(R)-BPO-27 is a potent CFTR inhibitor with an IC50 of 4 nM.
Valspodar is a P-glycoprotein (P-gp) inhibitor widely used as overcoming multidrug resistance modulator.
Dabigatran etexilate mesylate (BIBR 1048MS) is the orally active prodrug of dabigatran. Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI) with Ki value of 4.5 nM.IC50 Value: 4.5 nM (Ki); 10 nM(Thrombin-induced platelet aggregation) [1]in vitro: Dabigatran selectively and reversibly inhibited human thrombin(Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC(50): 10 nM), while showing no inhibitory effect on other platelet-stimulating agents.Thrombin generation in platelet-poor plasma (PPP), measured as the endogenous thrombin potential (ETP) was inhibited concentration-dependently (IC(50): 0.56 microM). Dabigatran demonstrated concentration-dependent anticoagulant effects in various species in vitro, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) and ecarin clotting time (ECT) in human PPP at concentrations of 0.23, 0.83 and 0.18 microM, respectively [1]. in vivo: Dabigatran prolonged the aPTT dose-dependently after intravenous administration in rats (0.3, 1 and 3 mg/kg) and rhesus monkeys (0.15, 0.3 and 0.6 mg/kg). Dose- and time-dependent anticoagulant effects were observed with dabigatran etexilate administered orally to conscious rats (10, 20 and 50 mg/kg) or rhesus monkeys (1, 2.5 or 5 mg/kg), with maximum effects observed between 30 and 120 min after administration, respectively [1]. Patients treated with dabigatran etexilate experienced fewer ischaemic strokes (3.74 dabigatran etexilate vs 3.97 warfarin) and fewer combined intracranial haemorrhages and haemorrhagic strokes (0.43 dabigatran etexilate vs 0.99 warfarin) per 100 patient-years [2].Clinical trial: An Evaluation of the Pharmacokinetics and Pharmacodynamics of Oral Dabigatran Etexilate in Hemodialysis Patients . Phase1
SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.IC50 value: 9.0(pKi) [1]Target: 5-HT2C antagonistin vitro: SB 242084 had over 100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors. In studies of 5-HT-stimulated phosphatidylinositol hydrolysis using SH-SY5Y cells stably expressing the cloned human 5-HT2C receptor, SB 242084 acted as an antagonist with a pKb of 9.3, which closely resembled its corresponding receptor binding affinity [1].in vivo: SB 242084 potently inhibited m-chlorophenylpiperazine (mCPP, 7 mgkg i.p. 20 min pre-test)-induced hypolocomotion in rats, a model of in vivo central 5-HT2C receptor function, with an ID50 of 0.11 mg/kg i.p., and 2.0 mg/kg p.o. SB 242084 (0.1-1 mg/kg i.p.) exhibited an anxiolytic-like profile in the rat social interaction test, increasing time spent in social interaction, but having no effect on locomotion. SB 242084 (0.1-1 mg/kg i.p.) also markedly increased punished responding in a rat Geller-Seifter conflict test of anxiety, but had no consistent effect on unpunished responding [1].
Tyrosinase-IN-5 (compound 16c) is a potent inhibitor of tyrosinase with an IC50 of 0.02 μM. Tyrosinase-IN-5 efficiently suppresses the melanogenesis without significant toxicity on cells[1].
Caesalmin E is a natural cassane furanoditerpene with anti-Para3 (Parainfluenza virus type 3) virus activities[1].
CG-806 is a pan FLT3/BTK Multi-Kinase inhibitor.
4,5-Dimethoxybenzene-1,2-diamine 4,5-Dimethoxybenzene-1,2-diamine can be used as a standard for the determination of methyldiacetaldehyde, an intermediate product of glycolysis and a diabetic ketone Biomarkers of acidosis[1].
Odoratone (Dehydroodoratol) has insecticidal activity (LC50: 154 ppm)[1].
Dimethylurea/citric acid is a highly efficient deep eutectic solvent (DES). Dimethylurea/citric acid can be used as a catalyst and a green reaction medium for the synthesis of bis(indolyl)methanes, quinolines and aryl-4, 5-diphenyl-1H-imidazoles.
Neopuerarin B is an isoflavones isolated from the water extraction of the dried roots of Pueraria lobata (Willd.). Neopuerarin B shows significant hepatoprotective effect[1].
Dehydroabietic acid possesses antiviral activity[1].
UNC-1062 is a potent and selective Mer kinase inhibitor with IC50 of 1.1 nM, Ki of 0.33 nM; shows improved selectivity and activity against Mer relative to other TAM family RTKs (78-fold selectivity over Axl and 36-fold over Tyro3); inhibits Mer auto-phosphorylation in human pre-B leukemia 697 cells with IC50 of 6.4 nM, also inhibits colony formation in soft agar in tumor cells.
SP-Chymostatin B is a potent inhibitor of many proteases, including chymotrypsin, papain, chymotrypsin-like serine proteinases, chymases, and lysosomal cysteine proteinases. It weakly inhibits human leucocyte elastase. It is effective at a final concentration of 100 to 200 μg/ml (10 to 100 μM).
AG-1557, compound 22 (T), is a ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase with a pIC50 value of 8.194[1].
Medronic Acid (Methylenediphosphonic acid) is a methylene-substituted bisphosphonate. Medronic acid has affinity for and adheres to the surface of hydroxyapatite crystals in the bone matrix. This agent accumulates at sites of osteoid mineralization and can be used, complexed with radioisotopes in bone imaging.
Butin is a major biologically active flavonoid isolated from the heartwood of Dalbergia odorifera, with strong antioxidant, antiplatelet and anti-inflammatory activities. Butin significantly alleviates myocardial infarction and improves heart function, together with prevents diabetes-induced cardiac oxidative damage in rat[1][2].
CCT241161 is an orally active pan-RAF inhibitor with IC50s of 3, 6, 10, 15 and 30 nM for LCK, CRAF, SRC, V600E-BRAF and BRAF, respectively. CCT241161 shows good activity to in BRAF and NRAS mutant melanomas. CCT241161 also exhibits anticancer cell proliferative activity[1].
3-Maleimidobenzoic acid N-hydroxysuccinimide ester is used as asymmetric spacers[1].
(Rac)-Azide-phenylalanine is a racemate of Azide-phenylalanine. Azide-phenylalanine is a phenylalanine derivative and a non-natural amino acid. Azide-phenylalanine can be site-specifically incorporated into proteins and used to label proteins[1].
Hellebrigenol is a metabolite of bufadienolides with antitumor activity[1].
IR5790 is a herbicide. IR5790 strongly inhibits protoporphyrinogen oxidase with an IC50 of 3 nM[1].
DMX-129 is an ΙΚΚε and TBK-1 inhibitor with IC50 values of <30 nM for both TBK1 and IKKε[1].
AHR antagonist 5 free base is a selective and orally active aryl hydrocarbon receptor (AHR) inhibitor. AHR antagonist 5 free base effectively blocks AHR from translocating from the cytoplasm to the nucleus. AHR antagonist 5 free base is highly selective for AHR over other receptors, transporters, and kinases[1].
Biotin-PEG8-Me-Tet is a biotin labeling.
Stachyose is a prebiotic, a non-reducing tetrasaccharide in the rafnose family of oligosaccharides with few side efects.
Nelonicline (ABT-126) citrate is an orally active and selective α7 nicotinic receptor agonist with high affinity to α7 nAChRs in human brain (Ki=12.3 nM). Nelonicline citrate is used for the research of shizophrenia and Alzheimer's disease[1][2][3].
Phenformin (1-phenethylbiguanide) is an orally active antidiabetic and anticancer agent. Phenformin has an incidence of associated lactic acidosis. Phenformin acts through acting AMPK activation and blocking mTOR pathway. Phenformin is also a substrate of P-glycoprotein (P-gp), and an OXPHOS inhibitor. Phenformin induces cancer cell apoptosis[1][2].
11β-HSD1-IN-7 (compound c10a) is a 11β‑HSD1 inhibitor with an IC50 value of 1.9 μM for human 11β‑HSD1. 11β-HSD1-IN-7 can be used for the research of diabetes and cognitive decline[1].