GAP214
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C95H182N3O19P
- 分子量:1701.44
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
TLR4 |
体外実験
GAP214 potently activates murine DC2.4 dendritic cells via the TLR4 pathway, inducing 3.5-fold higher IL-6 and 4.7-fold higher IL-12p70 secretion than PHAD, and increasing CD80+CD86+ double-positive cells to 17.98%[1].
GAP214 potently activates murine RAW264.7 macrophages via the TLR4 pathway, inducing higher IL-6 and TNF-α secretion than PHAD, and increasing CD80+CD86+ double-positive cells to 14.47%[1].
GAP214 potently activates human THP-1 monocytic cells, inducing higher IL-6 and TNF-α secretion than PHAD[1].
GAP214 (10-100 μg/mL; 24 h) exhibits no significant cytotoxicity against HEK293 or B16F10 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 6-8 weeks old, 5 mice per group)[1]
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Dosage:17 μg per mouse per immunization (formulated into liposomes with DSPC:cholesterol:GAP214 molar ratio 5:4:1)
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Administration:intraperitoneal injection; 3 doses at 2-week intervals
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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.
化学情報
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分子量 1701.44
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分子式 C95H182N3O19P
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SMILES
OC[C@@H]1[C@@H](OP(O)(O)=O)C(OC(C[C@H](OC(CCCCCCCCCCCCC)=O)CCCCCCCCCCC)=O)[C@@H](NC(C[C@H](OC(CCCCCCCCCCCCC)=O)CCCCCCCCCCC)=O)[C@H](OCC(CNC(C[C@H](O)CCCCCCCCCCC)=O)(CNC(C[C@H](O)CCCCCCCCCCC)=O)CO)O1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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How to Choose the Right Model Animal
Choosing the right model animal is a validity-driven decision in which the species, strain, sex, age, genetic background, disease-induction method, outcome measures, and welfare burden must match the scientific question rather than laboratory tradition or convenience. A model should be selected by judging face validity, construct validity, and predictive validity: whether it resembles the human phenotype, whether it reproduces relevant mechanisms, and whether results are likely to predict human biology or treatment response. Animal studies often fail to translate because of species differences, weak disease resemblance, poor experimental design, inadequate reporting, publication bias, and underuse of randomization, blinding, and sample-size justification. Unresolved questions include how to rank competing models objectively, how much human-disease complexity must be reproduced for a given objective, and when non-animal systems such as organoids, ex vivo tissue, or computational models
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)