1. Neuronal Signaling
  2. Transthyretin (TTR)
  3. Transthyretin-IN-3

Transthyretin-IN-3 (compound 6) is a designed benzofuran analogue. Transthyretin-IN-3 selectively binds to plasma transthyretin (TTR) to inhibit Amyloid aggregation (IC50=5.0±0.2 μM). Transthyretin-IN-3 can bind to TTR's thyroxine binding site specifically by carrying chlorine substituents at specific locations in its structure. This binding can prevent TTR tetramers from dissociating into unstable monomers.

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Transthyretin-IN-3 Chemical Structure

Transthyretin-IN-3 Chemical Structure

CAS No. : 3008535-20-1

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Description

Transthyretin-IN-3 (compound 6) is a designed benzofuran analogue. Transthyretin-IN-3 selectively binds to plasma transthyretin (TTR) to inhibit Amyloid aggregation (IC50=5.0±0.2 μM). Transthyretin-IN-3 can bind to TTR's thyroxine binding site specifically by carrying chlorine substituents at specific locations in its structure. This binding can prevent TTR tetramers from dissociating into unstable monomers[1].

In Vivo

Transthyretin-IN-3 ( 0.1 mg/kg, iv; 0.1 mg/kg, po; 8 h) had an oral bioavailability (BA) of 66.8%, comparable to the current therapeutic drug Tafamidis (HY-14852) in SD rats[1].
Pharmacokinetic Analysis in SD rats[1]

Route Dose (mg/kg) C0/max (ng/mL) CLtot (mL/h/kg) Vdss (mL/kg) AUC0_8 (ng•h/mL) BA (%)
i.v. 0.1 1718 20.6 112 3726 /
p.o. 0.1 395 / / 2524 67.7

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

Molecular Weight

552.53

Formula

C17H11ClI2O3

CAS No.
SMILES

O=C(C1=C(CC)OC2=CC=CC(Cl)=C12)C3=CC(I)=C(O)C(I)=C3

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

Purity & Documentation
References
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Transthyretin-IN-3 Related Classifications

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Transthyretin-IN-3
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HY-161505
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