Ro 24-7429
Names
[ CAS No. ]:
139339-45-0
[ Name ]:
Ro 24-7429
[Synonym ]:
Ro 24-7429
Aids003055
[7-Chloro-5-(1H-Pyrrol-2-Yl)-3H-1,4-Benzodiazepin-2-Yl]-Methyl-Amine
Aids-003055
Biological Activity
[Description]:
Ro24-7429 is a potent and orally active HIV-1 transactivator protein Tat antagonist. Ro24-7429 is also a runt-related transcription factor 1 (RUNX1) inhibitor. Ro24-7429 has anti-HIV, antifibrotic and anti-inflammatory effects[1][2].
[Related Catalog]:
[In Vitro]
Ro 24-7429 (0.1-5 μM; 3 days) induces apoptosis of cultured PBMCs in a dose-dependent manner[1]. Ro 24-7429 (1-25 μM) also induces apoptosis and inhibits antigen-induced lymphocyte proliferation[1]. Ro24-7429 (50-200 μM; 24-72 hours) strongly inhibits the proliferation of A549 and HLF cells in a dose-dependent manner. Ro24-7429 treatment (75 μM) significantly reduces TNF-α-induced up-regulation of RUNX1 mRNA by 50% at 48 hours[2]. Apoptosis Analysis[1] Cell Line: Peripheral blood mononuclear cells (PBMCs) Concentration: 0.1 μM, 1 μM, 5 μM Incubation Time: 3 days Result: Induced a dose-dependent increase in apoptosis of cultured PBMCs.
[In Vivo]
Ro24-7429 (17.5-70 mg/kg; i.p.; daily; for 14 or 21 days) treatment robustly ameliorates lung fibrosis and inflammation in the Bleomycin-induced pulmonary fibrosis (PF) mouse model. Ro24-7429 curbs expression of fibrosis markers in injured mouse lungs[2]. Animal Model: C57BL/6J male and female mice (aged 6 to 8 weeks) induced by Bleomycin[2] Dosage: 17.5 mg/kg, 35 mg/kg, and 70 mg/kg Administration: i.p.; daily; for 14 or 21 days Result: Ameliorated lung fibrosis and inflammation in the Bleomycin-induced PF mouse model.
[References]
Chemical & Physical Properties
[ Density]:
1.36g/cm3
[ Boiling Point ]:
514.6°C(760mmHg),计算值
[ Molecular Formula ]:
C14H13ClN4
[ Molecular Weight ]:
272.73300
[ Flash Point ]:
265°C
[ Exact Mass ]:
272.08300
[ PSA ]:
52.54000
[ LogP ]:
2.03060