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BBS-4

CAS No. : 402934-09-2

MCE 站：BBS-4

产品活性：BBS-4 是一种有效的、选择性诱导型一氧化氮合酶 (NOS2) 二聚抑制剂，IC₅₀ 值为 0.49 nM。BBS-4 可以保护小鼠免受败血症的心血管功能障碍的影响。

研究领域：Immunology/Inflammation

作用靶点：NO Synthase

In Vitro: 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).

In Vivo: 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.

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