WY-47766, a proton pump inhibitor, is used potentially for the treatment of postmenopausal osteoporosis.
AB-506 is a small-molecule inhibitor targeting HBV core protein, inhibits viral replication in vitro (IC50=77 nM).AB-506 binds to HBV core protein, accelerates capsid assembly and inhibits HBV pgRNA encapsidation.AB-506 blocks cccDNA establishment in HBV-infected HepG2-hNTCP-C4 cells and primary human hepatocytes, leading to inhibition of viral RNA, HBsAg, and HBeAg production (EC50=0.64-1.52 uM).AB-506 demonstrated activity across HBV genotypes A-H and maintains antiviral activity against nucleostide analog-resistant variants in vitro.AB-506 showed an 8 to 20-fold increase in EC50 values against L30F, L37Q, and I105T substitutions.AB-506 exhibits good oral bioavailability, systemic exposure, and higher liver to plasma ratios in rodents.
cFMS Receptor Inhibitor II is a CSF1R kinase inhibitor. CSF-1 is a cytokine[1].
ACAT-IN-10 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor extracted from patent EP1236468A1, example 197. ACAT-IN-10 weakly inhibits NF-κB mediated transcription[1].
Oxolamine citrate is a cough suppressant.
NSC117079 is a novel PHLPP inhibitor.
ODN 1585 is a potent inducer of IFN and TNFα production. ODN 1585 is a potent stimulator of NK (natural killer) function. ODN 1585 increases CD8+ T-cell function, including the CD8+ T cell-mediated production of IFN-γ. ODN 1585 induces regression of established melanomas in mice. ODN 1585 can confer complete protection against malaria in mice. ODN 1585 can be used for acute myelogenous leukemia (AML) and malaria research. ODN 1585 can be used as a vaccine adjuvant[1][2][3].
PAR-4 (1-6) amide human is an N-terminal fragment of protease-activated receptor 4 (PAR4). PAR-4 (1-6) amide human induce platelet aggregation[1].
BPR1R024 mesylate is an orally active and selective colony-stimulating factor-1 receptor (CSF1R) inhibitor.BPR1R024 mesylate is the equivalent of BPR1R024 (HY-132935). BPR1R024 has potent CSF1R inhibition activity with an IC50 value of 0.53 nM. BPR1R024 can be used for the research of immuno-oncology[1].
Quercetin pentaacetate could interact with F-protein with lower binding energy and better stability to block viral adhesion. Quercetin pentaacetate interacts with RSV and inhibit the viral adhesion on cell surface[1][2].
Capsiate, as a capsaicin analogue extracted from a non-pungent cultivar of CH-19 sweet red pepper, is an orally active agonist of TRPV1[1].
Phytohemagglutinin (PHA) is a lectin, obtained from the red kidney bean that binds to the membranes of T-cells, stimulates metabolic activity, cell division, and involves inflammatory pathways. Phytohemagglutinin (PHA) induces apoptosis via increasing proapoptotic protein Bax and activating caspases-3[1][2][3].
Brompheniramine ((±)-Brompheniramine) is a potent and orally active antihistamine of the alkylamine class. Brompheniramine is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research[1][2][3][4].
Swertisin, a C-glucosylflavone isolated from Swertia japonica, is known to have antidiabetic, anti-inflammatory and antioxidant effects. Swertisin is an adenosine A1 receptor antagonist[1][2].
Saccharin sodium hydrate is an orally active, non-caloric artificial sweeteners (NAS). Saccharin sodium hydrate has bacteriostatic and microbiome-modulating properties[1].
7β,25-Dihydroxycholesterol is an endogenous metabolite and is found to act as chemoattractants for immune cells expressing EBI2[1].
Nepafenac(AHR 9434; AL 6515; Nevanac) is a selective COX-2 inhibitor; is prodrug of Amfenac.IC50 value:Target: COX-2Nepafenac is a NSAID (nonsteroidal anti inflammatory drug) that is routinely used in opthamology to control pain following cataract surgery.
Cinchonain IIa is an antioxidant agent with EC50s of 6.8 μM and 26.5 μM for DPPH and PMS-NADH[1].
TYK2-IN-2 is an inhibitor of TYK2, used for treatment of inflammatory and autoimmune diseases.
U-73122 is an inhibitor of phospholipase C (PLC), phospholipase A2, and 5-LO (5-lipoxygenase).
ODN 105871, a G-modified inhibitory oligonucleotide (INH-ODN), is a selective TLR7 inhibitor. ODN 105871 can be uesd for inflammatory immune responses research[1].
6,4'-Dihydroxy-7-methoxyflavanone, a flavonoid, is a nature product that could be isolated from Heartwood Dalbergia odorifera. 6,4'-Dihydroxy-7-methoxyflavanone inhibits receptor activators of nuclear factor kappa-B ligand (RANKL) induced osteoclastogenesis. 6,4'-Dihydroxy-7-methoxyflavanone has antioxidant, anti-inflammatory and neuroprotective effects. 6,4'-Dihydroxy-7-methoxyflavanone can be used in research of osteoporosis[1].
Fmoc-Thr(GalNAc(Ac)3-β-D)-OH inhibits cancer cell growth, through targeting intricate cancer-specific pathways while simultaneously strengthening immunologic response[1].
Antibacterial agent 41 (example 3) is a antibacterial agent (extracted from patent WO2013030735A1)[1].
Deuruxolitinib (CTP-543), a deuterated Ruxolitinib, modulates the activity of JAK1/JAK2. Deuruxolitinib can be used for the research hair loss disorders (from patent WO2017192905A1, compound I)[1].
Pam3CSK4 is a toll-like receptor 1/2 (TLR1/2) agonist with an EC50 of 0.47 ng/mL for human TLR1/2[1].
Protopine hydrochloride, an isoquinoline alkaloid, is a specific reversible and competitive inhibitor of acetylcholinesterase. Protopine hydrochloride exhibits anti-inflammation, anti-microbial, anti-angiogenic and anti-tumour activity[1][2].
PF-3845 is a selective fatty acid amide hydrolase (FAAH) inhibitor (Ki = 0.23 μM); showing negligible activity against FAAH2.IC50 value: 0.23 uMTarget: FAAHPF-3845 selectively inhibits FAAH by carbamylating FAAH's serine nucleophile [1]. PF-3845 treated mice (10 mg/kg, i.p.) shows rapid and complete inactivation of FAAH in the brain, as judged by competitive activity-based protein profiling (ABPP) with the serine hydrolase-directed probe fluorophosphonate (FP)-rhodamine. PF-3845 shows a long duration of action up to 24 hour. PF-3845-treated mice also shows dramatic (>10-fold) elevation in brain levels of AEA and other NAEs (N-pamitoyl ethanolamine [PEA] and N-oleoyl ethanolamine [OEA]). FAAH is AEA-degrading enzyme fatty acid amide hydrolase. PF-3845 (1–30 mg/kg, oral administration [p.o.]) causes a dose dependent inhibition of mechanical allodynia with a minimum effective dose (MED) of 3 mg/kg (rats are analyzed at 4 hour post dosing with PF-3845). At higher doses (10 and 30 mg/kg), PF-3845 inhibits pain responses to an equivalent, if not greater, degree than the nonsteroidal anti-inflammatory drug naproxen (10mg/kg, p.o.) [1]. PF-3845 (10 mg/kg, i.p.) significantly reverses LPS-induced tactile allodynia, but doesn't modify paw withdrawal thresholds in the saline-injected paw [2].
Tenidap, a non-steroidal anti-inflammatory drug, is a selective COX-1 inhibitor, with IC50 values of 0.03 µM and 1.2 µM for COX-1 and COX-2, respectively. Tenidap has anti-inflammatory and antirheumatic properties[1][2].
Tyrphostin 25 (AG82) is a specific inhibitor of the EGFR tyrosine kinase. Tyrphostin 25 is also a GPR35 agonist with an IC50 of 0.94 µM and an EC50 of 5.3 µM[1][2].