Acoramidis HCl

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MedKoo CAT#: 125031

CAS#: 2242751-53-5 (HCl)

Description: 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

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

Theoretical Analysis

MedKoo Cat#: 125031
Name: Acoramidis HCl
CAS#: 2242751-53-5 (HCl)
Chemical Formula: C15H18ClFN2O3
Exact Mass: 328.10
Molecular Weight: 328.770
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 not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Related CAS #: 2242751-53-5 (HCl)   1446711-81-4 (free base)  

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:

Biological target:
In vitro activity:
In vivo activity:

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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.