1. Immunology/Inflammation Apoptosis
  2. Toll-like Receptor (TLR) Interleukin Related TNF Receptor
  3. GAP214

GAP214 是一种单糖 Toll 样受体 4 (TLR4) 激动剂。GAP214 可通过疏水相互作用、盐桥和氢键与 TLR4/MD-2 复合物结合,诱导该复合物二聚化以启动细胞内信号级联反应。GAP214 可作为疫苗佐剂,在小鼠模型中增强抗原特异性 IgG 抗体的产生。

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GAP214

GAP214 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GAP214 is a monosaccharide lipid A analogue and TLR4/MD-2 complex modulator.GAP214 binds to the TLR4/MD-2 complex via hydrophobic interactions, salt bridges, and hydrogen bonds, induces dimerization of the complex to initiate intracellular signaling cascades.GAP214 functions as an immunostimulant and vaccine adjuvant, enhances antigen-specific IgG antibody production in a mouse model[1].

IC50 & Target[1]

TLR4

 

体外研究
(In Vitro)

GAP214 可通过 TLR4 通路强效激活小鼠 DC2.4 树突状细胞,诱导的 IL-6 分泌水平较 PHAD 高 3.5 倍、IL-12p70 分泌水平较 PHAD 高 4.7 倍,还可将 CD80+CD86+双阳性细胞比例提升至 17.98%[1]
GAP214 可通过 TLR4 通路强效激活小鼠 RAW264.7 巨噬细胞,其诱导的 IL-6 和 TNF-α 分泌水平高于 PHAD,还能将 CD80+CD86+双阳性细胞比例提升至 14.47%[1]
GAP214 可强效激活人 THP-1 单核细胞,其诱导的 IL-6 和 TNF-α 分泌水平高于 PHAD[1]
GAP214 (10-100 μg/mL; 24 h) 对 HEK293 或 B16F10 细胞无显著细胞毒性[1]

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

体内研究
(In Vivo)

GAP214 (17 μg/只小鼠/次;腹腔注射;每 2 周 1 剂,共 3 剂) 在 BALB/c 小鼠中可作为强效 TLR4 激动剂疫苗佐剂,在三次免疫后诱导产生的 IgG 抗体滴度较 PHAD 对照组高 2.5 倍,同时可实现强效树突状细胞 (DC) 活化、抗原特异性 T 细胞应答及记忆 T 细胞形成[1]

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

Animal Model: BALB/c (female, 6-8 weeks old, 5 mice per group)[1]
Dosage: 17 μg per mouse per immunization (formulated into liposomes with DSPC:cholesterol:GAP214 molar ratio 5:4:1)
Administration: intraperitoneal injection; 3 doses at 2-week intervals
Result: Induced IgG antibody titers 3.3-fold higher than PHAD-adjuvanted control after first immunization (Day 14).
Induced IgG antibody titers 2.5-fold higher than PHAD-adjuvanted control after third immunization (Day 42).
Exhibited highest serum IL-6 levels among adjuvant groups at 2 hours post-immunization.
Promoted maturation and activation of dendritic cells, with 24.60% CD80+CD86+ DCs in spleen and 10.30% CD80+CD86+ DCs in draining lymph nodes after two immunizations and 3 days of observation.
Induced 5.88% IFN-γ+TNF-α+ CD4+ T cells and 4.92% IFN-γ+TNF-α+ CD8+ T cells in splenocytes, the highest among adjuvant groups.
Induced 12.03% CD4+ central memory T cells and 19.52% CD8+ central memory T cells in spleen, which were 1.5-fold and 2.5-fold higher than PHAD-adjuvanted control, respectively.
分子量

1701.44

Formula

C95H182N3O19P

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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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
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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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产品名称:
GAP214
目录号:
HY-182034
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