BBS-4
目录号 : GC27160BBS-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。
Cas No.:402934-09-2
Sample solution is provided at 25 µL, 10mM.
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[1].
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)[2].
Glpbio has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo, BBS-4 (10 mg/kg; i.p.; 1 h after endotoxin administration) prevents endotoxin-induced hypotension in mice[1].
BBS-4 (30 mg/kg; i.p.; 1 h after endotoxin administration) prevents endotoxin-induced myocardial dysfunction in mice[1].
BBS-4 (10 mg/kg; i.p.; 1 and 8 h after endotoxin administration) prevents endotoxin-induced impairment of murine hypoxic pulmonary vasoconstriction (HPV)[[1].
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[1].
BBS-2 (30 mg/kg; s.c. twice daily for 10 d) does not affect agonist-stimulated NOS3-dependent aortic relaxation ex vivo[1].
BBS-4 (10-30 mg/kg; i.p.) does not improve mortality rate in endotoxemic mice[1].
Glpbio has not independently confirmed the accuracy of these methods. They are for reference only.
References:
[1]. Ichinose F, et, al. A selective inducible NOS dimerization inhibitor prevents systemic, cardiac, and pulmonary hemodynamic dysfunction in endotoxemic mice. Am J Physiol Heart Circ Physiol. 2003 Dec; 285(6): H2524-30.
[2]. https://pubmed.ncbi.nlm.nih.gov/12907425/
Cas No. | 402934-09-2 | SDF | |
Canonical SMILES | O=C([C@@H]1N(C2=NC(N3C=CN=C3)=NC(C)=C2)CCC1)NCCC4=CC=C(OCO5)C5=C4 | ||
分子式 | C22H24N6O3 | 分子量 | 420.46 |
溶解度 | DMSO : 100 mg/mL (237.83 mM; Need ultrasonic) | 储存条件 | -20°C |
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1 mg | 5 mg | 10 mg |
1 mM | 2.3783 mL | 11.8917 mL | 23.7835 mL |
5 mM | 0.4757 mL | 2.3783 mL | 4.7567 mL |
10 mM | 0.2378 mL | 1.1892 mL | 2.3783 mL |
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