SML3971

A1899

≥97% (HPLC)

• Synonym(s): A 1899, A-1899, N-[(2,4-Difluorophenyl)methyl]-2′-[[[2-(4-methoxyphenyl)acetyl]amino]methyl][1,1′-biphenyl]-2-carboxamide, S 20951, S-20951, S20951
• Empirical Formula (Hill Notation): C₃₀H₂₆F₂N₂O₃
• CAS Number: 498577-46-1
• Molecular Weight: 500.54
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD06407754
• Assay: ≥97% (HPLC)
• Form: powder

Properties

• Quality Segment: 100
• assay: ≥97% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: -10 to -25°C

Description

Biochem/physiol Actions

Potent and selective TASK-1 potassium channel blocker that induces lasting respiratory alkalosis and stimulates breathing in anesthetized rats.




A1899 is a highly potent and selective non-voltage-dependent two-pore domain potassium channel K 2P 3.1 blocker (TASK-1, KCNK3, IC50 = 7 nM in CHO cells) with 10-fold selectivity over TASK-3 and much reduced or little potency towards TASK-2/4 (>8 µM in Xenopus oocytes) and other potassium channels. A1899 specifically blocks TASK-1 currents by 74% in Xenopus oocytes at 100 nM via an open-channel block mechanism. A1899 induces lasting respiratory alkalosis and stimulates breathing in anesthetized rats in vivo (5-25 mg/kg, i.v.). Also mitigates the endothelin-1 induced prolonged action potential duration in cardiomyocytes (at 200 nM).

Safety Information

• Storage Class: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable