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BC1618

رقم الكتالوجGC62135

يحفز BC1618 ، وهو مركب مثبط نشط عن طريق الفم Fbxo48 ، الإشارات المعتمدة على Ampk (عن طريق منع pAmpkα المنشط من التحلل بوساطة Fbxo48)

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BC1618 التركيب الكيميائي

Cas No.: 2222094-18-8

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
59٫00
متوفر
5mg
53٫00
متوفر
10mg
84٫00
متوفر
25mg
168٫00
متوفر
50mg
252٫00
متوفر
100mg
378٫00
متوفر

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مراجعات العميل

بناء على آراء العملاء.

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents

BC1618, an orally active Fbxo48 inhibitory compound, stimulates Ampk-dependent signaling (via preventing activated pAmpkα from Fbxo48-mediated degradation). BC1618 promotes mitochondrial fission, facilitates autophagy and improves hepatic insulin sensitivity[1].

BC1618 enhances pAmpkα protein stability during CHX treatment[1].BC1618 displays more than 1,000-fold enhanced activity to stimulate pAmpkα in cells than metformin[1].BC1618 (0.1-2 μM, 16 h) induced dose- and time-dependent increases in pAmpkα and pACC protein levels are also confirmed in human primary-like hepatocytes[1].BC1618 (1 μM) effectively disrupts the interaction between Fbxo48 and pAmpkα, and has no effect on Fbxo48, Ampkα1 or Ampkα2 messenger RNAs[1].BC1618 increases the abundance of a series of autophagic marker proteins during glucose depletion. BC1618 induces phosphorylation of the mTORC1 associated protein Raptor, reducing pS6 levels, all consistent with the known mTOR inhibitory effects exerted by activated Ampk[1].

BC1618 promotes mitochondrial fission, facilitates autophagy and improves hepatic insulin sensitivity in high-fat-diet-induced obese mice[1].BC1618, appears to be ~1,000-fold more potent than metformin and is extremely well tolerated in mice[1].BC1618 displays excellent oral bioavailability with a peak of 2,000 ng/mL within 0.5h and 500 ng/mL in plasma at 4h after an oral load of 20mg/kg[1].

[1]. Yuan Liu, et al. A Fbxo48 inhibitor prevents pAMPKα degradation and ameliorates insulin resistance. Nat Chem Biol. 2021 Mar;17(3):298-306.

مراجعات

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