Bromodiphenhydramine hydrochloride is a potent antihistamine with antimicrobial property. Bromodiphenhydramine hydrochloride inhibits a large number of Gram negative and Gram positive bacteria. Bromodiphenhydramine hydrochloride can be used for cutaneous allergies research[1][2][3].
Immepip is a H3 agonist. Immepip can reduce cortical histamine release. Immepip can be used for the research of neurological diseases[1].
Desloratadine-d5 is deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities[1][2].
GT-2016 is a potent, selective, and brain penetrant histamine H3 receptor antagonist with a Ki of 43.8 nM. GT-2016 displays selectivity against H1 and H2 receptors, and has non-active against histamine methyltransferase[1].
(S)-Flurbiprofen is an active enantiomer of Flurbiprofen, with IC50 values of 0.48 μM and 0.47 μM for COX-1 and COX-2, respectively[1].
4-Methylamino antipyrine hydrochloride is an active metabolite of Metamizole. Metamizole is a pyrazolone non-steroidal anti-inflammatory drug (NSAID) and inhibits COX. Metamizole is an nonopioid analgesic drug and can be used for pain and fever[1][2][3]. 4-Methylamino antipyrine hydrochloride has analgesic, antipyretic, and relatively weak antiinflammatory properties[2].
Corydalmine (L-Corydalmine), an alkaloid isolated from roots of Corydalis Chaerophylla, inhibits spore germination of some plant pathogenic as well as saprophytic fungi[1]. Corydalmine acts as an oral analgesic agent, exhibiting potent analgesic activity[2]. Corydalmine alleviates Vincristine-induced neuropathic pain in mice by inhibiting an NF-κB-dependent CXCL1/CXCR2 signaling pathway[3].
MAHMA NONOate is a NO donor. MAHMA NONOate effectively inhibits platelet aggregation induced by either collagen or ADP[1].
MLN3126 (MLN 3126, MLN-3126) is a potent, selective, orally available CCR9 antagonist with IC50 of 6.3 nM (CCL25-induced calcium mobilization); shows no significant antagonistic activity for other 12 chemokine receptors (CCR1, -2b, -4, -6, -7, -8, -10,CX3CR1, CXCR1, -2, -3 and -4) at 10 uM; dose dependently inhibits CCL25-induced chemotaxis of mouse thymocytes (IC90=1.8 uM); ameliorates inflammation in a T cell mediated mouse colitis model. Other Indication Phase 1 Discontinued
STING-IN-7 (compound 21) is a potent STING inhibitor with an IC50 of 11.5 nM. STING-IN-7 inhibits the phosphorylation of STING and interferon regulatory factor 3 (IRF3)[1].
Pembrolizumab is a humanized antibody inhibiting the programmed cell death 1 (PD-1) receptor, used in cancer immunotherapy.
ZK756326 dihydrochloride is a nonpeptide chemokine receptor agonist for the CC chemokine receptor CCR8.
Methylthiouracil is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2.
Oxyphenbutazone is a phenylbutazone derivative, with anti-inflammatory effect. Oxyphenbutazone is a non-selective COX inhibitor. Oxyphenbutazone selectively kills non-replicating Mycobaterium tuberculosis[1][2].
CDN-A is a cyclic di-nucleotide, it can be used to synthesis antibody-drug conjugate (ADC). Cyclic di-nucleotides are potent stimulators of innate and adaptive immune responses. In humans, cyclic di-nucleotide, which are either produced endogenously in response to foreign DNA or by invading bacterial pathogens, trigger the innate immune system by activating the expression of interferon genes[1][2][3].
JNJ-5207852 is a selective and potent histamine H3 receptor (H3R) antagonist, with pKis of 8.9, 9.24 for rat and human H3R, respectively.
SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM[1]. SK1-I shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I enhances autophagy and has antitumor activity[2].
PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy[1][2][3].
Mulberroside A, the major active anti-tyrosinase compound in the root bark extract of Morus alba L. (Moraceae), is widely employed as an active ingredient in whitening cosmetics. IC50 value: 1.29 μmol/L (inhibition of the monophenolase activity); KI value: 0.385 μmol/L (the inhibition constant of the effectors on tyrosinase); KIS value: 0.177 μmol/L (the inhibition constant of the enzyme-substrate complex) [3] Target:In vitro: Mulberroside A decreased the expressions of tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, and IL-6 and inhibited the activation of NALP3, caspase-1, and nuclear factor-κB and the phosphorylation of extracellular signal-regulated protein kinases, the c-Jun N-terminal kinase, and p38 exhibiting anti-inflammatory antiapoptotic effects [1]. Mulberroside A treatment significantly decreased the mRNA and protein expression of P-gp in Caco-2 cells after treatment with Mulberroside A (5–20 μM). PKC and NF-κB might play crucial roles in Mulberroside A-induced suppression of P-gp [2]. In vivo:
CCX140 is a potent CCR2 antagonist.
MeBIO is a potent AhR (aryl hydrocarbon receptor) agonist, with IC50 of 44 μM (GSK-3) and 55 μM (CDK1/cyclin B), respectively. MeBIO is inactive on GSK-3β[1].
Mizolastine dihydrochloride is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions. Target: Histamine H1-receptorMizolastine is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions. It does not prevent the actual release of histamine from mast cells, just prevents it binding to receptors. Side effects can include dry mouth and throat.Mizolastine has demonstrated antiallergic effects in animals and healthy volunteers and anti-inflammatory activity in animal models. Double-blind trials have shown mizolastine to be significantly more effective than placebo and as effective as other second generation antihistamine agents, such as loratadine or cetirizine, in the management of patients with perennial or seasonal allergic rhinitis and in patients with chronic idiopathic urticaria. Available data also suggest that prophylactic administration of mizolastine is significantly more effective than placebo and as effective as prophylactic terfenadine in delaying the onset of symptoms of seasonal allergic rhinitis.
IRAK4-IN-15 (compound 35) is a potent and selective IRAK4 inhibitor with an IC50 of 0.002 µM. IRAK4-IN-15 shows good human PK predictions with low intrinsic clearance. IRAK4-IN-15 shows great synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib. [1].
Retifanlimab is an anti-programmed cell death protein 1 (anti-PD-1) monoclonal antibody (mAb). Retifanlimab can be used for the research of gastroesophageal adenocarcinoma (GEA)[1].
[8]-Shogaol, one of the pungent phenolic compounds in ginger, exhibits anti-platelet activity (IC50=5 μM) and inhibits COX-2 (IC50=17.5 μM). [8]-Shogaol induces apoptosis in human leukemia cells[1][2][3][4].
AN-3485 is a benzoxaborole analog, Toll-Like Receptor(TLR) inhibitor with IC50 values ranging from 18 to 580 nM.
AZD 1678 is a potent, selective orally bioavailable CCR4 receptor antagonist with pIC50 of 8.6 for hCCR4, pIC50 of 9.0 for rCCR4; shows no significant activity against a panel of chemokine receptors (CXCR1, CXCR2, CCR1, CCR2b, CCR5, CCR7, CCR8; inactive at 10 uM); inhibits Th2 cell CCL22 driven chemotaxis in 0.3% HSA with pIC50 of 6.8. Asthma Phase 1 Clinical
Lafutidine, a newly developed histamine H(2)-receptor antagonist, inhibits gastric acid secretion.Target: histamine H(2)-receptorLafutidine, a newly developed histamine H(2)-receptor antagonist, inhibits gastric acid secretion.It is currently marketed in Japan (Stogar) China (Lemeiting) and India (Lafaxid). It not only suppresses gastric acid secretion, but also has cytoprotective properties by the virtue of its property to induce the collagen synthesis in the gastric mucosa. It has a novel mechanism of action in addition to blocking the H2 receptors, it decreases inflammation by modulating calcitonin gene-related peptide (CGRP) and vanilloid receptors. It is also found to stimulate mucin biosynthesis and promote the restitution of damaged mucosa.Lafutidine is absorbed in the small intestine, reaches gastric cells via the systemic circulation, and then directly and rapidly binds to gastric cell histamine H2 receptors, thereby inhibiting the stimulation of cAMP and a resultant decrease in acid production (antisecretory action). It causes a sustained increase in intracellular Ca2+ ion concentration in endothelial cells resulting in the release of Calcitonin Gene Related Peptide (CGRP), which causes acid suppression by decreasing the vagal tone. Lafutidine also increases plasma somatostatin levels which decreases secretion of gastrin from G cells. This decrease in gastrin causes inhibition of parietal cells, resulting in decrease in gastric acid secretion.
PD-1/PD-L1-IN 6 (compound A13) is a potent PD-1/PD-L1 interaction inhibitor, with an IC50 of 132.8 nM. PD-1/PD-L1-IN 6 exhibits outstanding immunoregulatory activity. PD-1/PD-L1-IN 6 significantly elevates interferon-γ secretion in a Hep3B/OS-8/hPD-L1 and CD3 T cell co-culture model, without significant toxic effect. PD-1/PD-L1-IN 6 restores the immune response in a T cell-tumor co-culture model[1].
Oxidized ATP (oATP) trisodium salt is a broad-spectrum P2 receptor inhibitor. Oxidized ATP trisodium salt irreversibly antagonizes P2X7R activation. Oxidized ATP trisodium salt inhibits c-reactive protein (CRP)-induced NLRP3 inflammasome activation. Oxidized ATP trisodium salt can be used for research of atherosclerosis[1][2].