| Identification | Back Directory | [Name]
Acetamide, N-[3-[[5-chloro-2-[[5-(3-thienyl)-2-pyridinyl]amino]-4-pyrimidinyl]amino]phenyl]- | [CAS]
2825567-97-1 | [Synonyms]
Acetamide, N-[3-[[5-chloro-2-[[5-(3-thienyl)-2-pyridinyl]amino]-4-pyrimidinyl]amino]phenyl]- | [Molecular Formula]
C21H17ClN6OS | [MOL File]
2825567-97-1.mol | [Molecular Weight]
436.92 |
| Chemical Properties | Back Directory | [density ]
1.451±0.06 g/cm3(Predicted) | [storage temp. ]
4°C, away from moisture and light | [form ]
Solid | [pka]
14.70±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
Cathepsin C-IN-5 (compound SF38) is a potent, selective and orally active Cathepsin C inhibitor with IC50s of 59.9 nM, 4.26 µM, >5 µM, >5 µM, >5 µM for Cat C, Cat L, Cat S, Cat B, Cat K, respectively. Cathepsin C-IN-5 inhibits the Cat C activity in bone marrow and blood. Cathepsin C-IN-5 decreases the activation of NSPs (neutrophil serine proteases). Cathepsin C-IN-5 shows anti-inflammatory activity[1]. Cathepsin C-IN-5 (compound SF38) shows inhibition in THP-1 and U937 cells with IC50s of 115.4, 70.2 nM, respectively[1]. Cathepsin C-IN-5 (1500 mg/kg) shows no significant weight loss or toxic reaction within 7 days after the administration in ICR mice[1].
Cathepsin C-IN-5 (10 mg/kg for p.o.; 2 mg/kg for i.v.) shows good bioavailability with F=42.07%[1].
Cathepsin C-IN-5 (2, 10, 50 mg/kg; p.o.) shows effective antiinflammatory activity and potential protective effect in an animal model of ALI[1]. | [Uses]
Cathepsin C-IN-5 (compound SF38) is a potent, selective and orally active Cathepsin C inhibitor with IC50s of 59.9 nM, 4.26 μM, >5 μM, >5 μM, >5 μM for Cat C, Cat L, Cat S, Cat B, Cat K, respectively. Cathepsin C-IN-5 inhibits the Cat C activity in bone marrow and blood. Cathepsin C-IN-5 decreases the activation of NSPs (neutrophil serine proteases). Cathepsin C-IN-5 shows anti-inflammatory activity[1]. | [in vivo]
Cathepsin C-IN-5 (1500 mg/kg) shows no significant weight loss or toxic reaction within 7 days after the administration in ICR mice[1].
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Cathepsin C-IN-5 (10 mg/kg for p.o.; 2 mg/kg for i.v.) shows good bioavailability with F=42.07%[1].
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Cathepsin C-IN-5 (2, 10, 50 mg/kg; p.o.) shows effective antiinflammatory activity and potential protective effect in an animal model of ALI[1]. | Animal Model: | C57BL/6 male mice (acute lung injury (ALI) mice model)[1] | | Dosage: | 2, 10, 50 mg/kg (one hour after administration, received LPS (20 mg/kg)) | | Administration: | P.o. | | Result: | Decreased the levels of proinflammatory cytokines (TNF-a, IL-6, and GM-CSF) and increased the the concentration of the anti-inflammatory cytokine (IL-10) in a dose-dependent manner. |
| [storage]
4°C, away from moisture and light | [References]
[1] Chen X, et al. Non-peptidyl non-covalent cathepsin C inhibitoEEr bearing a unique thiophene-substituted pyridine: Design, structure-activity relationship and anti-inflammatory activity in vivo. Eur J Med Chem. 2022 Jun 5;236:114368. DOI:10.1016/j.ejmech.2022.114368 |
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