| Identification | Back Directory | [Name]
Methanone, [4-(6-amino-3-pyridazinyl)-1-piperidinyl][5-(4-fluorophenoxy)-4-methoxy-2-pyridinyl]- | [CAS]
2311863-36-0 | [Synonyms]
TRPC6-IN-3
Methanone, [4-(6-amino-3-pyridazinyl)-1-piperidinyl][5-(4-fluorophenoxy)-4-methoxy-2-pyridinyl]- | [Molecular Formula]
C22H22FN5O3 | [MOL File]
2311863-36-0.mol | [Molecular Weight]
423.44 |
| Chemical Properties | Back Directory | [Boiling point ]
689.6±55.0 °C(Predicted) | [density ]
1.325±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
5.26±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
TRPC6-IN-3 (compound 17) is a potent, orally active transient receptor potential C6 ion channel (TRPC6) inhibitor. TRPC6-IN-3 modulates not only intracellular calcium concentration, but also membrane potential by modulating the flux of cations including calcium and sodium ions. TRPC6-IN-3 can be used in research of respiratory system[1]. | [in vivo]
TRPC6-IN-3 (compound 17; 1-10 mg/kg; p.o.; orally 12 h and 2 h before LPS challenge; LPS-induced mice) inhibits LPS-induced vascular leakage and inhibits accumulation of Broncho-Alveolar-Lavage protein (BALF protein) in a mouse model[1].
TRPC6-IN-3 (3 mg/kg; p.o.; daily, for 4 d; H1N1-induced mice) reduces H1N1-induced vascular leakage in a mouse model[1]. | Animal Model: | LPS-induced mice[1] | | Dosage: | 1, 3, and 10 mg/kg | | Administration: | Oral administration; orally 12 h and 2 h before LPS challenge | | Result: | Reduced BALF protein concentration of 56 % at 3 mg/kg and 62 % at 10 mg/kg. |
| Animal Model: | H1N1-induced mice[1] | | Dosage: | 3 mg/kg | | Administration: | Oral administration; daily, for 4 days | | Result: | Inhibited Evans blue extravasation from the blood to the BALF and reduced BALF Evans blue by 24 % at 3 mg/kg. |
| [References]
[1] Thierry B, et, al. Inhibitors of TRPC6 for treating respiratory conditions. WO2021209510. |
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