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Acoramidis hydrochloride (Synonyms: AG10 hydrochloride)

Cat. No.: HY-109165A
Handling Instructions

Acoramidis (AG10) hydrochloride is an orally active and selective kinetic stabilizer of WT and V122I-TTR (transthyretin). Acoramidis (AG10) hydrochloride is used in the study for transthyretin amyloidosis.

For research use only. We do not sell to patients.

Acoramidis hydrochloride Chemical Structure

Acoramidis hydrochloride Chemical Structure

CAS No. : 2242751-53-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 330 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
Estimated Time of Arrival: December 31
25 mg USD 950 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Acoramidis (AG10) hydrochloride is an orally active and selective kinetic stabilizer of WT and V122I-TTR (transthyretin). Acoramidis (AG10) hydrochloride is used in the study for transthyretin amyloidosis[1][2].

In Vitro

Acoramidis (AG10, 0.1-10 μM for TTR ∼5 µM) stabilizes V122I- and WT-TTR equally well and also exceeds their efficacy to stabilize WT and mutant TTR in whole serum[1].
Acoramidis (AG10) stimulates the mitochondrial QO2 in a concentration-dependent manner between 10 and 100 μM[3].
Acoramidis (AG10) has very minimal inhibition of two common off-targets in drug discovery, the potassium ion channel hERG (IC50 > 100 µM) and a number of cytochrome P450 isozymes (IC50 > 50 µM) (low toxicity)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1].

Cell Line: Human serum (TTR ∼5 µM).
Concentration: 0.1 and 10 μM.
Incubation Time: 72 h.
Result: Was significantly more effective than tafamidis in stabilizing TTR.
The concentration of AG10 to 10 µM resulted in stabilization of almost all of TTR in serum.
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
Molecular Weight

328.77

Formula

C₁₅H₁₈ClFN₂O₃

CAS No.

2242751-53-5

SMILES

O=C(O)C1=CC=C(F)C(OCCCC2=C(C)NN=C2C)=C1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (190.10 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0416 mL 15.2082 mL 30.4164 mL
5 mM 0.6083 mL 3.0416 mL 6.0833 mL
10 mM 0.3042 mL 1.5208 mL 3.0416 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (6.33 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (6.33 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.33 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

AcoramidisAG10AG 10AG-10OthersInhibitorinhibitorinhibit

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Product Name:
Acoramidis hydrochloride
Cat. No.:
HY-109165A
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