SCH 42495 is an orally active neutral metalloendopeptidase (NEP) inhibitor with antihypertensive effect. SCH 42495 is the orally active ethylester prodrug of SCH 42354[1].
p53-MDM2-IN-1 (Example 30) is an inhibitor of p53-MDM2/X protein interaction with an Ki value of 23.35 µM. p53-MDM2-IN-1 can be used for anti-tumor research[1].
Prudomestin, isolated from the heartwood of Prunus domestica, shows potent xanthine oxidase (XO) inhibitory activity (IC50≈6 µM)[1][2].
Dicoumarol is an inhibitor of both NAD(P)H:quinone oxidoreductase 1 (NQO1) and PDK1 with IC50s of 0.37 and 19.42 μM, respectively.
IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT, respectively[1]. Anticancer activity[1].
Memantine, an amantadine derivative with low to moderate-affinity for NMDA receptors, inhibit CYP2B6 and CYP2D6 with Ki of 0.51 nM and 94.9 μM, respectively..Target: NMDA Receptor, Memantine (Ebixa, Axura, Namenda, Akatinol) is a moderate-affinity, uncompetitive, voltage-dependent, NMDA-receptor antagonist with fast on/off kinetics that inhibits excessive calcium influx induced by chronic overstimulation of the NMDA receptor. Memantine is approved in the US and the EU for the treatment of patients with moderate to severe dementia of the Alzheimer's type [1]. Memantine has considerable therapeutic potential for the myriad of clinical entities associated with NMDA receptor-mediated neurotoxicity [2]. Memantine blocked 200 microM NMDA-evoked responses with a 50% inhibition constant (IC50) of approximately 1 microM at -60 mV and an empirical Hill coefficient of approximately 1 [3].
N-Methylbenzamide is a potent phosphodiesterase 10A (PDE10A) inhibitor. N-Methylbenzamide has anti-cancer activity[1][2].
JNJ-10311795 (RWJ-355871), a potent dual inhibitor of neutrophil cathepsin G (Ki = 38 nM) and mast cell chymase (Ki = 2.3 nM), exhibits noteworthy antiinflammatory activity[1].
Hs-27 is a Novel Hsp90 Inhibitor, Exhibits Diagnostic and Therapeutic Potential in Triple Negative Breast Cancer.
Araloside A (Chikusetsusaponin IV) is a component of Panax japonicus, with low-renin-inhibitory activity, with an IC50 of 77.4 μM[1].
DG051 is a potent leukotriene A4 hydrolase inhibitor of leukotriene B4 biosynthesis in the enzyme assay with an IC50=47 nM.
β-Apo-8'-carotenal (Apocarotenal), a provitamin A carotenoid, is an inducer of CYPlA1 and CYPlA2 in rat. β-Apo-8'-carotenal is present in many fruits and vegetables[1].
Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells.
Gly-β-MCA, a bile acid, is a potent, sable, intestine-selective and oral bioactive farnesoid X receptor (FXR) inhibitor that may be a candidate for the treatment of metabolic disorders[1].
hCAI/II-IN-4 (compound 6d) is a potent dual hCA I/II inhibitor with Ki values of 16.95, 15.22 and 27.04 nM for hCA I, hCA II and hCA Ⅸ, respectively. hCAI/II-IN-4 has anti-hypoxia activities and low toxicity. hCAI/II-IN-4 can be used for acute mountain sickness (AMS) research[1].
Reproterol is a dual acting β2-adrenoceptor agonist and PDE inhibitor. The theophylline constituent of Reproterol inhibits phosphodiesterase activity induced by adenylyl cyclase. Reproterol has the potential for asthma research[1][2].
Fotagliptin is a Dipeptidyl Peptidase IV (DPP-4) inhibitor (IC50=2.27 nM). Fotagliptin displays great security in rat and dog. Fotagliptin can be used for Type 2 diabetes mellitus research[1].
Garadacimab (CSL312) is a first-in-class, fully human IgG4 monoclonal antibody targeting activated factor XII (FXIIa). Garadacimab has the potential for hereditary angioedema research[1].
FASN inhibitor 1 is a fatty acid synthase (FASN) inhibitor extracted from patent US20170119786A1, compound 242A.
Iristectorigenin B (Iristectrigenin B) is a liver X receptor (LXR) modulator. Iristectrigenin B stimulates the transcriptional activity of both LXR-α and LXR-β[1].
Fuzapladib sodium (IS-741 sodium) is a potent and orally active phospholipase A2 inhibitor. Fuzapladib sodium can block the adhesion of inflammatory cells to microvascular endothelial cells, inhibits the infiltration of neutrophils into the pancreas or acute pancreatitis, and has anti-acute pancreatitis effects[1][2].
ALP/Carbonic anhydrase-IN-1 (Compound 1e) is a dual carbonic anhydrase (CA) and alkaline phosphatase (ALP) inhibitor. ALP/Carbonic anhydrase-IN-1 shows IC50 values of 0.44 µM, 1.61 µM, 0.51 µM, and 0.107 µM for CA-II, CA-IX, CA-XII, and ALP, respectively[1].
Dihydromethysticin is one of the six major kavalactones found in the kava plant; has marked activity on the induction of CYP3A23.
SMER3, a Rapamycin enhancer, is a selective Skp1-Cullin-F-box (SCF)Met30 ubiquitin ligase inhibitor. SMER3 enhances Rapamycin's growth inhibitory effect by inhibition of SCFMet30[1].
Grazoprevir potassium salt (MK-5172 potassium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
Acitretin sodium(Ro 10-1670) is a second-generation, systemic retinoid that has been used in the treatment of psoriasis.Target: RAR/RXRAcitretin sodium is a second-generation, systemic retinoid that has been approved for the treatment of psoriasis since 1997. It can be considered one of the treatments of choice for pustular and erythrodermic psoriasis. However, the efficacy of acitretin sodium as a monotherapy for plaque psoriasis is less, although it is often used in combination therapy with other systemic psoriasis therapies, especially ultraviolet B or psoralen plus ultraviolet A phototherapy, to increase efficacy. Such combination treatments may potentially minimise toxicity by using lower doses of each of the two agent [1].Thirty-nine male adult Wistar albino rats were divided into 3 groups as two experimental groups and one control group. The first group consisting 14 rats were applied orally standard dose (0.75 mg/kg/day) acitretin sodium and the second group consisting 16 rats were applied high dose (1.5 mg/kg/day) acitretin sodium. Acitretin sodium was given within dimetil sulphoxide (DMSO), which was diluted with saline solution as a ratio of 1/10, in order to increase its solubility. The control group consisting 9 rats were given only saline solution including DMSO for 8 weeks. After 8 weeks of the administration, half of the rats in the first and second groups and the entire control group were sacrificed under deep ether anaesthesia and bilateral orchiectomy was made. The remainingrats were compared with the control group using a similar method at the end of 8 weeks of wash-off period. The orchiectomy materials were histopathologically evaluated under the light microscope for spermatogenesis according to parameters including spermatogenetic activity, spermatogenetic organization, seminiferous tubular diameter, interstitial Leydig cells and fibroblasts. In our study it was concluded that the standard and high doses of acitretin sodium do not have any effect on the spermatogenesis of threats [2].Clinical indications: PsoriasisFDA Approved Date: Toxicity: nausea; headache; itching; red or flaky skin; dry or red eyes; dry mouth; depression; hair loss
ML148 is a potent and selective 15-PGDH inhibitor with an IC50 of 56 nM. ML148 has the potential for the research of prostaglandin-signaling pathways[1].
Saterinone hydrochloride is a phosphodiesterase III (PDE III) inhibitor.
SR3335 is a selective RORα synthetic ligand, directly binds to RORα (Ki 220 nM) but not other RORs, and functions as a selective partial inverse agonist of RORα in cell-based assays.
RV01 is an analogue of resveratrol, inhibits DNA damage, reduces acetaldehyde dehydrogenase 2 (ALDH2) mRNA expression induced by ethanol, and exhibits hydroxyl radical scavenging activity[1]. RV01 decreases iNOS expression, with anti-neuroinflammatory activity[2].