Ocedurenone is a corticosteroid receptor antagonist. Ocedurenone can be used for the research of kidney disease (WO2018054357, compound I)[1].
Aclacinomycin A (Aclarubicin) is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A is an inhibitor of topoisomerase I and II. Aclacinomycin A inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis[1][2][3].
Biochanin A is a naturally occurring fatty acid amide hydrolase (FAAH) inhibitor, which inhibits FAAH with IC50s of 1.8, 1.4 and 2.4 μM for mouse, rat, and human FAAH, respectively.
Fenvalerate is a potent protein phosphatase 2B (calcineurin) inhibitor with an IC50 of 2-4 nM for PP2B-Aα. Fenvalerate is a pyrethroid ester insecticide and acaricide[1].
PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.IC50 value: 19 nM [1]Target: DGAT1PF-04620110 and imipramine (internal standard) were separated using a Hypersil Gold C18 column, with a mixture of acetonitrile and 10 mm ammonium formate (90:10, v/v) as the mobile phase. The ion transitions monitored in positive-ion mode [M + H](+) of multiple-reaction monitoring were m/z 397.0 -260.2 for PF-04620110 and m/z 280.8 - 86.0 for imipramine. The detector response was specific and linear for PF-04620110 at concentrations within the range 0.05-50 μg/mL and the signal-to-noise ratios for the samples were ≥10 [2].
β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol[1][2][3].
ML-030 is a potent PDE4 inhibitor, with IC50 of 6.7 nM, 12.9 nM, 48.2 nM, 37.2 nM, 452 nM and 49.2 nM for PDE4A, PDE4A1, PDE4B1, PDE4B2, PDE4C1,and PDE4D2, respectively.
(-)-Talarozole is a potent inhibitor of retinoic acid metabolism extracted from patent WO 1997049704 A1.
Lipiferolide is an antiplasmodial agent (IC50: 1.8 μg/mL) that can be isolated from Liriodendron tulipifera. Lipiferolide also inhibits FPTase, and has antitumor activity[1][2].
Chalepensin, a furanocoumarin, is a competitive CYP2A6 inhibitor. Chalepensin also inhibits human CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 to different extents[1].
Homo Sildenafil-d5 is the deuterium labeled Homo Sildenafil. Homo Sildenafil, an analog of Sildenafil, acts as a phosphodiesterase inhibitor[1][2].
Rodatristat ethyl (KAR5585) is an orally active tryptophan hydroxylase 1 (TPH1) inhibitor with nanomolar in vitro potency. Rodatristat ethyl reduces the level of 5-HT and significantly reduces pulmonary arterial hypertension (PAH)[1][2].
Stigmasterol glucoside is a sterol isolated from P. urinaria with high antioxidant and anti-inflammatory activities[1], act as an inhibitor of 5α-reductase with an IC50 of 27.2 µM[2].
C12 NBD sphingomyelin is an active derivative of sphingomyelin (HY-113498) that is tagged with fluorescent C12 nitrobenzoxadiazole (C12 NBD). C12 NBD sphingomyelin can be used as a sphingomyelinase substrate for studying the metabolism and transport of sphingomyelins (Ex=470 nm, Em=525 nm)[1].
Tectol, isolated from Lippia sidoides, exhibits significant activity against human leukemia cell lines HL60 and CEM[1]. Tectol is a farnesyltransferase (FTase) inhibitor with IC50s of 2.09 and 1.73 μM for human and T. brucei FTase. Tectol inhibits drug-resistant strain of P. falciparum (FcB1) with an IC50 of 3.44 μM[1][2].
Chymostatin is a potent cathepsin G inhibitor. Chymostatin inhibits fungal growth when combined with other pepsin inhibitors. Chymostatin can be used for acute lung injury and pancreatitis research[1].
AZD1656 is a potent, selective and orally active glucokinase activator with an EC50 of 60 nM. AZD1656 has the potential for type 2 diabetes research[1][2][3].
CDK2-IN-12 (compound 10b) is a potent CDK2 inhibitor, with an IC50 of 11.6 μM. CDK2-IN-12 inhibits hCA (carbonic anhydrase) isoforms I, II, IX and XII, with KI values of 3534, 638.4, 44.3, and 48.8 nM. CDK2-IN-12 shows anticancer activity[1].
Tauro-β-muricholic acid (TβMCA) is a trihydroxylated bile acid. Tauro-β-muricholic acid is a competitive and reversible FXR antagonist (IC50 = 40 μM). Tauro-β-muricholic acid has antiapoptotic effect. Tauro-β-muricholic acid inhibits bile acid-induced hepatocellular apoptosis by maintaining the mitochondrial membrane potential[1][2].
N-Benzylpalmitamide is a macamide isolated from Lepidium meyenii, acts as an inhibitor of fatty acid amide hydrolase (FAAH).
DHODH-IN-9 (Compound 10k) is an azine-bearing analogue and is a human dihydroorotate dehydrogenase inhibitor. DHODH-IN-9 has antiviral effect with a pMIC50 of 7.4[1].
Enalkiren (A-64662) is a potent dipeptide renin inhibitor with an IC50 of 0.78 nM in a purified renal renin-angiotensinogen system (pH=6.0). Enalkiren suppresses renin activity, and also reduces systolic and diastolic blood pressure. Enalkiren can be used to research essential hypertension[1][2].
Licopyranocoumarin is an isoflavonoid that shows CYP3A4 inhibitory activity with an IC50 of 32 μM. Licopyranocoumarin has potent neuroprotective activities[1].
hCAII-IN-3 (compound 7e) is a potent and selective inhibitor of carbonic anhydrase (CA II/IX) with Kis of 124.2 and 30.5 nM, respectively. hCAII-IN-3 has the potential for the research of cancer diseases[1].
HIF-2α-IN-7 is a hypoxia inducible factor 2α (HIF-2α) inhibitor. HIF-2α-IN-7 can inhibit HIF-2α with an EC50 value of 6nM. HIF-2α-IN-7 can be used for the research of various types of diseases including cancer, liver disease, inflammatory disease, pulmonary diseases and iron load disorders[1].
Cathepsin K inhibitor 3 (compound 23) is a highly selective cathepsin K inhibitor with an IC50 value of 0.5 nM. Cathepsin K inhibitor 3 has a favorable pharmacokinetic profile and may be used in osteoarthritis (OA) disease studies[1].
ethyl ester of Dabigatran, which is an emerging oral anticoagulant which is a direct inhibitor of thrombin activity. IC50 value:Target: thrombinDabigatran provides a stable anticoagulation effect without any need to perform periodical laboratory controls. Of note, there is a growing amount of clinical evidence which shows its safety and efficacy. For these reasons, Dabigatran may suppose a revolution in oral anticoagulation. Dabigatran etexilate was rapidly converted to Dabigatran, with peak plasma dabigatran concentrations being attained after approximately 1.5 h; the bioavailability of Dabigatran after p.o. administration of Dabigatran etexilate was 7.2%.
Mirodenafil(SK3530) is a phosphodiesterase type 5 (PDE-5) inhibitor developed for the treatment of erectile dysfunction.Target: PDE5Mirodenafil is a newly developed oral phosphodiesterase type 5 inhibitor. Mirodenafil, in doses of 50 or 100 mg, significantly improved erectile function and were well tolerated in a representative population of Korean men with broad-spectrum ED of various etiologies and severities [1]. The concurrent administration of mirodenafil with alcohol was not associated with clinically significant hemodynamic changes in these healthy male volunteers in Korea. The pharmacoki-netics of mirodenafil were not significantly altered by this concurrent administration. Mirodenafil administered with alcohol had a tolerability profile comparable to that of mirodenafil alone [2]. In these healthy Korean male volunteers, the coadministration of ketoconazole and rifampicin resulted in significant changes in systemic exposure to mirodenafil [3].
Omapatrilat is a dual inhibitor of the metalloproteases ACE and NEP with Ki values of 0.64 and 0.45 nM, respectively.
CAY10581, a pyranonaphthoquinone derivative, is a highly specific and reversible uncompetitive IDO Inhibitor with an IC50 of 55 nM[1][2].