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HE 3286
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
HE 3286图片
CAS NO:1001100-69-1
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
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。
生物活性

HE 3286 is a synthetic derivative of a natural anti-inflammatory steroid, β-AET. HE 3286 is an orally active partialNF-κBinhibitor. HE3286 reduces proinflammatory signals, includingIL-6and 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[1][2][3].

IC50& Target

NF-κB[3]

体外研究
(In Vitro)

HE 3286 attenuates NF-κB phosphorylation, but not influences IκB phosphorylation of LPS-induces (100 ng/mL; 0-2 hours) murine macrophages[3].
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[3].

Western Blot Analysis[3]

Cell Line:LPS-induced murine macrophages
Concentration:100 nM
Incubation Time:overnight
Result:Attenuated NF-κB phosphorylation.
Blocked the activation of IKK, JNK, p38, and ERK partially.
体内研究
(In Vivo)

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[1].
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[2].
HE 3286 (80 mg/kg; 0-24h) freely penetrates the BBB in male CD-1 mice[4].
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 Parkinson's disease mice[4].

Clinical Trial
分子量

330.46

性状

Solid

Formula

C21H30O3

CAS 号

1001100-69-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

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