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MedChemExpress - Model Bezisterim - ...

MedChemExpress - Model Bezisterim - 1001100-69-1

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

MCE China：Bezisterim

Brand：MedChemExpress (MCE)

Cat. No.HY-108039

CAS：1001100-69-1

Synonyms：HE 3286; NE-3107

Purity：95.0%

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

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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. 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 Vitro：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].

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 (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].

IC50 & Target：NF-κB[3] In Vitro 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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Bezisterim Related Antibodies Western Blot Analysis[3] Cell Line: LPS-induced murine macrophages

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

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