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glucocorticoid receptor agonist
Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs. It acts as an anti-inflammatory and immunosuppressant. Its potency is about 20-30 times that of the naturally occurring hormone hydrocortisone and 4-5 times of prednisone.- Ken Kobayashi, .et al. , Cell Tissue Res, 2022, Sep;389(3):501-515 PMID: 35748981
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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TLR7 agonist
Imiquimod (Aldara) is a a heterocyclic imidazoquinoline amide that acts as an immune response modifier.- David Diaz-Carballo, .et al. , Commun Biol, 2021, Mar 3;4(1):276 PMID: 33658617
- Kunishita Y, .et al. , Front Immunol, 2020, Feb 7;11:98 PMID: 32117252
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COX inhibitor/histamine H1 receptor agonist
Fexofenadine HCl is an antihistamine that inhibits Cox-1, Cox-2, and is a histamine H1 receptor agonist -
TLR7 agonist
PF-4878691 (3M-852A) is a potent, orally active, and selective Toll-like receptor 7 (TLR7) agonist modelled to dissociate its antiviral and inflammatory activities. -
GPR35/CXCR8 agonist
GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC50 of 5.8 nM, displays good druggability. -
human-specific STING agonist
STING agonist-1 (G10) is a novel human-specific STING agonist that elicits antiviral activity against emerging Alphaviruses. -
TLR8 agonist
VTX-2337 is a small-molecule Toll-like receptor 8 (TLR8) agonist with potential immunostimulating and antineoplastic activities.- Yinwen Cheng, .et al. , Sci Rep, 2021, Jan 15;11(1):1535 PMID: 33452311
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TLR7 agonist
GS-9620 is a potent and selective orally active small molecule agonist of Toll-like receptor 7.- Yu-Geun Ji, .et al. , J Pharm Biomed Anal, 2019, 12 November, 112987
- Zhikuan Zhang, .et al. , Cell Reports, 2018, 25(12): 3371-3381.e5 PMID: 30566863
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GPR3 agonist/NOS/ NADPH oxidases inhibitor
Diphenyleneiodonium chloride has been shown to be a potent irreversible inhibitor of NOS2 (iNOS) from macrophages and NOS3 (eNOS) from endothelial cells. -
Integrin agonist
Leukadherin 1 is an allosteric activator of CD11b/CD18. Increases CD11b/CD18-dependent cell adhesion to fibrinogen (EC50 = 4 μM). -
Thrombopoietin(TPO) receptor agonist
Avatrombopag is a novel orally-active thrombopoietin (TPO) receptor agonist. -
TLR7 agonist
Isatoribine is a novel guanosine analogue showing immunostimulatory activity both in vivo and in vitro. -
c-mpl (TpoR) receptor agonist
Eltrombopag olamine is a new, orally active thrombopoietin-receptor (c-mpl) agonist that stimulates thrombopoiesis. -
TLR7/8 Agonist
Resiquimod is an immune response modifier that acts as a potent TLR 7/8 agonist. Phase 2. -
TPO agonist
TPO agonist 1 can increase production of platelets by stimulating the TPO receptor in people with chronic ITP. -
CCR8 agonist
ZK-756326 is a potent, selective and non-peptide CCR8 chemokine receptor agonist. ZK 756326 inhibited the binding of the CCR8 ligand I-309 (CCL1), with an IC(50) value of 1.8 μM. -
glucocorticoid receptor agonist
Dexamethasone acetate (Dexamethasone 21-acetate) is a glucocorticoid receptor agonist. -
GPR35/CXCR8 agonist
Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8. -
STING agonist
ADU-S100 (MIW815) is a synthetic cyclic dinucleotide (CDN) agonist (activator) of Stimulator of Interferon Genes (STING), a receptor crucial to activate the innate (endogenous) immune system. -
TLR7 agonist
TLR7-agonist-1 is a potent and selective Toll-like Receptor 7 (TLR7) agonist with a LEC of 0.4 μM. -
TLR7 agonist
Gardiquimod is a chemical compound which acts selectively at both mouse and human forms of toll-like receptor 7 (TLR7). It functions as an immune response modifier. CAS: 1159840-61-5 (TFA) 1020412-43-4 (free base) -
glucocorticoid receptor agonist
Dexamethasone Phosphate disodium is a is a water-soluble form of the synthetic glucocorticoid dexamethasone. -
thrombopoietin (TPO) receptor agonist
Lusutrombopag, also known as S-888711, is an orally bioavailable, small molecule thrombopoietin (TPO) receptor agonist being developed by Shionogi for chronic liver disease (CLD) patients with thrombocytopenia prior to elective invasive surgery. -
glucocorticoid receptor agonist
Dexamethasone palmitate (DXP) is a prodrug of Dexamethasone, which is a glucocorticoid receptor agonist. Dexamethasone palmitate (DXP) has a 47-fold lower affinity for the glucocorticoid receptor than Dexamethasone. Anti-inflammatory agent. -
STING receptor agonist
STING agonist-4 is an stimulator of Interferon Genes (STING) receptor agonist with an apparent inhibitory constant (IC50) of 20 nM. -
TLR7 agonist
TLR7 agonist 1 is a potent, selective and oral TLR7 agonist with an IC50 of 90 nM. -
ERRγ agonist
GSK5182 is a highly selective inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM and does not interact with other nuclear receptors, including ERRα or ERα.- Sen He, .et al. , Toxicology, 2021, May 4;457:152805 PMID: 33961950
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IL receptor agonist
NO-prednisolone is a nitric oxide (NO)-releasing derivative of Prednisolone. NO-prednisolone potently stimulates IL-10 production in vivo. -
STING agonist
Cyclic-di-GMP is a STING agonist and a ubiquitous second messenger that regulates biofilm formation, motility, and virulence in diverse bacterial species. -
STING agonist
STING agonist-3, compound 3, is a selective and non-nucleotide small-molecule STING agonist, which has durable anti-tumor effect and tremendous potential to improve treatment of cancer. -
GPR35/CXCR8 agonist
Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8. -
TLR7/8 agonist
Telratolimod is a toll like receptors 7/8 (TLR7/8) agonist, with antitumor activity. -
S1PR1 agonist
FTY720 (S)-Phosphate is an agonist of S1P receptor 1 (S1PR1), used in the research of acute inflammatory diseases such as acute lung injury. -
STING receptor agonist
diABZI STING agonist-1 is a selective stimulator of interferon genes (STING) receptor agonist, with an EC50s of 130 nM for human PBMCs. -
STING receptor agonist
diABZI STING agonist-1 (trihydrochloride) is a selective stimulator of interferon genes (STING) receptor agonist, with an EC50s of 130 for human PBMCs. -
TLR7/8 agonist
TLR7/8 agonist 1 dihydrochloride is a toll-like receptor (TLR7)/TLR8 dual-agonistic imidazoquinoline.