TTR stabilizer-2
TTR stabilizer-2 is an orally active and blood-brain barrier-penetrant TTR stabilizer. TTR stabilizer-2 binds to the thyroxine-binding pocket, stabilizes the TTR tetramer, and reduces subunit exchange and tetramer dissociation. TTR stabilizer-2 has an EC50 of 17.7 nM against human TTR and a Kd value of 4.8 nM against human TTR. TTR stabilizer-2 shows weak inhibition of human PDE4D. TTR stabilizer-2 can be used in research on nervous system-related diseases, such as ATTR amyloidosis.
For research use only. We do not sell to patients.
- Formula: C17H24N4O2
- Molecular Weight:316.40
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
PDE4D |
In Vitro
TTR stabilizer-2 stabilizes WT, V30M, and V122I TTR tetramers in human plasma and buffer, and completely inhibits subunit exchange at 5 µM and above[1].
TTR stabilizer-2 weakly inhibits human PDE 4D3 with an IC50 >161 µM[1].
The CLint,app of TTR stabilizer-2 in cryopreserved human hepatocytes is 22.1 µL/min/106 cells[1].
TTR stabilizer-2 (10 µM; 240 min) forms the N-glucuronide metabolite (M2) and the N-depyrazole metabolite (M4) in human hepatocytes[1].
TTR stabilizer-2 exhibits high permeability in RRCK cells, with a Papp (AB) of 40.6 × 10-6 cm/s[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | AUC0-∞ | CLplasma | Vdss | T1/2 | Cmax | Tmax | F |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 1.0 mg/kg | i.v. | 26000 ng·h/mL | 0.65 mL/min/kg | 0.27 L/kg | 6.3 h | / | / | / |
| Rat[1] | 3.0 mg/kg | p.o. | 17600 ng·h/mL | / | / | 4.3 h | 1800 ng/mL | 0.17 h | 23 % |
| Dog[1] | 1.0 mg/kg | i.v. | 8120 ng·h/mL | 2.05 mL/min/kg | 0.92 L/kg | 6.5 h | / | / | / |
| Dog[1] | 3.0 mg/kg | p.o. | 7390 ng·h/mL | / | / | 7.3 h | 1190 ng/mL | 0.375 h | 30 % |
Chemical Information
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Molecular Weight 316.40
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Formula C17H24N4O2
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SMILES
COC1=CC=NC(OC)=C1C2CCN(C3=C(C)NN=C3C)CC2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TTR stabilizer-2 Related Classifications
HY-190900 Related Classifications
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