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Bezisterim

CAS No. : 1001100-69-1

MCE 站：Bezisterim

产品活性：Bezisterim (HE 3286; NE-3107) 是天然抗炎类固醇 β-AET 的合成衍生物。Bezisterim 是具有口服活性的 NF-κB 部分抑制剂。Bezisterim 降低了促炎信号，包括 IL-6 和基质金属肽酶 3。Bezisterim 可自由穿过小鼠血脑屏障。Bezisterim 可用于溃疡性结肠炎、关节炎、实验性自身免疫性脑脊髓炎的研究。是

研究领域：NF-κB

作用靶点：NF-κB

In Vitro: Bezisterim attenuates NF-κB phosphorylation, but not influences IκB phosphorylation of LPS-induces (100 ng/mL; 0-2 hours) murine macrophages.
Bezisterim (100 nM, overnight) partially blocks the activation of IKK, JNK, p38, ａnd ERK of LPS-induces (100 ng/mL; 0-2 hours) murine macrophages.

In Vivo: Bezisterim (25-50 mg/kg; oral gavage; daily for 22-49 days) reduces joint inflammation, synovial proliferation, ａnd erosion of DBA/1 Lac male collagen-induced arthritis mice .
Bezisterim (40 mg/kg; intraperitoneal injection; daily for 40 days) suppresses inflammation, reduces demyelination ａnd axonal loss, ａnd promotes RGC survival during experimental optic neuritis of experimental autoimmune encephalomyelitis mice.
Bezisterim (80?mg/kg; 0-24h) freely penetrates the BBB in male CD-1 mice.
Bezisterim (40 mg/kg; gavage; twice-daily for 4 days) increases the numbers of tyrosine hydroxylase-positive cells ａnd decreases the numbers of damaged neurons in Parkinson＇s disease mice.

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