Coppersensor-1 (CS1) is a boron dipyrromethene (BODIPY)-based fluorescent sensor for selective and sensitive detection of copper(I) ions (Cu+) in biological samples, including live cells[1].
4,5-Diaminofluorescein is a fluorescent detector for nitric oxide (NO) in cells and tissues[1].
5-Fluorocytidine is a member of cytidines, inhibits maturation of the 45S ribosomal RNA precursor[1].
Lumateperone Tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a SERT blocker (Ki = 61 nM). IC50 value: 0.54 nM (Ki, for 5-HT2A receptor )Target: 5-HT2A receptorLumateperone also possesses affinity for the D1 receptor (Ki = 52 nM) and weak affinity for the α1A- and α1B-adrenergic receptors (Ki = 173 nM at α1) and D4 receptor. Lumateperone does not significantly bind to the 5-HT2B, 5-HT2C, H1, or mACh receptors. Lumateperone shows a 60-fold difference in its affinities for the 5-HT2A and D2 receptors, which is far greater than that of most or all existing atypical antipsychotics, such as risperidone (12-fold), olanzapine (12.4-fold), and aripiprazole (0.18-fold).[1]in vivo: It is thought that this property may improve the effectiveness and reduce the side effect profile of Lumateperone relative to currently-available antipsychotics, a hypothesis which is supported by the observation of minimal catalepsy in mice treated with Lumateperone.[1]
17:0-22:4 PE-d5 is deuterium labeled 17:0-22:4 PE.
DBCO-N-bis(PEG4-NHS ester) is a PEG linker which contains two PEG4-NHS ester and a DBCO group. DBCO-N-bis(PEG4-NHS ester) is useful for protein modification or labeling.
Fursultiamine is a vitamin B1 derivative.
D-Galactosyl-β-1,1'-N-tridecanoyl-D-erythro-sphingosine-d7 is deuterium labeled D-Galactosyl-β-1,1'-N-tridecanoyl-D-erythro-sphingosine.
BR102910 is a selective fibroblast activation protein (FAP) inhibitor with the IC50 of 2 nM. BR102910 also inhibits prolyl oligopeptidase (PREP) with the IC50 of 49.00 μM. BR102910 can be used for the researchof type 2
Nec-4, a tricyclic derivative, is a potent receptor interacting protein 1 (RIP1) inhibitor, with an IC50 of 2.6 μM, Ki of 0.46 μM.
Condurango glycoside E is a glycoside compound that can be isolated from the bark extract of Marsdenia cundurango[1].
NK007 is a novel anti-SARS-CoV-2 agent with an EC50 value of 30 nM.
NS9283 is a positive positive allosteric modulator of (α4)3(β2)2 nicotinic ACh receptors. NS9283 can be used in a series of neurological conditions such as attention deficit hyperactivity disorder (ADHD), schizophrenia, Parkinson's disease and Alzheimer's disease[1].
p97-IN-1 is a potent p97 inhibitor with an IC50 <30 nM (WO2015109285A1, compound FF07)[1].
(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
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.
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.
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.
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.
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].
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.