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BBS-4

目录号 : GC27160

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。

BBS-4 Chemical Structure

Cas No.:402934-09-2

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥2,822.00
现货
5mg
¥2,565.00
现货
10mg
¥4,140.00
现货

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Sample solution is provided at 25 µL, 10mM.

Description

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/

化学性质

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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