Nogapendekin alfa is a superagonist of IL-15. Nogapendekin alfa promotes the proliferation and viability of immune cells. Nogapendekin alfa combines with Inbakicept (HY-P99661) at a ratio of 2:1, to form ALT-803, an IL-15 cytokine antibody fusion protein. ALT-803 reduces tumor burden by activation of NK cells and CD8+ T cells[1].
Hydroxyzine pamoate 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 ug/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].
Oxazolone is a haptenizing agent that induces acute or chronic inflammation of the large intestine and is used to construct models of colitis. Oxazolone can cause Th1/Th2-dependent colitis with weight loss and diarrhea. Oxazolone-induced inflammation can be mitigated by neutralizing anti-IL-4 or anti-TNF-α antibodies or decoy IL-13R2-α-FC proteins[1].
Betahistine is an orally active histamine H1 receptor agonist and a H3 receptor antagonist[1]. Betahistine is used for the study of rheumatoid arthritis (RA)[3].
Desmethyl Celecoxib (compound 3b) is a selective cyclooxygenase-2 (COX-2) inhibitor (IC50=32 nM) with anti-inflammatory activities. Desmethyl Celecoxib is an analog of Celecoxib and with the optimal yield of 75%[1].
L-156602 is a C5a receptor antagonist. L-156602 inhibits inflammation, and the migration of monocytes and neutrophils to the infiltrating site in mouse inflammatory models. L-156602 suppresses the efferent phase of delayed-type hypersensitivity (DTH)[1][2].
2-Aminoquinoline is a promising compound as bioavailable nNOS inhibitor but suffers from low human nNOS inhibition, low selectivity versus human eNOS, and significant binding to other CNS targets. 2-Aminoquinoline has the potential for the research of antineurodegenerative agents[1].
Cimetidine sulfoxide (Cimetidine sulphoxide) is a sulfoxide metabolite of Cimetidine. Cimetidine is a histamine H2-receptor antagonist. Cimetidine has the potential for peptic ulcer disease and upper gastrointestinal haemorrhage treatment[1].
Curvularin, a fungal metabolite and a potent mycotoxin naturally isolated from Curvularia lunata, inhibits cytokine-induced nitric oxide synthase (iNOS), with an IC50 of 9.5 µM[1][2].
Dovanvetmab (ZTS-00521505) is an IgG1-κ antibody targeting Felcat IL31. Mainly expressed by CHO (Chinese Hamster Ovary) cells[1].
Ketotifen (fumarate) is a second-generation noncompetitive H1-antihistamine and mast cell stabilizer, which is used to prevent asthma attacks.Target: Histamine Receptor Ketotifen is a second-generation noncompetitive H1-antihistamine and mast cell stabilizer. It is most commonly sold as a salt of fumaric acid,ketotifen fumarate, and is available in two forms. In its ophthalmic form, it is used to treat allergic conjunctivitis, or the itchy red eyes caused by allergies. In its oral form, it is used to prevent asthma attacks. Side effects include drowsiness, weight gain, dry mouth, irritability, and increased nosebleeds.Ketotifen relieves and prevents eye itchiness and/or irritation associated with most seasonal allergies. It starts working within minutes after administering the drops. The drug has not been studied in children under three. The mean elimination half life is 12 hours. Besides its anti-histaminic activity, it is also a functional leukotriene antagonist and a phosphodiesterase inhibitor. The drug may also help relieve the symptoms of Irritable bowel syndrome.
Imsidolimab (ANB 019) is a high-affinity, humanized monoclonal antibody of anti-IL-36R. Imsidolimab antagonizes IL-36 cytokine signal transduction. Imsidolimab has potential application in generalized pustular psoriasis (GPP) and other inflammatory skin diseases[1][2].
Maraviroc is a selective CCR5 antagonist with activity against human HIV.
Guselkumab is a recombinant human IgG1 monoclonal antibody against the IL-23p19 subunit. Guselkumab binds to human and cynomolgus monkey IL-23 with Kd values of 3.3 and 1.9 pmol/L, respectively. Guselkumab inhibits production of cytokines lying downstream of the IL-23 signaling pathway and can be used for psoriatic arthritis research[1].
Dibenzo(a,i)pyrene is a 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) receptor ligand[1].
Methapyrilene (Thenylpyramine) hydrochloride is an orally active H1-receptor antihistamine and an anticholinergic agent of the pyridine chemical class. Methapyrilene hydrochloride has hepatotoxicity and can be used as a hepatotoxin that cause periportal hepatic necrosis in vivo[2]
SC-236 is an orally active COX-2 specific inhibitor (IC50 = 10 nM) and a PPARγ agonist. SC-236 suppresses activator protein-1 (AP-1) through c-Jun NH2-terminal kinase. SC-236 exerts anti-inflammatory effects by suppressing phosphorylation of ERK in a murine model[1][2][3][4][5].
Nifeviroc is an orally active CCR5 antagonist. Nifeviroc is used for the study of HIV type-1 infection[1].
N'-Nitro-D-arginine (NOLA), a nitric oxide synthesis inhibitor, also is a vasodilator that relaxes the smooth muscles and increases blood flow to the penis, improving erections. N'-Nitro-D-arginine also inhibits neutrophil migration by blocking receptors for tumour necrosis factor alpha (TNFα) and interleukin 8 (IL8) [1].
Bifarcept is a recombinant antibody of interferon receptor type I (IFN-RI). Bifarcept can bind IFN-β and prolong its serum half-life[1].
Thonzylamine is an orally active H1 histamine receptor antagonist, exhibits good antihistaminic and antianaphylactic properties. Thonzylamine can be used for the research of hypersensitivity diseases, nasal congestion, allergic conjunctivitis and other allergic diseases[1][2].
Clemastine Fumarate is a selective histamine H1 receptor antagonist with IC50 of 3 nM.Target: Histamine H1 ReceptorClemastine Fumarate inhibits histamine induced rise in [Ca2+]i in HL-60 cells with an IC50 of 3 nM as compared with that of chlorpheniramine or diphenhydramine with IC50 values of 20 nM and 100 nM, respectively [1]. Clemastine showed a first-pass reduction in the extent of absorption, with oral bioavailability calculated as 39.2 +/- 12.4%. Extravascular distribution of drug was suggested by the high volume of distribution (799 +/- 315 L) and low Cmax (0.577 +/- 0.252 ng/mL/mg) observed at 4.77 +/- 2.26 hours after administration, and by the biphasic decline in plasma concentration. The terminal elimination half-life (t1/2) of clemastine was 21.3 +/- 11.6 hours. Steady-state concentrations of clemastine were consistent with linear pharmacokinetic processes, and clearance was unaffected by age in the range studied, or by race [2].
Imrecoxib (BAP-909) is a novel and selective cyclooxygenase 2 (COX-2) inhibitor with an IC50 value of 18 nM, it also inhibits COX1- activity with an IC50 value of 115 nM. Imrecoxib (BAP-909) has anti-inflammatory effect[1].
Kaempferol 3-O-β-D-glucuronide (Kaempferol-3-glucuronide), one conjugated kaempferol metabolite, has anti-inflammatory effect. Kaempferol 3-O-β-D-glucuronide significantly inhibits various pro-inflammatory mediators like IL-1β, NO, PGE2, and LTB4. Kaempferol 3-O-β-D-glucuronide upregulates the secretion of anti-inflammatory cytokine IL-10[1][2].
Cyclic di-GMP (c-di-GMP) diammonium is a STING activator and a global bacterial second messenger, which regulates biofilm formation, motility, and virulence in diverse bacterial species[1][2].
Nodinitib-1 (ML130;CID-1088438) is a NOD1 inhibitor with an IC50 of 0.56 μM.
Leronlimab (PRO 140) is a humanized IgG4 anti-CCR5 monoclonal antibody. Leronlimab inhibits CCR5-mediated HIV-1 viral and lung metastasis in mouse tumor models. Leronlimab can be used for the research of HIV nonalcoholic steatohepatitis (NASH) and cancer[1].
PMX 205 is a potent complement C5a receptor (C5aR; CD88) antagonist.
MK-886 (L 663536) sodium salt is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 sodium salt is also a non-competitive PPARα antagonist and can induce apoptosis[1][2][3].
Ravulizumab (ALXN1210) is a humanized monoclonal antibody that specifically binds with high affinity to the human complement protein C5. Ravulizumab can be used for the research of paroxysmal nocturnal hemoglobinuria, atypical hemolytic uremic syndrome, and myasthenia gravis[1].