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TLR7 agonist

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By Targets:	ADC Cytotoxin (2) Apoptosis (2) Autophagy (7) Drug-Linker Conjugates for ADC (5) EGFR (1) HBV (1) HCV (4) HIV (4) HSV (7) IFNAR (4) Influenza Virus (2) Interleukin Related (1) Isotope-Labeled Compounds (2) Liposome (1) MAPKAPK2 (MK2) (1) NF-κB (1) NOD-like Receptor (NLR) (1) Nucleoside Antimetabolite/Analog (5) PD-1/PD-L1 (2) Reactive Oxygen Species (2) SARS-CoV (7) TNF Receptor (3) Toll-like Receptor (TLR) (95)
By Research Areas:	Cancer (53) Infection (22) Inflammation/Immunology (65) Neurological Disease (1)
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Oligonucleotides:	Adjuvant (1)

104

Inhibitors & Agonists

Fluorescent Dye

Biochemical Assay Reagents

Isotope-Labeled Compounds

Click Chemistry

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-111358

TLR7 agonist 1	Toll-like Receptor (TLR)	Infection
TLR7 agonist 1 is a potent, selective and oral *TLR7* agonist with an IC₅₀ of 90 nM.

HY-145961

TLR7 agonist 4	Toll-like Receptor (TLR)	Cancer
TLR7 agonist 4 (Compound 1.2) is a *TLR7* agonist with an EC₅₀ of 4.3 nM .

HY-168159

TLR7 agonist 27	Toll-like Receptor (TLR) NOD-like Receptor (NLR)	Inflammation/Immunology
TLR7 agonist 27 (compound 24) is a potent *TLR7* agonist with an EC₅₀ of 238.1 nM. TLR7 agonist 27 shows weak agonistic activity against NOD2 (nucleotide-binding oligomerization domain 2) (EC₅₀ of 6.2 μM). TLR7 agonist 27 is a potent immunostimulant, and can be used as a vaccine adjuvant and/or immunotherapeutic .

HY-170899

TLR7 agonist 28	Toll-like Receptor (TLR)	Cancer
TLR7 agonist 28 (compound 3) is a potent *TLR7* agonist. TLR7 agonist 28 can conjugat to antitumor monoclonal antibodies (mAbs) for cancer immunotherapy .

HY-162579

TLR7 agonist 22	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7 agonist 22 (Compound 11a) emerges as a selective TLR7 agonist with an IC₅₀ value of 25.86 μM. TLR7 agonist 22 inhibits the cellular HBsAg secretion and effectively activates TLR7, thereby inducing the secretion of **TLR7-regulated *cytokines IL-12, TNF-αand IFN-αin human PBMC cells. TLR7* agonist 22 is a promising for research in the field of developing novel immunomodulatory anti-HBV agents .****

HY-173070

TLR7 agonist 29	Toll-like Receptor (TLR) IFNAR PD-1/PD-L1 ADC Cytotoxin	Inflammation/Immunology Cancer
TLR7 agonist 29 (Compound 1) is the agonist for *TLR7* with an EC₅₀ of 5.2 nM for human TLR7 (EC₅₀ for mouse TLR7 is 48.2 nM). TLR7 agonist 29 activates bone marrow-derived macrophages (BMDMs), stimulates myeloid cells in the tumor microenvironment, promotes the expression of PD-L1, CD86 and IFN-α. TLR7 agonist 29 can be used as payload for synthesis of ADC .

HY-168157

TLR7 agonist 26	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7 agonist 26 (Compound 4) is a potent Toll-like receptor 7 (TLR7) agonist, with an EC₅₀ of 225.5 nM. TLR7 agonist 26 shows immunopotentiating effects .

HY-162115

TLR7 agonist 17	Toll-like Receptor (TLR)	Cancer
TLR7 agonist 17 (compound 20) is a potent *TLR7* agonist with EC₅₀ values of 12 nM and 17 nM for hTLR7 and mTLR7, respectively. TLR7 agonist 17 shows anticancer activity .

HY-163670

TLR7 agonist 21	Toll-like Receptor (TLR)	Infection
TLR7 agonist 21 (Compound 27B) is a selective agonist for Toll-like receptor 7(TLR7), with an EC₅₀ of 17.53 nM (for human TLR7) and 41.7 nM (for mouse TLR7). TLR7 agonist 21 stimulates the secretion of pro-inflammatory cytokines, such as IL-6, TNF-α, IFN-α1, and IL-4. TLR7 agonist 21 acts as a vaccine adjuvant, increases levels of IgG and IgA, and protects the mouse from influenza virus infections .

HY-173079

TLR7 agonist 30	Toll-like Receptor (TLR) Drug-Linker Conjugates for ADC	Cancer
TLR7 agonist 30 (compound 2) is an agent-linker conjugate for ADC. TLR7 agonist 30 contains a TLR7 agonist (compound 1) and a cleavable linker, and has potent anti-tumor activity .

HY-156177

TLR7 agonist 16	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7 agonist 16 (compound 16d) is a highly potent *TLR7* agonist with an EC₅₀ of 18 nM. TLR7 agonist 16 potently induces the activation of mouse macrophages and hPBMCs at low-nanomolar concentrations .

HY-156176

TLR7 agonist 15	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7 agonist 15 (compound 16b) is a highly potent *TLR7* agonist with an EC₅₀ of 18 nM. TLR7 agonist 15 potently induces the activation of mouse macrophages and hPBMCs at low-nanomolar concentrations .

HY-156175

TLR7 agonist 14	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7 agonist 14 (compound 17b) is a highly potent *TLR7* agonist with an EC₅₀ of 18 nM. TLR7 agonist 14 potently induces the activation of mouse macrophages and hPBMCs at low-nanomolar concentrations .

HY-153072

TLR7 agonist 7	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7 agonist 7 (compound IIb-26) is an *TLR7* agonist with an EC₅₀ value of ~4 nM .

HY-153070

TLR7 agonist 5	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7 agonist 5 (compound IIb-11) is an *TLR7* agonist with an EC₅₀ value of ~4 nM .

HY-153073

TLR7 agonist 8	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7 agonist 8 (compound IIb-34) is an *TLR7* agonist with an EC₅₀ value of ~4 nM .

HY-161726

TLR7 agonist 23	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7 agonist 23 (compound 12b) is a potent Toll Like Receptor-7 (TLR7) agonist with a EC₅₀ of 0.15 uM. TLR7 agonist 23 can be used in the study of immunological diseases .

HY-152726

TLR7 agonist 9	Toll-like Receptor (TLR) Nucleoside Antimetabolite/Analog	Infection Cancer
TLR7 agonist 9 (compound 10) is an aonist of *TLR7. TLR7* agonist 9 can be used for research of cancer and infectious disease . TLR7 agonist 9 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-153071

TLR7 agonist 6	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7 agonist 6 (compound IIb-19) is an *TLR7* agonist with an EC₅₀ value of 1.0 nM .

HY-103039

TLR7 agonist 2 1 Publications Verification	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7 agonist 2 is a potent and selective Toll-like Receptor 7 (TLR7) agonist with a LEC of 0.4 μM.

HY-117602

TLR7 agonist 3 1 Publications Verification	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7 agonist 3 (Compound 2) is a potent agonist of toll-like receptor 7 (TLR7). TLR7 has an important role in immune activation processes and represents an emerging agent discovery target for the development of immunomodulators .

HY-162163

TLR7 agonist 19	Toll-like Receptor (TLR)	Cancer
TLR7 agonist 19 (Compound 14) is a Toll-like receptor 7 (TLR7) agonist with excellent pharmacokinetic properties and synergistic antitumor activity.

HY-158694A

TLR7 agonist 20 hydrochloride	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7 agonist 20 hydrochloride is an imidazoquinoline analogue. TLR7 agonist 20 hydrochloride is a potent *TLR7* specific agonist, with an EC₅₀ value of 0.23 μM for hTLR7. TLR7 agonist 20 hydrochloride shows strong adjuvant activity on spike antibody levels which induces a strong T helper 1 (Th1) response with increase in IgG2b and IgG2c, in addition to IgG1 .

HY-158694

TLR7 agonist 20	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7 agonist 20 (compound 23) is an imidazoquinoline analogue. TLR7 agonist 20 is a potent *TLR7* specific agonist, with an EC₅₀ value of 0.23 μM for hTLR7. TLR7 agonist 20 shows strong adjuvant activity on spike antibody levels which induces a strong T helper 1 (Th1) response with increase in IgG2b and IgG2c, in addition to IgG1 .

HY-162725

TLR7 agonist 24	Toll-like Receptor (TLR)	Infection Inflammation/Immunology
TLR7 agonist 24 (Compound 21) is an agonist for *TLR7* with EC₅₀ of 3.72 μM. TLR7 agonist 24 can be used as a vaccine adjuvant when combined with Aluminum Hydroxide (HY-B1521), that enhances the immune response against SARS-CoV-2 and hepatitis B antigens .

HY-162116

TLR7 agonist 18	Toll-like Receptor (TLR)	Inflammation/Immunology Cancer
TLR7 agonist 18 (Compound 21a) is a selective Toll-like receptor 7 (TLR7) agonist with an EC₅₀ of 7.8 μM. TLR7 agonist 18 is not cytotoxic to hTLR7 cotransfected HEK293 cell lines and can induce the secretion of several cytokines, including IL-1β, IL-12p70, IL-8, and TNF-α. TLR7 agonist 18 can be used in vaccine, asthma, allergy and anti-cancer research .

HY-154271

TLR7 agonist 12	Nucleoside Antimetabolite/Analog	Cancer
TLR7 agonist 12 (example 20) is a *TLR7* agonist, also is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc .

HY-154361

TLR7 agonist 13	Nucleoside Antimetabolite/Analog	Cancer
TLR7 agonist 13 is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7) . TLR7 agonist 13 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-115400

1V209 3 Publications Verification TLR7 agonist T7	Toll-like Receptor (TLR)	Cancer
1V209 (TLR7 agonist T7) is a Toll-like receptor 7 (TLR7) agonist and has anti-tumor effects. 1V209 can be conjugated with various polysaccharides to improve its water solubility, and enhance its efficacy, and maintain low toxicity .

HY-149072

TLR7 agonist 11	Nucleoside Antimetabolite/Analog	Cancer
TLR7 agonist 11 is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc .

HY-149071

TLR7 agonist 10	Nucleoside Antimetabolite/Analog	Cancer
TLR7 agonist 10 is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc .

HY-139017

TLR7/8 agonist 4	Toll-like Receptor (TLR)	Cancer
TLR7/8 agonist 4 (compound 41) is a potent *TLR7/8* agonist. TLR7/8 agonist 4 has anti-cancer activity .

HY-147236

TLR7/8 agonist 7	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7/8 agonist 7 (compound 10) is a **TLR7/8 agonist*. TLR7/8 agonist* 7 activates a variety of immune cells and it can be used to synthesize immune stimulating antibody conjugate (ISAC) molecules. TLR7/8 agonist 7 can be used for the research of immunity .

HY-139017A

TLR7/8 agonist 4 TFA	Toll-like Receptor (TLR)	Cancer
TLR7/8 agonist 4 TFA (compound 41) is a potent *TLR7/8* agonist. TLR7/8 agonist 4 has anti-cancer activity .

HY-103698

TLR7/8 agonist 1	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7/8 agonist 1 is a toll-like receptor (TLR7)/TLR8 dual-agonistic imidazoquinoline.

HY-103698A

TLR7/8 agonist 1 dihydrochloride	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7/8 agonist 1 dihydrochloride is a toll-like receptor *TLR7/TLR8* dual-agonistic imidazoquinoline .

HY-130797

TLR7/8 agonist 3	Toll-like Receptor (TLR)	Cancer
TLR7/8 agonist 3 is a potent *TLR7* and *TLR8* agonist, extracted from patent WO2016057618 (compound of formula (II)) .

HY-153544

TLR7/8 agonist 9	Toll-like Receptor (TLR)	Cancer
TLR7/8 agonist 9 (Compound 25a) is a *TLR7/8* agonist, with EC₅₀s of 40 nM and 23 nM for hTLR7/8. TLR7/8 agonist 9 has anti-tumor activity and improves the antitumor activity of PD-1/PD-L1 blockade. TLR7/8 agonist 9 can be used for research of cancer immunotherapy .

HY-145885

TLR7/8 agonist 6	Toll-like Receptor (TLR)	Infection Inflammation/Immunology Cancer
TLR7/8 agonist 6 (Compound 4) is the potent agonist of *TLR7/8* with IC₅₀s of 0.18 and 5.34 μM, respectively. TLR7/8 agonist 6 is an imidazoquinoline derivative compound. Toll-like receptors (TLRs) 7 and 8 are key targets in the development of immunomodulatory drugs for researching infectious disease, cancer, and autoimmune disorders .

HY-153543

TLR7/8 agonist 8	Toll-like Receptor (TLR)	Cancer
TLR7/8 agonist 8 (compound 24m) is a potent toll-like receptor 7/8 (TLR7/8) dual agonist, with EC₅₀s of 27 and 12 nM for hTLR7 and hTLR8, respectively. TLR7/8 agonist 8 can improve the antitumor activity of PD-1/PD-L1 blockade .

HY-156691A

TLR7/8 agonist 4 hydroxy-PEG6-acid hydrochloride	Drug-Linker Conjugates for ADC	Cancer
TLR7/8 agonist 4 hydroxy-PEG6-acid hydrochloride is a drug-linker conjugates for ADC>. TLR7/8 agonist 4 hydroxy-PEG6-acid hydrochloride is the hydrochloride form of TLR7/8 agonist 4 hydroxy-PEG6-acid. TLR7/8 agonist 4 hydroxy-PEG6-acid consists of TLR7/8 agonist 4 (HY-139017) and a non-cleavable linker Hydroxy-PEG6-acid (HY-133050), and can be used for synthesis of ADCs .

HY-170770

TLR7/8 agonist 12	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7/8 agonist 12 (compound 9) is an hTLR7/8 agonist, with EC₅₀ values of 11 nM (hTLR7) and 150 nM (hTLR8), respectively. TLR7/8 agonist 12 has the potential for immunomodulation .

HY-162845

TLR7/8 agonist 11	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7/8 agonist 11 (compound 30) is a potent agonist of hTLR7 and hTLR8, with EC₅₀s of 31.1 nM and 13.1 nM, respectively. TLR7/8 agonist 11 plays an important role in adaptive and innate immune responses .

HY-145960

*MC-Val-Cit-PAB-Amide-TLR7* agonist 4**	EGFR Toll-like Receptor (TLR)	Inflammation/Immunology
MC-Val-Cit-PAB-Amide-TLR7 agonist 4 (example 15) is a *HER2-TLR7* and *HER2-TLR8* immune agonist conjugate .

HY-139018

TLR7/8 agonist 4 hydroxy-PEG10-acid	Drug-Linker Conjugates for ADC	Cancer
TLR7/8 agonist 4 hydroxy-PEG10-acid (compound 9) is a drug-linker conjugates for ADC with potent antitumor activity by using TLR7/8 agonist 4 (HY-139018; a TLR7/8 agonist), linked via the non-cleavable ADC linker hydroxy-PEG10-acid (HY-133307) .

HY-139018A

TLR7/8 agonist 4 hydroxy-PEG10-acid hydrochloride	Drug-Linker Conjugates for ADC	Cancer
TLR7/8 agonist 4 hydroxy-PEG10-acid hydrochloride (compound 9) is a drug-linker conjugates for ADC with potent antitumor activity by using TLR7/8 agonist 4 (HY-139018; a TLR7/8 agonist), linked via the non-cleavable ADC linker hydroxy-PEG10-acid (HY-133307) .

HY-156691

TLR7/8 agonist 4 hydroxy-PEG6-acid	Drug-Linker Conjugates for ADC	Cancer
TLR7/8 agonist 4 hydroxy-PEG6-acid is a drug-linker conjugates for ADC. TLR7/8 agonist 4 hydroxy-PEG6-acid consists of TLR7/8 agonist 4 (HY-139017) and a non-cleavable linker Hydroxy-PEG6-acid (HY-133050), and can be used for synthesis of ADCs .

HY-156693

MTvkPABC-P5	Toll-like Receptor (TLR)	Inflammation/Immunology
MTvkPABC-P5d, a *TLR7* agonist, is an immune stimulant. MTvkPABC-P5d can be used for synthesis of immune-stimulating antibody conjugates (ISACs) .

HY-164485

INI-4001	Toll-like Receptor (TLR)	Neurological Disease
INI-4001 is a *TLR7/8* agonist, with EC₅₀ values of 1.89 μM and 4.86 μM for *TLR7/8, respectively. INI-4001 induces signaling and SEAP* production through *TLR7* and *TLR8* .

HY-160227

ORN 06	Toll-like Receptor (TLR)	Inflammation/Immunology
ORN 06 (Compound R-0006), a U-rich single-stranded RNA (containing 6 repeats of the UUG sequence motif), is a *TLR7/8* agonist. ORN 06 stimulates human *TLR7/8*-mediated or murine *TLR7*-mediated immunity .

Cat. No.	Product Name	Type

HY-13740G

Resiquimod (GMP) R848 (GMP); S28463 (GMP)	Fluorescent Dye
Resiquimod (R848) (GMP) is Resiquimod (HY-13740) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist. Resiquimod (GMP) can induce human mMDSC to mature into inflammatory macrophages .

HY-111582G

BBIQ (GMP)	Fluorescent Dye
BBIQ (GMP) is BBIQ (HY-111582) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. BBIQ is a potent and selectively toll-like receptor 7 (TLR7) agonist with an EC₅₀ of  59.1 nM. BBIQ is a powerful vaccine adjuvant that enhances innate immune responses .

Cat. No.	Product Name	Type

HY-13740G

Resiquimod (GMP) R848 (GMP); S28463 (GMP)	Biochemical Assay Reagents
Resiquimod (R848) (GMP) is Resiquimod (HY-13740) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist. Resiquimod (GMP) can induce human mMDSC to mature into inflammatory macrophages .

HY-111582G

BBIQ (GMP)	Biochemical Assay Reagents
BBIQ (GMP) is BBIQ (HY-111582) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. BBIQ is a potent and selectively toll-like receptor 7 (TLR7) agonist with an EC₅₀ of  59.1 nM. BBIQ is a powerful vaccine adjuvant that enhances innate immune responses .

Cat. No.	Product Name	Chemical Structure

HY-13740S

Resiquimod-d5 1 Publications Verification
Resiquimod-d₅ is deuterium labeled Resiquimod. Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α .

HY-B0180S1

Imiquimod-d9
Imiquimod-d₉ is deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19[1][2].

HY-B0180S

Imiquimod-d6
Imiquimod-d₆ is the deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19[1][2].

Cat. No.	Product Name		Classification

HY-154361

TLR7 agonist 13		Alkynes
TLR7 agonist 13 is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7) . TLR7 agonist 13 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-159100

PVP-037		Azide
PVP-037 is a potent *TLR7* and *TLR8* agonist adjuvant. PVP-037 shows broad innate immune activation and enhances vaccine immune responses .

HY-159102

PVP-037.2		Azide
PVP-037.2 is a *TLR7/8* agonist. PVP-037.2 can serve as an adjuvant to enhance vaccine-induced T_H1 type immune responses, increasing the production of antigen-specific antibodies IgG1 and IgG2c .

Cat. No.	Product Name		Classification

HY-111582

BBIQ		Adjuvant
BBIQ is a imidazoquinoline compound and a potent and selectively toll-like receptor 7 (TLR7) agonist with an EC₅₀ of ?59.1?nM for human TLR7. BBIQ is a powerful vaccine adjuvant that enhances innate immune responses .

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