MedKoo Cat#: 125031 | Name: Acoramidis HCl

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Acoramidis, also known as AG-10. is novel, potent, highly selective, orally bioavailable transthyretin (TTR) stabilizer with potential disease-modifying activity. AG-10 inhibits amyloidogenesis and cellular toxicity of the familial amyloid cardiomyopathy-associated V122I transthyretin. AG10 has been shown to stabilize Transthyretin (TTR or TBPA) --- a transport protein in serum and cerebrospinal fluid that carries the thyroid hormone thyroxine (T4) and retinol-binding protein bound to retinol --- in Symptomatic Transthyretin Amyloid Cardiomyopathy. In this way, AG10 mimics a naturally occurring genetic variant, T119M, that protects from Transthyretin Amyloidosis.

Chemical Structure

Acoramidis HCl
CAS#2242751-53-5 (HCl)

Theoretical Analysis

MedKoo Cat#: 125031

Name: Acoramidis HCl

CAS#: 2242751-53-5 (HCl)

Chemical Formula: C15H18ClFN2O3

Exact Mass: 328.1000

Molecular Weight: 328.77

Elemental Analysis: C, 54.80; H, 5.52; Cl, 10.78; F, 5.78; N, 8.52; O, 14.60

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Synonym
Acoramidis hydrochloride; AG10; AG-10; AG 10;
IUPAC/Chemical Name
3-(3-(3,5-dimethyl-1H-pyrazol-4-yl)propoxy)-4-fluorobenzoic acid hydrochloride
InChi Key
MGFZEARHINUOMX-UHFFFAOYSA-N
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
SMILES Code
Cl.CC1=C(CCCOC2=CC(=CC=C2F)C(O)=O)C(C)=NN1
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 328.77 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Judge DP, Falk RH, Maurer MS, Shah SJ, Witteles RM, Grogan M, Selby VN, Jacoby D, Hanna M, Nativi-Nicolau J, Patel J, Rao S, Sinha U, Turtle CW, Fox JC, Heitner SB. Transthyretin Stabilization by AG10 in Symptomatic Transthyretin Amyloid Cardiomyopathy. J Am Coll Cardiol. 2019 Mar 12. pii: S0735-1097(19)33920-8. doi: 10.1016/j.jacc.2019.03.012. [Epub ahead of print] PubMed PMID: 30885685. 2: Miller M, Pal A, Albusairi W, Joo H, Pappas B, Haque Tuhin MT, Liang D, Jampala R, Liu F, Khan J, Faaij M, Park M, Chan W, Graef I, Zamboni R, Kumar N, Fox J, Sinha U, Alhamadsheh M. Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. J Med Chem. 2018 Sep 13;61(17):7862-7876. doi: 10.1021/acs.jmedchem.8b00817. Epub 2018 Aug 22. PubMed PMID: 30133284; PubMed Central PMCID: PMC6276790. 3: Petty JT, Sergev OO, Ganguly M, Rankine IJ, Chevrier DM, Zhang P. A Segregated, Partially Oxidized, and Compact Ag10 Cluster within an Encapsulating DNA Host. J Am Chem Soc. 2016 Mar 16;138(10):3469-77. doi: 10.1021/jacs.5b13124. Epub 2016 Mar 7. PubMed PMID: 26924556; PubMed Central PMCID: PMC6118400. 4: Penchala SC, Connelly S, Wang Y, Park MS, Zhao L, Baranczak A, Rappley I, Vogel H, Liedtke M, Witteles RM, Powers ET, Reixach N, Chan WK, Wilson IA, Kelly JW, Graef IA, Alhamadsheh MM. 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. Epub 2013 May 28. PubMed PMID: 23716704; PubMed Central PMCID: PMC3683741. 5: Avlonitis N, Chalmers S, McDougall C, Stanton-Humphreys MN, Brown CT, McCarron JG, Conway SJ. Caged AG10: new tools for spatially predefined mitochondrial uncoupling. Mol Biosyst. 2009 May;5(5):450-7. doi: 10.1039/b820415m. Epub 2009 Mar 31. PubMed PMID: 19381360. 6: Soltoff SP. 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. Epub 2003 Dec 19. PubMed PMID: 14688271.