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

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GAP214

GAP214 Chemical Structure

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Description

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

 

In Vitro

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.

In Vivo

GAP214 (17 μg per mouse per immunization; intraperitoneal injection; 3 doses at 2-week intervals) functions as a potent TLR4 agonist vaccine adjuvant in BALB/c mice, inducing IgG antibody titers 2.5-fold higher than the PHAD control after three immunizations, alongside robust DC activation, antigen-specific T cell responses, and memory T cell formation[1].

MedChemExpress (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.
Molecular Weight

1701.44

Formula

C95H182N3O19P

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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Room temperature in continental US; may vary elsewhere.

Storage

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

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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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GAP214
Cat. No.:
HY-182034
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