1. Immunology/Inflammation Anti-infection
  2. Toll-like Receptor (TLR) SARS-CoV
  3. INI-4001

INI-4001 is a TLR7/8 agonist and vaccine adjuvant. INI-4001 regulates innate and adaptive immune responses by activating murine TLR7 and human TLR7/TLR8. INI-4001 enhances IgG and neutralizing antibody responses against Powassan virus (POWV), reduces viral loads in the brain, liver and spleen, provides complete protection against lethal POWV challenge, and skews immune responses toward a Th1 phenotype. When INI-4001 is used in combination with Al (OH)3 and SARS-CoV-2 RBD antigen, it efficiently adsorbs to Al (OH)3, promotes Th1 immunity and enhances SARS-CoV-2 neutralizing antibody responses. INI-4001 is applicable to research related to Powassan virus infection and COVID-19.

For research use only. We do not sell to patients.

INI-4001

INI-4001 Chemical Structure

CAS No. : 2549050-07-7

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Description

INI-4001 is a TLR7/8 agonist and vaccine adjuvant. INI-4001 regulates innate and adaptive immune responses by activating murine TLR7 and human TLR7/TLR8. INI-4001 enhances IgG and neutralizing antibody responses against Powassan virus (POWV), reduces viral loads in the brain, liver and spleen, provides complete protection against lethal POWV challenge, and skews immune responses toward a Th1 phenotype. When INI-4001 is used in combination with Al (OH)3 and SARS-CoV-2 RBD antigen, it efficiently adsorbs to Al (OH)3, promotes Th1 immunity and enhances SARS-CoV-2 neutralizing antibody responses. INI-4001 is applicable to research related to Powassan virus infection and COVID-19[1][2].

IC50 & Target

TLR7

 

TLR8

 

In Vitro

INI-4001 (200 μg/mL; 1 h) adsorbs efficiently to mixed formulations of aluminum oxyhydroxide (AH) and aluminum phosphate (AP) in 2% glycerin, with no desorption observed in the presence of INI-2002 or SARS-CoV-2 RBD[2].

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

In Vivo

INI-4001 (10 nmol; s.c.; prime-boost 2-4 weeks apart, single administration) adjuvant enhances the immunogenicity and protective efficacy of POW-VLP vaccines in mice, conferring 100% survival against lethal POWV-I and POWV-II challenge, reducing viral tissue burden, inducing durable antibody responses with 80% long-term survival 9 months post-boost, and mediating protection via humoral immunity independent of CD4+ or CD8+ T cells[1].
INI-4001 (10 μg per mouse; i.m.; day 0, day 14, day 42) co-delivered with SARS-CoV-2 RBD and aluminum salt (Alhydrogel or Adju-phos) significantly enhances RBD-specific IgG and Th1-skewed IgG2c antibody titers, induces robust antigen-specific Th1 (IFNγ-producing) T cell responses, and improves surrogate viral neutralization activity in C57BL/6 mice[2].

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

Animal Model: C57BL/6 (male, 7 weeks old at vaccination)[1]
Dosage: 10 nmol (prime-boost vaccination); 10 nmol (single vaccination)
Administration: s.c.; prime-boost 2-4 weeks apart; single administration
Result: Induced a mean log10 IgG endpoint titer of 4.9, with 11/18 mice having measurable FRNT50 neutralizing antibody titers.
Conferred 100% survival against lethal POWV-I challenge, compared to 50% survival with alum.
Reduced POWV-I viral RNA loads in the brain, liver, and spleen compared to mock-vaccinated mice post-challenge.
Enabled passive transfer of sera to protect 4/5 naïve mice from lethal POWV-I challenge.
Maintained 100% survival against lethal POWV-I challenge even after CD4+ or CD8+ T cell depletion.
Induced cross-reactive IgG antibodies to POWV-II and Langat virus, and conferred 100% survival against lethal POWV-II challenge, compared to 40% survival with alum; vaccinated mice had minimal weight loss (max ~3% initial weight) compared to alum-vaccinated survivors (10% weight loss).
Maintained significantly higher IgG and neutralizing antibody titers than alum-vaccinated mice for 36 weeks post-boost; enabled 80% survival against lethal POWV-I challenge 36 weeks post-boost.
Conferred 100% survival against lethal POWV-I challenge with single vaccination.
Molecular Weight

1141.50

Formula

C59H109N6O13P

CAS No.
SMILES

OC1=NC2=C(N)N=C(O[C@@H](C)CCC)N=C2N1CC3CCN(CCOP(OCCOCCOCCOC[C@H](OC(CCCCCCCCCCCCCCC)=O)COC(CCCCCCCCCCCCCCC)=O)(O)=O)CC3

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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.

Purity & Documentation
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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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INI-4001
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HY-164485
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