Basic information Safety Supplier Related

AZD-3161

Basic information Safety Supplier Related

AZD-3161 Basic information

Product Name:
AZD-3161
Synonyms:
  • AZD-3161 (AZD3161)
  • AZD-3161
  • 3-Pyridinecarboxamide, N-[(3S)-3,4-dihydro-5-(5-methoxy-2-pyrazinyl)-2H-1-benzopyran-3-yl]-6-[(2,2,2-trifluoroethoxy)methyl]-
CAS:
1369501-46-1
MF:
C23H21F3N4O4
MW:
474.43
Mol File:
1369501-46-1.mol
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AZD-3161 Chemical Properties

Boiling point:
633.5±55.0 °C(Predicted)
Density 
1.41±0.1 g/cm3(Predicted)
pka
13.08±0.20(Predicted)
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AZD-3161 Usage And Synthesis

Uses

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[1][2].

Definition

ChEBI: Pavinetant is a member of the class of quinolines that is the amide obtained by formal condensation of the carboxy group of 3-[(methanesulfonyl)amino]-2-phenylquinoline-4-carboxylic acid with the amino group of (1S)-1-phenylpropan-1-amine. A neurokinin-3 receptor antagonist that has been trialled as a potential drug for treatment of schizophrenia and menopausal symptoms. It has a role as a neurokinin-3 receptor antagonist and an antipsychotic agent. It is a member of quinolines, a secondary carboxamide, a sulfonamide and an aromatic amide.

in vivo

AZD-3161 (16-99 μmol/kg; p.o.) displays a dose dependent antinociceptive effect in the phase 1 of the formalin model of pain in rats[1].
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].

References

[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. DOI:10.1016/j.bmcl.2012.06.105
[2] Bagal SK, et, al. Recent progress in sodium channel modulators for pain. Bioorg Med Chem Lett. 2014 Aug 15; 24(16): 3690-9. DOI:10.1016/j.bmcl.2014.06.038

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