A TTR kinetic stabilizer
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Alternative(s)
41522Acoramidis
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Acoramidis (hydrochloride)

Item No. 41536

Technical Information
Formal Name
3-[3-(3,5-dimethyl-1H-pyrazol-4-yl)propoxy]-4-fluoro-benzoic acid, monohydrochloride
CAS Number
2242751-53-5
Synonyms
  • AG-10
Molecular Formula
C15H17FN2O3• HCl
Formula Weight
Purity
≥98%
A solid
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=C(C1=CC=C(C(OCCCC2=C(C)NN=C2C)=C1)F)O.Cl
InChi Code
InChI=1S/C15H17FN2O3.ClH/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);1H
InChi Key
MGFZEARHINUOMX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    Acoramidis is a kinetic stabilizer of transthyretin (TTR).1 It selectively binds to wild-type TTR and TTRV122I with negative cooperativity (Kd1s = 4.8 and 6.2 nM, respectively; Kd2s = 314 and 139 nM, respectively) over COX-1, COX-2, and the thyroid hormone nuclear receptor (IC50s = >10 µM for all). Acoramidis inhibits pH-induced amyloidogenesis of wild-type TTR and TTRV122I, indicating tetramer stabilization, when used at stoichiometric ratios of 1:1 and 1:0.5 with the number of TTR binding sites. It stabilizes TTRV122I in serum isolated from patients with familial amyloid cardiomyopathy when used at a concentration of 10 µM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Penchala, S.C., Connelly, S., Wang, Y., et alAG10 inhibits amyloidogenesis and cellular toxicity of the familial amyloid cardiomyopathy-associated V122I transthyretin. Proc. Natl. Acad. Sci. USA 110(24), 9992-9997 (2013).