| Identification | Back Directory | [Name]
1,5-Naphthyridin-3-amine, 6-[3-(5-chloro-2,4-difluorophenyl)-1H-pyrazol-4-yl]-N-[2-[4-(1-methylethyl)-1-piperazinyl]ethyl]- | [CAS]
2442519-59-5 | [Synonyms]
THRX-144644
1,5-Naphthyridin-3-amine, 6-[3-(5-chloro-2,4-difluorophenyl)-1H-pyrazol-4-yl]-N-[2-[4-(1-methylethyl)-1-piperazinyl]ethyl]- | [Molecular Formula]
C26H28ClF2N7 | [MOL File]
2442519-59-5.mol | [Molecular Weight]
512 |
| Chemical Properties | Back Directory | [Boiling point ]
679.6±55.0 °C(Predicted) | [density ]
1.329±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
9.75±0.50(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
THRX-144644 is a Lung-restricted ALK5 inhibitor with an IC50 value of 0.14 nM. THRX-144644 avoids systemic toxicities associated with TGFβ pathway inhibition[1]. | [in vivo]
THRX-144644 (2-60 mg/kg; Inhalation: nebulizer, daily, for 14 days) is a Lung-selective inhibitor and targets to the lungs in Sprague Dawley rats[1]. | Animal Model: | Sprague Dawley rats[1] | | Dosage: | 2, 10, and 60 mg/kg | | Administration: | Inhalation: nebulizer, daily, for 14 days | | Result: | Had the L:P ratio (AUC) was 0.44.
Had lung-to-plasma ratios ranged from 100- to 1200-fold in rats across dose level.
Had lung trough (24 h) concentrations in rats ranged from 3- to 17-fold above the PCLS IC50 across tolerated doses.
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| [IC 50]
ALK5: 0.14 nM (IC50) | [References]
[1] Maher JM, et, al. Lung-restricted ALK5 inhibition avoids systemic toxicities associated with TGFβ pathway inhibition. Toxicol Appl Pharmacol. 2022 Mar 1;438:115905. DOI:10.1016/j.taap.2022.115905 |
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