HE 3286 是天然抗炎类固醇 β-AET 的合成衍生物。HE 3286 是具有口服活性的 NF-κB 部分抑制剂。HE 3286 降低了促炎信号，包括 IL-6 和基质金属肽酶 3。HE 3286 可自由穿过小鼠血脑屏障。HE 3286 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。

HE 3286 is a synthetic derivative of a natural anti-inflammatory steroid, β-AET. HE 3286 is an orally active partial NF-κB inhibitor. HE3286 reduces proinflammatory signals, including IL-6 and matrix metallopeptidase 3. HE 3286 freely penetrates the blood brain barrier in mice. HE 3286 can be used for the research of the ulcerative colitis, arthritis, experimental autoimmune encephalomyelitis.

Solid

NF-κB

HE 3286 attenuates NF-κB phosphorylation, but not influences IκB phosphorylation of LPS-induces (100 ng/mL; 0-2 hours) murine macrophages.
HE 3286 (100 nM, overnight) partially blocks the activation of IKK, JNK, p38, and ERK of LPS-induces (100 ng/mL; 0-2 hours) murine macrophages. has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis

HE 3286 (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 .
HE 3286 (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.
HE 3286 (80?mg/kg; 0-24h) freely penetrates the BBB in male CD-1 mice.
HE 3286 (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 Parkinsons disease mice. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Auci D, et al. A new orally bioavailable synthetic androstene inhibits collagen-induced arthritis in the mouse: androstene hormones as regulators of regulatory T cells. Ann N Y Acad Sci. 2007;1110:630-640.
[2]. Khan RS, et al. HE3286 reduces axonal loss and preserves retinal ganglion cell function in experimental optic neuritis. Invest Ophthalmol Vis Sci. 2014;55(9):5744-5751. Published 2014 Aug 19.