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1001100-69-1

1001100-69-1 structure
1001100-69-1 structure
  • Name: HE 3286
  • Chemical Name: 17α-ethynylandrost-5-ene-3β,7β,17β-triol
  • CAS Number: 1001100-69-1
  • Molecular Formula: C21H30O3
  • Molecular Weight: 330.46
  • Catalog: Research Areas Inflammation/Immunology
  • Create Date: 2018-06-04 16:15:31
  • Modify Date: 2025-08-25 07:48:38
  • HE3286, a synthetic derivative of the adrenal steroid β-AET, is an orally-active partially NF-κB inhibitor [1][2].
Name 17α-ethynylandrost-5-ene-3β,7β,17β-triol
Synonyms 17α-ethynyl-5-androstene-3β,7β,17β-triol
17α-ethynyl-androst-5-ene-3β,7β,17β-triol
HE 3286
Description HE3286, a synthetic derivative of the adrenal steroid β-AET, is an orally-active partially NF-κB inhibitor [1][2].
Related Catalog
In Vitro HE3286 attenuates NF-κB phosphorylation, but not influences IκB phosphorylation of LPS-induces (100 ng/ml; 0-2 hours) murine macrophages [3]. HE3286 (100 nM, overnight) partially, but significantly, 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, but significantly.
In Vivo HE3286 (80 mg/kg; 0-24h) freely penetrates the BBB in male CD-1 mice[4]. HE3286 (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 PD mice [4]. HE3286 (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 EAE mice [2]. HE3286 (25-50 mg/kg; oral gavage; daily for 22-49 days) reduces joint inflammation, synovial proliferation, and erosion of DBA/1 Lac male CIA mice [1].
References

[1]. [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]. [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.

[3]. [3] Lu M,et al. A new antidiabetic compound attenuates inflammation and insulin resistance in Zucker diabetic fatty rats. Am J Physiol Endocrinol Metab. 2010;298(5):E1036-E1048.

[4]. [4] Nicoletti F, et al. 17α-Ethynyl-androst-5-ene-3β,7β,17β-triol (HE3286) Is Neuroprotective and Reduces Motor Impairment and Neuroinflammation in a Murine MPTP Model of Parkinson's Disease. Parkinsons Dis. 2012;2012:969418.
Molecular Formula C21H30O3
Molecular Weight 330.46
Exact Mass 330.21900
PSA 60.69000
LogP 2.64520
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