Description
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.
Product information
CAS Number: 1369501-46-1
Molecular Weight: 474.43
Formula: C23H21F3N4O4
Chemical Name: N-[(3S)-5-(5-methoxypyrazin-2-yl)-3,4-dihydro-2H-1-benzopyran-3-yl]-6-[(2,2,2-trifluoroethoxy)methyl]pyridine-3-carboxamide
Smiles: COC1=CN=C(C=N1)C1C=CC=C2OC[C@H](CC=12)NC(=O)C1C=NC(COCC(F)(F)F)=CC=1
InChiKey: LRHQXIQLHVPUNA-INIZCTEOSA-N
InChi: InChI=1S/C23H21F3N4O4/c1-32-21-10-28-19(9-29-21)17-3-2-4-20-18(17)7-16(12-34-20)30-22(31)14-5-6-15(27-8-14)11-33-13-23(24,25)26/h2-6,8-10,16H,7,11-13H2,1H3,(H,30,31)/t16-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. AZD-3161 inhibits Adenosine Transporter (AT) and Cannabinoid B1 (CB1) receptor, with IC50s of 1.8 μM and 5 μM, respectively.
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. AZD-3161 (3 μmol/kg; i.v.) exhibits long half-life (2.2 h) and Vss (4.2 L/kg). AZD-3161 (10 μmol/kg; p.o.) exhibits high oral bioavailability (44%), long half-life (4.8 h) and Cmax (0.30 μmol/L).
Products are for research use only. Not for human use.
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