Nifedipine is a potent calcium channel blocker and drug of choice for cardiac insufficiencies.
Olmesartan is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure.
MPP+ iodide, a toxic metabolite of the neurotoxin MPTP, causes symptom of Parkinson's disease in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ iodide is taken up by the dopamine transporter into dopaminergic neurons where it exerts its neurotoxic action on mitochondria by affecting complex I of the respiratory chain. MPP+ iodide is also a high affinity substrate for the serotonin transporter (SERT)[1][2].
2'-Deoxycytidine-13C9,15N3 (Deoxycytidine-13C9,15N3; Cytosine deoxyriboside-13C9,15N3; Deoxyribose cytidine-13C9,15N3) is 13C and 15N-labeled 2'-Deoxycytidine (HY-D0184). 2'-Deoxycytidine, a deoxyribonucleoside, could inhibit biological effects of Bromodeoxyuridine (Brdu).
QL-IX-55 is a selective ATP-competitive inhibitor of mTORC1/2 with IC50s of 50/50/10-50 nM for Human mTORC1/Yeast mTORC1/Yeast mTORC2, respectively.
Biotin-C2-maleimide is an antibody conjugate reagent, can bind to many biomolecules without significantly changing the biological activity of the target molecule[1][2].
9-Decen-1-ol is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
1,4-Dibromo-butane-1,1,2,2,3,3,4,4-d8 is the deuterium labeled 1,4-Dibromo-butane[1].
Cathepsin L-IN-3 is a tripeptide-sized cathepsin L inhibitor.
Lupulone is a beta-acid from the hop plant H. lupulus with diverse biological activities including antibacterial, antioxidant, and anticarcinogenic properties[1][2][3].
Falcarinol (Panaxynol) is a natural, orally active Hsp90 inhibitor targeting both the N-terminal and C-terminal of Hsp90 with limited toxicities. Falcarinol (Panaxynol) induces apoptosis[1].
Glucocerebrosidase Glucosylceramidase; GCase is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
TP0586532 is a non-hydroxamate LpxC inhibitor (IC50=0.101 μM). TP0586532 as a compound with a low cardiovascular risk that is effective against K. pneumoniae, including resistant strains[1].
GBR-12879 dihydrochloride is a potent inhibitor of dopamine uptake[1].
3-aminopiperidine-2-one is a metabolite from all living organisms. 3-aminopiperidine-2-one is a delta-lactam that is 2-piperidone substituted at position 3 by an amino group.
Succinyl phosphonate trisodium salt (SP) is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts[1][4].Succinyl phosphonate trisodium salt (SP) is an 2-Oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner[2].Succinyl phosphonate trisodium salt (SP) inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ[3].
Benalaxyl is a fungicide. Benalaxyl has good control of blue mould (Peronospora tubacina)[1].
Antiviral agent 5 is an intermediate used in antiviral agents targeting 3C and 3CL proteases including SARS-CoV-2 Mpro.
11beta-Hydroxyprogesterone is a potent inhibitors of 11β-Hydroxysteroid dehydrogenase; also activates human mineralocorticoid receptor in COS-7 cells with an ED50 of 10 nM.
Pancreatic Polypeptide, rat is an agonist of NPY receptor, with high affinity at NPYR4.
Protectin D1, neuroprotectin D1 when generated by neural cells, is a member of a new family of bioactive products generated from docosahexaenoic acid. Protectin D1 is also a specialized pro-resolving mediator with potent pro-resolving and anti-inflammatory effects in vivo in several human disease models[1][2].
Lamivudine 13C,15N2 is a labelled impurity of Lamivudine (BCH-189). Lamivudine is a nucleoside reverse transcriptase inhibitors (NRTIs), and can inhibit HIV reverse transcriptase 1/2 and the reverse transcriptase of hepatitis B virus[1][2].
N-ε-propargyloxycarbonyl-L-lysine hydrochloride is a modified amino acid (L-lysine) for cancer therapy development[1].
Chamaechromone is a biflavonoid ingredient isolated from the roots of Stellera chamaejasme L. (Thymelaeaceae). Chamaechromone possesses anti-hepatitis B virus (HBV) effects against the surface antigen of HBV (HBsAg) secretion and has insecticidal activities[1].
Hydroxyfasudil is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.
Dabigatran etexilate(BIBR-1048) 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
RXFP1 receptor agonist-6 (Example 7) is a RXFP1 receptor agonist. RXFP1 receptor agonist-6 inhibits cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 12 nM[1].
Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
O4I2 is a potent Oct3/4 inducer in various human cell lines including human fibroblasts.Target: Oct3/4O4I2 activates Oct3/4 in HEK293 and embryonal NCCIT cells, and also in Oct-deficient HeLa and terminally differentiated human fibroblasts. O4I2 activates also other pluripotencyassociatedgenes such as Lin28 and Nanog in a drug-like manner. O4I2 shows high activity in enforcing Oct3/4 expression. O4I2 activates Oct3/4 on the transcriptional and translational level in human fibroblasts. O4I2 promotes the expression of pluripotency-associated genes as analyzed by qRT-PCR in human neonatal foreskin fibroblasts (HFFs). O4I2 markedly stimulates Oct3/4 even at 5 μM after 72 h treatment on the translational level.
Glucosamine (hydrochloride) is a natural product.IC50 value:Target:In vitro: Glucosamine hydrochloride exhibited dose-dependent DPPH antioxidant activity [1]. Short-term (4 h) glucosamine hydrochloride treatment inhibited HIF-1α at the protein level, decreased phosphorylation of p70S6K and S6, translation-related proteins [2]. In the obstructed kidneys and TGF-β1-treated renal cells, glucosamine hydrochloride significantly decreased renal expression of α-smooth muscle actin, collagen I, and fibronectin [3]. In vivo: