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Pregn-5-en-20-yne-3,7,17-triol, (3β,7β,17α)-

Product NamePregn-5-en-20-yne-3,7,17-triol, (3β,7β,17α)-
CAS1001100-69-1
MFC21H30O3
MW330.47
EINECS
MOL File1001100-69-1.mol

Chemical Properties

Boiling point	485.8±45.0 °C(Predicted)
Density	1.20±0.1 g/cm3(Predicted)
pka	12.99±0.70(Predicted)
form	Solid
color	Off-white to light yellow

Usage And Synthesis

Uses

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.

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 ^[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 (80mg/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].

References

[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. DOI:10.1196/annals.1423.066
[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. DOI:10.1167/iovs.14-14672
[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. DOI:10.1152/ajpendo.00668.2009
[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. DOI:10.1155/2012/969418

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