1. Anti-infection
  2. HBV
  3. DF-006

DF-006 是一种首创的口服有效的 ALPK1 (α-激酶 1) 的激动剂。DF-006 通过激活 NF-κB 通路刺激先天免疫反应,从而刺激肝脏局部的先天免疫。DF-006 可降低血清乙型肝炎病毒 (HBV) DNA (EC50 = 2.7 pM)、HBsAg 和 HBeAg 水平,表现出强效抗病毒效果,适用于慢性乙型肝炎 (CHB) 的免疫治疗研究。

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DF-006 Chemical Structure

DF-006 Chemical Structure

CAS No. : 2311947-41-6

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DF-006 is a first-in-class orally active agonist of ALPK1 (α-kinase 1). DF-006 can stimulate the innate immune response by activating the NF-κB pathway and strongly stimulate the innate immunity in the liver locally. DF-006 reduces the levels of serum HBV DNA (EC50 = 2.7 pM), HBsAg and HBeAg, and has shown strong antiviral effects. DF-006 is suitable for research on the immunotherapy of chronic hepatitis B (CHB)[1].

体外研究
(In Vitro)

DF-006 (0.3 pM-10 nM; 10天处理) 在原代人肝细胞 (PHH) 中显著抑制 HBV DNA 复制(EC50 = 2.7 pM) ,但未降低 cccDNA 水平[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Real Time qPCR

Cell Line: Primary human hepatocytes (PHHs)
Concentration: 1 pM, 10 pM, 100 pM, 1 nM, 10 nM
Incubation Time: 72 h post-infection for 10 days
Result: Potently suppressed HBV DNA (EC50 = 2.7 pM)
Decreased encapsidated pgRNA (55%) and rcDNA (97%)
No significant reduction in cccDNA
Upregulated NF-κB target genes (TNF, IFN-β etc.)

ELISA Assay[1]

Cell Line: Primary human hepatocytes (PHHs)
Concentration: 1 pM, 10 pM, 100 pM, 1 nM, 10 nM
Incubation Time: 24 h post-infection for 10 days
Result: Reduced by up to 36% at 72 pM
No significant reduction observed
药代动力学
(Parmacokinetics)
Species Dose SampleTime Route
Mice 20 mg/kg 0, 2, 4, 8 hours post-dose p.o.
体内研究
(In Vivo)

DF-006 (0.02-25 μg/kg;口服灌胃;21-28 天) 可降低血清 HBV DNA (最高2.4 log10)、HBsAg (0.66 log10) 和 HBeAg,并减少肝内 HBcAg (57%) 和 HBsAg[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6J mice (4-week-old) were injected with 1011 vector genomes of AAV- HBV through the tail vein
Dosage: 1 μg/kg, 5 μg/kg, 25 μg/kg
Administration: Oral gavage; once daily; for 28 days
Result: Reduced HBV DNA by 2.4 log10 copies/μL at 25 μg/kg.
Decreased HBsAg y 0.66 log10 IU/mL at 5 μg/kg and Significantly reduced at 5 μg/kg.
HBcAg nuclear staining decreased by 57% at 5 μg/kg.
Animal Model: Male C57BL/6J mice (4-week-old) were injected with 1011 vector genomes of AAV- HBV through the tail vein
Dosage: 0.02 μg/kg, 0.08 μg/kg, 0.25 μg/kg, 1 μg/kg
Administration: Oral gavage; once daily; for 21 days
Result: Potently suppressed HBV replication at doses as low as 0.08 μg/kg, with maximal efficacy at 25 μg/kg.
Reduced serum HBV DNA, HBsAg/HBeAg, and intrahepatic HBcAg/nucleocapsids.
No ALT elevation or overt toxicity, supporting clinical potential.
Animal Model: Male C57BL/6J mice (4-week-old) were injected with 1011 vector genomes of AAV- HBV through the tail vein
Dosage: DF-006 (10 μg/kg) combined with Entecavir (HY-13623) (ETV, 50 μg/kg)
Administration: Oral co-administration daily for 28 days
Result: Showed additive reduction of serum HBV DNA (1.3 log10 vs monotherapy).
分子量

805.57

Formula

C25H34FN5O18P2S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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DF-006
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HY-176507
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