For research use only. Not for therapeutic Use.
Bezisterim (HE 3286; NE-3107) is a synthetic derivative of a natural anti-inflammatory steroid, β-AET. Bezisterim is an orally active partial NF-κB inhibitor. HE3286 reduces proinflammatory signals, including IL-6 and matrix metallopeptidase 3. Bezisterim freely penetrates the blood brain barrier in mice. Bezisterim can be used for the research of the ulcerative colitis, arthritis, experimental autoimmune encephalomyelitis[1][2][3]. Bezisterim is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Bezisterim attenuates NF-κB phosphorylation, but not influences IκB phosphorylation of LPS-induces (100 ng/mL; 0-2 hours) murine macrophages[3].
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[3].
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 [1].
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[2].
Bezisterim (80?mg/kg; 0-24h) freely penetrates the BBB in male CD-1 mice[4].
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[4].
| Catalog Number | I009888 |
| CAS Number | 1001100-69-1 |
| Synonyms | (3S,7R,8R,9S,10R,13S,14S,17R)-17-ethynyl-10,13-dimethyl-1,2,3,4,7,8,9,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthrene-3,7,17-triol |
| Molecular Formula | C21H30O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C21H30O3/c1-4-21(24)10-7-16-18-15(6-9-20(16,21)3)19(2)8-5-14(22)11-13(19)12-17(18)23/h1,12,14-18,22-24H,5-11H2,2-3H3/t14-,15-,16-,17-,18+,19-,20-,21-/m0/s1 |
| InChIKey | JJKOQZHWYLMASZ-FJWDNACWSA-N |
| SMILES | CC12CCC(CC1=CC(C3C2CCC4(C3CCC4(C#C)O)C)O)O |
| Reference | [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. [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]. 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. |
