Theophylline (1,3-Dimethylxanthine) sodium glycinate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline sodium glycinate inhibits PDE3 activity to relax airway smooth muscle. Theophylline sodium glycinate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline sodium glycinate induces apoptosis. Theophylline sodium glycinate can be used for asthma and chronic obstructive pulmonary disease (COPD) research[1][2][3][4][5].
Aloenin aglycone (compound 13) is an NF-κB inhibitor that can be isolated from aloe exudate. Aloenin aglycone inhibits TNFα-induced NF-κB transcriptional activity (IC50: 18.7 μM). Aloenin aglycone (10 μM) also reduced inducible nitric oxide synthase (iNOS) and intercellular adhesion molecule 1 (ICAM-1) gene expression after treatment of HepG2 cells with 10 ng/mL TNFα[1].
CP-424174 is a reversible inhibitor against IL-1β processing with an IC50 of 210 nM.CP-424174 indirectly inhibits NLRP3[1].
1,3,5-Trihydroxy-4-prenylxanthone is a Na+/H+ exchange system (Na+/H+ Exchanger (NHE)) inhibitor with a minimum inhibitory concentration of 10 μg/mL[1]. 1,3,5-Trihydroxy-4-prenylxanthone is a phosphodiesterase type 5 (PDE5) (Phosphodiesterase (PDE)) inhibitor with an IC50 value of 3.0 μM[3]. 1,3,5-Trihydroxy-4-prenylxanthone inhibits Lipopolysaccharide (LPS) (Lipopolysaccharides (HY-D1056))-induced NO production in RAW264.7 macrophages, and has anti-inflammatory activities[2].
AZD8848 is a selective toll-like receptor 7 (TLR7) antedrug agonist which is developed for the research of asthma and allergic rhinitis[1].
7,4'-Dihydroxyflavone (7,4'-DHF) is a flavonoid isolated from Glycyrrhiza uralensis, the eotaxin/CCL11 inhibitor, has the ability to consistently suppress eotaxin production and prevent dexamethasone (Dex)‐paradoxical adverse effects on eotaxin production[1]. 7,4'-Dihydroxyflavone (7,4'-DHF) inhibits MUC5AC gene expression, mucus production and secretion via regulation of NF-κB, STAT6 and HDAC2.7,4'-Dihydroxyflavone (7,4'-DHF) decreases phorbol 12-myristate 13-acetate (PMA) stimulated NCI-H292 human airway epithelial cell MUC5AC gene expression and mucus production with IC50 value of 1.4 µM[1].
FRG-8701 is a new Histamine H2-receptor antagonist with an IC50 of ranging from 0.25 to 0.43 μM.
H3 receptor antagonist 1 is an antagonist of histamine H3 receptor, used in the research of neurological disease.
Meloxicam-13C,d3 is deuterium labeled Meloxicam. Meloxicam is a non-steroidal antiinflammatory agent, inhibits COX activity, with IC50s of 0.49 µM and 36.6 µM for COX-2 and COX-1, respectively.
(±)-Naproxen ((Rac)-Naproxen) is a racemate of Naproxen (HY-15030). Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively.
TPO agonist 1 can increase production of platelets by stimulating the TPO receptor in people with chronic ITP. (Idiopathic Thrombocytopenic Purpura)target: TPO receptor agonist1、TPO receptor agonists can be also used in Bone marrow fibrosis2、TPOreceptor agonists can decrease bleeding events and reduced need for adjunctive or rescue treatments.
3-Hydroxykynurenamine, also known as 3-Hydroxy-L-kynurenamine or 3-HKA, is a biogenic amine produced via an alternative pathway of tryptophan metabolism. In vitro, 3-HKA has an anti-inflammatory profile by inhibiting the IFN-γ mediated STAT1/NF-κΒ pathway in both mouse and human dendritic cells (DCs) with a consequent decrease in the release of pro-inflammatory chemokines and cytokines, most notably TNF, IL-6, and IL12p70. 3-HKA has protective effects in an experimental mouse model of psoriasis by decreasing skin thickness, erythema, scaling and fissuring, reducing TNF, IL-1β, IFN-γ, and IL-17 production, and inhibiting generation of effector CD8+ T cells. Similarly, in a mouse model of nephrotoxic nephritis, besides reducing inflammatory cytokines, 3-HKA improves proteinuria and serum urea nitrogen, overall ameliorating immune-mediated glomerulonephritis and renal dysfunction.
Hydroxyzine D4 is deuterium labeled Hydroxyzine. Hydroxyzine is a heterocyclic histamine H1-receptor antagonist. Hydroxyzine has anticholinergic, anxiolytic and analgesic properties[1].
2',3'-cGAMP (2'-3'-cyclic GMP-AMP) is a molecule in endogenous cGAMP mammalian cells which contains two distinct phosphodiester linkages, one between 2′-OH of GMP and 5′-phosphate of AMP, and the other between 3′-OH of AMP and 5′-phosphate of GMP. 2',3'-cGAMP is produced in mammalian cells in response to DNA in the cytoplasm and binds to STING with a high affinity and is a potent inducer of interferon-β (IFNβ)[1].
Dexanabinol (HU-211) is an artificially synthesized cannabinoid derivative and lacks cannabimimetic effects. Dexanabinol exhibits not only the antioxidant and neuroprotective activities in brain but also anti-inflammatory activity by inhibiting NF-κB and decreasing cytokines such as TNFα and interleukin-6, which could ensure the integrity of BBB and reduce cell apoptosis and death. Dexanabinol is widely used in head injury or stroke treatment and has been shown to be safe in animals and humans[1].
CU-115 is a potent TLR8 antagonist (IC50=1.04 µM), and shows selective for TLR8 over TLR7 (IC50=>50 µM). CU-115 decreases TNF-α and IL-1β production activated by R-848 in THP-1 cells[1].
IACS-8779 disodium is a highly potent stimulator of interferon genes (STING) agonist with robust systemic antitumor efficacy. IACS-8779 disodium shows robust activation of the STING pathway in vitro and a superior systemic anti-tumor response in the B16 murine model of melanoma[1].
7-Nitroindazole is a selective nNOS inhibitor with antinociceptive and cardiovascular effects. 7-Nitroindazole is a useful tool to evaluate the biological roles of nitric oxide in the central nervous system[1][2].
E104 (compound 1) is a potent and selective TLR7 agonist. E104 can be delivered by antibody-drug conjugate (ADC) technology to elicit potent anticancer activity. E104 induces the activation of mouse macrophages and hPBMCs[1].
TLR8 agonist 6 (Compound A) is a TLR8 agonist, with an EC50 of 0.052 μM. TLR8 agonist 6 induces IL-12p40 production in human PBMC (EC50: 0.031 μM). TLR8 agonist 6 can be used in the research of virus resistance, infection resistance, autoimmunity, tumor, etc[1].
ODN 1018 (1018 ISS), an oligodeoxynucleotide, is a TLR-9 agonist. ODN 1018 is also a synthetic immunostimulatory sequence that can be used as vaccine adjuvant. Sequence: 5′-TGACTGTGAACGTTCGAGATGA-3′[1][2].
Lipoteichoic acid, a cell wall component of Staphylococcus aureus, activates the complement system via C3 induction and CD55 inhibition[1].
AT791 is a novel orally available, small molecule inhibitor of TLR7 and TLR9 with IC50 of 3.33 uM and 0.04 uM respectively, inhibits DNA-TLR9 interaction in vitro; shows weak activity against TLR4 (IC50>10 uM); potently inhibits IL-6 production induced by CpG2216 and suppresses both IL-6 and α-interferon production induced by CpG oligo.
Bromfenac sodium is a potent and orally active inhibitor of COX, with IC50s of 5.56 and 7.45 nM for COX-1 and COX-2, respectively. Bromfenac sodium is a brominated non-steroidal anti-inflammatory/analgesic drug (NSAID), and it is commonly used for the research of postoperative inflammation and pain following cataract surgery, and pseudophakic cystoid macular edema (CME)[1][2].
COX-2-IN-5 (compound 11a) is a potent COX-2 inhibitor with an IC50 value of 0.65 µM. COX-2-IN-5 has the potential for the research of inflammation[1].
KYN-101 (KYN101) is a potent, selective synthetic antagonist of aryl hydrocarbon receptor (AHR) with IC50 of 22 nM in human HepG2 DRE-luciferase reporter assay and 23 nM in murine Hepa1 Cyp-luc assay.KYN-101 reverses IDO/TDO-mediated tumor progression and improves the efficacy of PD-1 blockade in B16 IDO tumor-bearing mice, as well as CT26 colorectal cancer model expressing endogenous high levels of IDO.
4-Methylhistamine (hydrochloride) is a potent, high affinity H4 receptor agonist Ki of 7 nM. 4-Methylhistamine (hydrochloride) displays more than 100-fold selectivity over other human histamine receptor subtypes[1].
Zaltidine(CP-57361) is a H2-receptor antagonist, which has the antisecretory action.IC50 Value: Target: H2 receptorin vitro:in vivo: In eight healthy male volunteers single oral doses of 5 mg, 25 mg and 100 mg produced dose-related inhibition of basal and pentagastrin-stimulated acid output (M.A.O.) with an estimated ID50 of 40 mg for the latter. In eight subjects with duodenal ulceration single 100 mg and 200 mg doses produced 85% and 97% inhibition of M.A.O. at peak (3 h post-dose) and 20% and 23% inhibition at 24 h, respectively; inhibition of basal acid output was 97% at 3 h and 50% at 24 h with both doses [1]. One hundred and thirty-five patients were randomly allocated to 4 weeks' treatment with either 150 mg zaltidine once daily or placebo. Fifty-nine were treated for a full 4 weeks with zaltidine before the trial was stopped. Healing rates after 4 weeks of zaltidine and placebo were 86% and 19%, respectively (p less than 0.001) [2].
YM-1 is a stable and soluble MKT-077 (HY-15096) analog and an orally active Hsp70 inhibitor. YM-1 induces cell death of HeLa cells and up-regulates the level of p53 and p21 proteins[1][2].
MHP is an activator of sphingosine kinase (SPHK1), and significantly stimulates CAMP mRNA and protein production in KC.