Cefprozil (Cefzil) is a second-generation cephalosporin type antibiotic[1].
Guaiacol-d7 is the deuterium labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Randaiol is an antioxidant that can be isolated from the stem bark of Magnolia officinalis. Randaiol inhibits LPS-induced NO production and has anti-inflammatory and antioxidant activities[1].
Cedirogant (ABBV-157) is an orally active RORγt inverse agonist. Cedirogant can be used for psoriasis research[1][2].
IL-17A inhibitor 2 is an IL-17A inhibitor for treating psoriasis, rheumatoid arthritis, and multiple sclerosis.
GENZ-882706 is a potent colony stimulating factor-1 receptor (CSF-1R) Inhibitor extracted from patent WO 2017015267A1.
STING-IN-4 (Compound 1) is a STING inhibitor that inhibits STING expression and hence reducing activation of STING and nuclear factor-κB (NF-κB) signaling. STING-IN-4 shows anti-inflammatory activity and can be used for the research of sepsis[1].
Hydroxyzine Dihydrochloride is a histamine H1-receptor antagonist.Target: Histamine H1-ReceptorHydroxyzine inhibits carbachol (10 μM)-induced serotonin release by 34% at 10 μM, by 25% 1 μM and by 17% 0.1 μM in pretreated bladder slices for 60 min [1]. Hydroxyzine (0.1 mM) treatment inhibits the progression and severity of EAE by 50% and the extent of mast cell degranulation by 70% in Lewis rats with allergic encephalomyelitis (EAE) [2]. Hydroxyzine (500 M) significantly increases transport of etoposide to the serosal site in the jejunal everted sacs. Hydroxyzine significantly reduces the efflux and approximately 2.4 g/mL of etoposide in the jejunum and ileum. Hydroxyzine (0.2 μg/mL) significantly enhances the efflux of RH123 to the lumen [3].Hydroxyzine (500 μM) significantly decreases the steady-state etoposide concentration 2-fold, where the steady-state concentration reached about 0.055 μM/mL in Sprague-Dawley rats [3]. Hydroxyzine (12.5 mg/kg, 25 mg/kg and 50 mg/kg i.p.) shows little direct analgesic activity but markedly potentiates only the effect of morphine on the vocalization after-discharge which represents the affective component of pain in rats. Hydroxyzine (50 mg/kg i.p.) potentiates morphine on the tail-flick test, while Hydroxyzine (12.5 mg/kg i.p.) decreases morphine antinociception in rats [4].
Anagrelide Hydrochloride(BL4162A) is a drug used for the treatment of essential thrombocytosis.Target: PDEAnagrelide hydrochloride is an oral imidazoquinazoline agent that has been shown to reduce elevated platelet counts and the risk of thrombosis in patients with thrombocythaemia in various myeloproliferative disorders (MPD). It is currently approved by the FDA as oral treatment for essential thrombocythaemia (ET) and thrombocythaemia associated with polycythaemia vera (PV). Anagrelide is known to inhibit platelet cyclic adenosine monophosphate (cAMP) phosphodiesterase at concentrations that exceed those achieved at doses used to treat ET. Anagrelide is extensively metabolised in the liver and its metabolites are primarily excreted in the urine [1]. Anagrelide is an established platelet-reducing drug. Studies have also investigated the effects of anagrelide on platelets, indicating that platelet function is as important as platelet counts in ET [2].
Warangalone is an anti-malarial compound which can inhibit the growth of both strains of parasite 3D7 (chloroquine sensitive) and K1 (chloroquine resistant) with IC50s of 4.8 μg/mL and 3.7 μg/mL, respectively. Warangalone can also inhibit cyclic AMP-dependent protein kinase catalytic subunit (cAK) with an IC50 of 3.5 μM.
(Rac)-Indoximod (1-Methyl-DL-tryptophan) is an indoleamine 2,3-dioxygenase (IDO) inhibitor. Co-treatment with IFN-γ and (Rac)-Indoximod markedly reduces the activity of human cardiac myofibroblasts (hCMs) expressing α-SMA and induces apoptosis through up-regulating the IRF-1, Fas, and FasL genes[1].
Adapalene sodium salt(CD 271; Differin), a synthetic retinoid, is a Retinoic acid receptor agonist (RAR).Target: Retinoic acid receptor agonist (RAR)Adapalene sodium salt is a third-generation topical retinoid primarily used in the treatment of mild-moderate acne and is also used (off-label) to treat keratosis pilaris as well as other skin conditions. Adapalene sodium salt is possibly more effective than tretinoin 0.025% gel in the treatment of acne vulgaris [1].Thirty-six rats of either sex were divided into six groups (two control groups, and an etodolac, indomethacin, tretinoin and adapalene sodium salt group) of six animals each. Each group was given different drugs or chemicals. The inhibitory activities of the drugs were determined on carrageenan-induced rat-paw oedema. The inhibition rate (53.48%) in the tretinoin group was found to be higher than adapalene sodium salt and controls (P < 0.05). Adapalene sodium salt was found to have an inhibition rate of 10.28%, and when compared with the other groups, was found to have no statistically significant anti-inflammatory activity [2].Clinical indications: Acne; Purpura; SunburnFDA Approved Date: 1996Toxicity: Skin redness; dryness; itching; scaling; mild burning
(S)-Ketorolac is a nonsteroidal anti-inflammatory agent. (S)-ketorolac exhibits potent COX1 and COX2 enzyme inhibition[1].
Asperulosidic Acid (ASPA), a bioactive iridoid glycoside, is extracted from the herbs of Hedyotis diffusa Willd. Asperulosidic Acid (ASPA) has anti-tumor, anti-oxidant, and anti-inflammatory activities[1].ASPA is related to the inhibition of inflammatory cytokines (TNF-α, IL-6) and mediators via suppression of the NF-κB and mitogen-activated protein kinase (MAPK) signaling pathways[2].
N-cis-Feruloyl tyramine (cis-N-(4-Hydroxyphenethyl) ferulamide) is a natural phenolic compound, exhibits modest inhibitory activity on LPS-activated NO production in RAW 264.7 cells[1].
Methyl 3,4-dihydroxybenzoate (Protocatechuic acid methyl ester;Methyl protocatechuate) is a major metabolite of antioxidant polyphenols found in green tea. Antioxidant and anti-inflammatory effect[1].
ChemR23-IN-1 (compound 2) is a ChemR23 inhibitor with IC50s of 38 nM and 100 nM for human and mouse ChemR23, respectively. ChemR23-IN-1 inhibits chemotaxis of CAL-1 triggered by Chemerin in vitro[1].
ATL-801, an A2B receptor selective antagonist, ameliorates murine colitis[1].
TCJL37 is a potent, selective, and orally bioavailable TYK2 inhibitor with a Ki of 1.6 nM. TCJL37 can be used for the research of inflammatory bowel diseases (IBD)[1].
Suberosin, isolated from Plumbago zeylanica, exhibits anti-inflammatory and anticoagulant activity. Suberosin suppresses PHA-induced PBMC proliferation and arrested cell cycle progression from the G1 transition to the S phase through the modulation of the transcription factors NF-AT and NF-κB[1][2].
(-)-Integerrimine, a pyrrolizidine alkaloid, has antiulcerogenic activity. (-)-Integerrimine is also a mutagenic and weakly clastogenic agent in Drosophila[1][2].
Sorbicillin, a sorbicillinoid analogue, acts as a potent anti-inflammation agent[1].
Pennogenin is a bioactive component which can be isolated from T. govanianum rhizomes. Pennogenin exhibits significant in vitro inhibitory effect on release of ROS[1].
AC-264613 is a potent and selective protease-activated receptor (PAR-2) agonist with a pEC50 of 7.5[1].
λ-Carrageenan is a seaweed polysaccharide which has been generally used as proinflammatory agent in the basic research. λ-Carrageenan is a potent antitumor agent[1].
Rebamipide mofetil is an orally active prodrug of Rebamipide (OPC12759). Rebamipide is a mucoprotective agent. Rebamipide induces COX-2 expression, increases PGE2 levels, and enhances gastric mucosal defense in a COX-2-dependent manner[1].
Inuviscolide is an apoptosis inducer. Inuviscolide can induce of G2/M arrest in human melanoma cell lines. Inuviscolide exhibits antineoplastic and anti-inflammatory activities[1][2][3].
Pheniramine (Prophenpyridamine;Tripoton) is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine displays antitumor effect and induces leukemia cells apoptosis. Pheniramine is also a safe and effective local anesthetic, with antipruritic effects[1][2][3][4].
Traumatic Acid is a monounsaturated dicarboxylic acid isolated from Phaseolus vulgaris. Traumatic Acid can cause a decrease in membrane phospholipid peroxidation and show antioxidant and stimulatory effects on collagen biosynthesis. Traumatic Acid is a potential agent for the treatment of many skin diseases connected with collagen biosynthesis disorders and oxidative stress[1].
AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes[1][4]. AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro[2]. AZD7325 has the potential for the investigation of anxiety and dravet syndrome[3]. PAM: positive allosteric modulator.