AZD-3161
AZD-3161 is a potent and selective blocker of NaV1.7 channel, with a pIC50 of 7.1. AZD-3161 can be used for the research of neuropathic and inflammatory pain.
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- CAS No.: 1369501-46-1
- Formule: C23H21F3N4O4
- Masse moléculaire:474.43
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
pIC50: 7.1 (NaV1.7 channel)[1]
In Vitro
AZD-3161 (compound 29) is selective for NaV1.7 over NaV1.5 and hERG, with pIC50s of 7.1, 4.9 and 4.9, respectively[1].
AZD-3161 inhibits Adenosine Transporter (AT) and Cannabinoid B1 (CB1) receptor, with IC50s of 1.8 μM and 5 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AZD-3161 (3 μmol/kg; i.v.) exhibits long half-life (2.2 h) and Vss (4.2 L/kg)[1].
AZD-3161 (10 μmol/kg; p.o.) exhibits high oral bioavailability (44%), long half-life (4.8 h) and Cmax (0.30 μmol/L)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1369501-46-1
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Masse moléculaire 474.43
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Formule C23H21F3N4O4
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SMILES
O=C(C1=CC=C(COCC(F)(F)F)N=C1)N[C@@H]2COC3=CC=CC(C4=NC=C(OC)N=C4)=C3C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Kers I, et, al. Structure and activity relationship in the (S)-N-chroman-3-ylcarboxamide series of voltage-gated sodium channel blockers. Bioorg Med Chem Lett. 2012 Sep 1; 22(17): 5618-24. [Content Brief]
[2]. Bagal SK, et, al. Recent progress in sodium channel modulators for pain. Bioorg Med Chem Lett. 2014 Aug 15; 24(16): 3690-9. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AZD-3161 Related Classifications
HY-117714 Related Classifications
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