- MOL File
- 1446711-81-4.mol
AG-10 1446711-81-4 Property
- Boiling point:
- 542.5±50.0 °C(Predicted)
- Density
- 1.282±0.06 g/cm3(Predicted)
- solubility
- DMSO: Soluble: =10 mg/ml
Ethanol: Slightly soluble: 0.1-1 mg/ml - pka
- 3.98±0.10(Predicted)
- form
- Solid
- color
- White to off-white
- InChI
- InChI=1S/C15H17FN2O3/c1-9-12(10(2)18-17-9)4-3-7-21-14-8-11(15(19)20)5-6-13(14)16/h5-6,8H,3-4,7H2,1-2H3,(H,17,18)(H,19,20)
- InChIKey
- WBFUHHBPNXWNCC-UHFFFAOYSA-N
- SMILES
- C(O)(=O)C1=CC=C(F)C(OCCCC2=C(C)NN=C2C)=C1
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P321Specific treatment (see … on this label).
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
AG-10 1446711-81-4 Chemical Properties,Usage,Production
Uses
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 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 |
References
[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. DOI:10.1073/pnas.1300761110
[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. DOI:10.1002/cpdd.700
[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. DOI:10.1074/jbc.M305396200
AG-10 1446711-81-4 Preparation Products And Raw materials
Raw materials
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