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Chemical Structure : AG10
Catalog No.: PC-49857Not For Human Use, Lab Use Only.
AG10 is a potent and selective kinetic stabilizer and ligand of transthyretin (TTR) ligand with apparent binding constant (Kapp) of 193 nM for WT-TTR.
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AG10 is a potent and selective kinetic stabilizer and ligand of transthyretin (TTR) ligand with apparent binding constant (Kapp) of 193 nM for WT-TTR.
AG10 binds TTR with negative cooperativity (Kd1 = 4.8 nM, Kd2 = 314 nM), V122I-TTR with Kd1 of 6.2 ± 2.0 nM and a Kd2 of 139 ± 80 nM.
AG10 is a highly effective and selective stabilizer of WT and V122I-TTR.
AG10 also prevents the dissociation of V122I-TTR in serum obtained from patients with FAC and protects human cardiomyocytes from TTR amyloid toxicity very effectively.
AG10 binds V122I-TTR with high affinity and to kinetically stabilize the tetramer, G10 is significantly better than tafamidis in inhibiting the amyloidogenesis of WT and V122I-TTR.
AG10 prevents dissociation of V122I-TTR in serum samples obtained from patients with familial amyloid cardiomyopathy.
AG10 stabilizes V122I- and WT-TTR equally well and also exceeds their efficacy to stabilize WT and mutant TTR in whole serum.
| M.Wt | 292.31 | |
| Formula | C15H17FN2O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Sravan C Penchala, et al. Proc Natl Acad Sci U S A. 2013 Jun 11;110(24):9992-7.
2. Sravan C Penchala , et al. Nat Chem Biol. 2015 Oct;11(10):793-8.
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