| Description |
SB26019 is a potent anti-neuroinflammatory agent. SB26019 regulates NF-κB activation by inducing monomeric α-tubulin formation. SB26019-induced α-tubulin monomer inhibits p65 translocation[1].
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| Related Catalog |
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| In Vitro |
SB26019（10 μM；持续 6 小时）抑制炎症标记基因的产生，例如 Ccl2、Cxcl10、Il-1β、Il-6、Nos2 和 Tnf[1]。 SB26019 (1.25-10 μM; 1-12 h) 以时间和剂量依赖的方式诱导 IκB 降解[1]。 SB26019（IC50 为 1.13 μM）与抗炎调节剂秋水仙碱（IC50 为 4.20 μM）相比，产生更多的 α-微管蛋白单体和更少的微管蛋白聚合物[1]. SB26019 (10 μM) 诱导的 α-微管蛋白单体抑制 J774A.1 和 RAW264.7 小鼠巨噬细胞中的 p65 易位[1]。 RT-PCR[1] Cell Line: BV-2 murine microglial cells Concentration: 10 μM Incubation Time: 6 h Result: Suppressed the production of inflammatory marker genes. Western Blot Analysis[1] Cell Line: J774A.1 cells Concentration: 1.25 μM, 2.5 μM, 5 μM, 10 μM Incubation Time: 1 h, 3 h, 6 h, 12 h Result: Dose- and time-dependent IκB degradation without affecting the total amount of p65 in J774A.1 cells.
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| In Vivo |
SB26019（2-5mg/kg；i.p；每天；持续 4 天）改善体内神经炎症[1]。Pharmacokinetic (PK) analysis of SB26019[1]. Parameters I.P.,5 mg/kg Tmax (h) 0.17 ± 0.00 Cmax (μg/mL) 1.20 ± 0.26 T1/2 (h) 3.57 ± 0.62 AUCt (μg h/mL) 1.77 ± 0.30 AUC∞ (μg h/mL) 1.79 ± 0.31 CL (L/h/kg) NA Vss (L/kg) NA Ft (%) NA Animal Model: 10-week-old female C57BL/6 mice (20-25 g)[1] Dosage: 2 mg/kg, 5 mg/kg Administration: i.p; daily; for 4 days Result: Suppressed microglial activation by downregulating lba-1 and proinflammatory cytokines.
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| References |
[1]. Junhyeong Yim, et al. Phenotype-based screening rediscovered benzopyran-embedded microtubule inhibitors as anti-neuroinflammatory agents by modulating the tubulin-p65 interaction. Exp Mol Med. 2022 Dec 12;1-10.
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