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编 号:F349272
分子式:C22H24N6O3
分子量:420.46
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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生物活性:
BBS-4 is a potent and selective inducible nitric oxide synthase (NOS2) dimerization inhibitor, with an IC50 of 0.49 nM. BBS-4 can protect mice from the cardiovascular dysfunction of sepsis.

体内研究:
BBS-4 (10 mg/kg; i.p.; 1 h after endotoxin administration) prevents endotoxin-induced hypotension in mice.BBS-4 (30 mg/kg; i.p.; 1 h after endotoxin administration) prevents endotoxin-induced myocardial dysfunction in mice.BBS-4 (10 mg/kg; i.p.; 1 and 8 h after endotoxin administration) prevents endotoxin-induced impairment of murine hypoxic pulmonary vasoconstriction (HPV).BBS-4 (10 mg/kg; i.p.; 1 and 8 h after endotoxin administration) does not affect the endotoxin-induced increase in pulmonary NOS2 gene expression, but it (30 mg/kg) prevents cardiac and pulmonary NOS2 protein dimerization and increases plasma nitrate and nitrite (NOx) concentration in mice.BBS-2 (30 mg/kg; s.c. twice daily for 10 d) does not affect agonist-stimulated NOS3-dependent aortic relaxation ex vivo.BBS-4 (10-30 mg/kg; i.p.) does not improve mortality rate in endotoxemic mice.

体外研究:
BBS-4 exhibits ~300–2000-fold selective for inhibiting iNOS dimerization in cells versus CYP-3A4 (~150 nM in a microsomal benzyloxyresorufin assay; ~1 μM in a cell-based testosterone hydroxylase assay).
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