MCC950 sodium is a potent, selective NLRP3 inhibitor with IC50s of 7.5 and 8.1 nM in BMDMs and HMDMs, respectively.
PF-05241328 is a potent and selective inhibitor of human Nav1.7 voltage-dependent sodium channels (Nav1.7), with an IC50 of 31 nM.
ML233 is a non-peptide based potent apelin receptor (APJ) agonist (EC50=3.7 μM). ML233 displays >21-fold selective over the closely related angiotensin 1 (AT1) receptor (>79 μM)[1].
Hyaluronic acid sodium salt is a biopolymer composed of repeating units of disaccharides with various applications.
Salvianolic acid C is a noncompetitive Cytochrome P4502C8 (CYP2C8) inhibitor and a moderate mixed inhibitor of Cytochrome P45022J2 (CYP2J2), with Kis of 4.82 μM and 5.75 μM for CYP2C8 and CYP2J2, respectively.
Bis-tris propane (BTP) is a water-soluble buffer substance. Bis-tris propane can be used as a suitable buffer for polymerase chain reaction (PCR). Bis-tris propane can enhance the stability or activity of restriction enzymes[1][2].
Tricin 7-O-β-D-glucopyranoside is a potent and orally active neuroprotective agent. Tricin 7-O-β-D-glucopyranoside induces Apoptosis. Tricin 7-O-β-D-glucopyranoside decreases the expression of TNF-α induced phosphor-κB-α, phosphor-NF-κB, HMGB1[1].
ABCG2-IN-2 is a potent ABCG2 inhibitor with favorable oral pharmacokinetic profiles in mice. ABCG2-IN-2 can be used for the research of tumor multidrug resistance (MDR) and erythropoietic protoporphyria (EPP)[1].
Pamidronate disodium, a bisphosphonate drug, can help to strengthen bones.Target: OthersPamidronate belongs to the family of medications known as bisphosphonates. It is used to treat hypercalcemia (high blood calcium) by people who have cancer. Pamidronate is also used to treat cancer that has spread to bones (bone metastases) due to different types of tumours and multiple myeloma (cancer of the bone marrow). Pamidronate is also used to treat the symptoms of Paget's disease of bone.
cDEPMPO is a potent anticancer prodrug. High concentrations of DEPMPO spin-trap the ·OH radical together with aryl radicals arising from one-electron reduced BTO (benzotriazine 1,4-di-N-oxide) compounds[1].
N2-iso-Butyroyl-3’-O-(methoxyethyl)guanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7)[1].
(Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumorassociated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses[1].
20-HETE(20-hydroxy Arachidonic Acid) is a potent vasoconstrictor produced in vascular smooth muscle (VSM) cells. It depolarizes VSM by blocking the open-state probability of Ca2+-activated K+-channels.IC50 Value:Target: 20-Hydroxyeicosatetraenoic acid (20-HETE) is a cytochrome P450-derived arachidonic acid metabolite that has been shown to increase smooth muscle contractions and proliferation, stimulate endothelial dysfunction and activation and promote hypertension. in vitro: Addition of 20-HETE to the bath (1-100 nM), reduced the frequency of opening of the large-conductance Ca(2+)-activated K+ channel recorded using cell-attached patches on VSM [1]. In kidney, 20-HETE induces diuresis by inhibiting Na+-K+-ATPase in proximal tubules and Na+/K+/Cl+ cotransporter in the thick ascending limb of Henle's loop [2].in vivo: In Cyp4a14(-/-) mice, which display androgen-driven and 20-HETE-dependent hypertension, treatment with20-HETE antagonist abolished remodeling of renal resistance arteries measured as media thickness (24±1 vs. 15±1μm) and M/L (0.29±0.03 vs. 0.17±0.01) [4]. The transgenic mice had overexpressed hepatic CYP4F2, high hepatic 20-HETE and fasting plasma glucose levels but normal insulin level. The GP activity was increased and the cAMP/PKA-PhK-GP pathway was activated in the transgenic mice compared with wild-type mice [5]. Clinical trial: Mechanisms of Response to Diesel Exhaust in Subjects With Asthma. Phase not specified
1,4-Dibromobutane-d4 is the deuterium labeled 1,4-Dibromobutane[1].
Elastase from porcine pancreas is a single polypeptide chain of 240 amino acid residues. Elastase from porcine pancreas is a serine protease that can hydrolyze proteins and polypeptide. Elastase from porcine pancreas can induce emphysema in hamsters[1][2][3].
TMB monosulfate is a chromogenic substrate used in staining procedures in immunohistochemistry as well as being a visualizing reagent used in enzyme-linked immunosorbent assays (ELISA).
[Nle13]-Motilin, a motilin analogue, is a motilin receptor agonist[1][2].
ICI 199441 is a potent and selective κ-opioid receptor agonist. ICI 199441 can improve heart resistance to ischemia/reperfusion[1].
Cromolyn sodium is an antiallergic drug.Target: Calcium ChannelCromolyn sodium is a chromone complex that acts by inhibiting the release of chemical mediators from sensitized mast cells. It is used in the prophylactic treatment of both allergic and exercise-induced asthma, but does not affect an established asthmatic attack.Pretreatment of IIR mice with Cromolyn sodium prior to ischemia exhibited no changes of ET-1 levels, injury score and inflammation (P>0.05, PreCr vs. M groups). In conclusion, administration of Cromolyn sodium after reperfusion, but not prior to ischemia, attenuates IIRI by downregulating ET-1 and suppressing sustained MC activation [1]. cromolyn sodium has a role in the prevention of Chronic lung disease(CLD). Cromolyn sodium cannot be recommended for the prevention of CLD in preterm infants [2].
MES-d13 is the deuterium labeled MES[1]. MES (2-Morpholinoethanesulphonic acid) is a buffering agent in biology and biochemistry. MES is one of the Good's buffers, the buffer capacity ranging pH 5.5-7.0. MES is broadly used to regulate pH value for plants culture medium, reagent solution, and physiological experiments[2][3].
(+)-Menthyl acetate is a compound isolated from natural Cunila angustifolia Benth essential oil. The selectivity of (+)-Menthyl acetate is higher than that of MCF-7 cell line, IC50=34.0 μg?mL-1, and lower than that of SK-Mel-28 cell line, IC50=279.9 μg?mL-1, on A549 cell without fatal [1].
Akt inhibitor-IV (AKTIV) acts as a PI3K-Akt inhibitor at the E isomer (HY-14971), with potent cytotoxicity[1].
R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.IC50 value: 2.5 nM [1]Target: ALK5in vitro: R-268712 is a novel and specific inhibitor of activin receptor-like kinase 5 (ALK5), a transforming growth factor β (TGF-β) type I receptor. R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM, an approximately 5000-fold more selectivity for ALK5 than p38 mitogen-activated protein kinase (MAPK). R-268712 is a weak inhibitor of p38 MAP kinase (IC50: 12.1 μM).[1]in vivo: Oral administration of R-268712 at doses of 1, 3 and 10 mg/kg also inhibited the development of renal fibrosis in a dose-dependent manner in a unilateral ureteral obstruction (UUO) model. [1]
Nonadecanoic acid is a 19-carbon long saturated fatty acid. Nonadecanoic acid is the major constituent of the substance secreted by Rhinotermes marginalis to defence[1].
Fluconazole (mesylate) is a triazole antifungal drug used in the treatment and prevention of superficial and systemic fungal infections.Target: AntifungalFluconazole (mesylate) is the mesylate salt form of fluconazole, which is a triazole antifungal intended for oral treatment of superficial and systemic mycoses. In tests done in standard mycological media, the compound had minimal inhibitory concentrations against pathogenic Candida species that were usually in excess of 100 mg/l. Fluconazole inhibited branching and hyphal development in C. albicans at concentrations as low as 10(-6) M (0.3 mg/l), but miconazole and ketoconazole were still active in these tests at concentrations 100 times lower than this [1]. Oral fluconazole was not associated with a significantly increased risk of birth defects overall or of 14 of the 15 specific birth defects of previous concern. Fluconazole exposure may confer an increased risk of tetralogy of Fallot [2]. Fluconazole is predicted to be ineffective against Cryptococcus gattii in the koala as a sole therapeutic agent administered at 10 mg/kg p.o. every 12 h [3].Clinical indications: Balanitis; Candida infection; Cryptococcus infection; Cryptococcus neoformans meningitis; Dermatomycosis; Female genital tract infection; Fungal infection; Fungal respiratory tract infection; Fungal urinary tract infection; Prophylaxis; Tinea capitis; Tinea corporis; Tinea cruris; Tinea pedis .Toxicity: Symptoms of overdose include hallucinations and paranoid behavior.
Z-Phe-(4-F)-OH is a phenylalanine derivative[1].
PU-139 is a potent, unselective HAT (Histone acetyltransferase) inhibitor that blocks the HATs Gcn5, p300/CBP-associated factor (PCAF), CREB protein (CBP) and p300; triggers caspase-independent cell death in cell culture, blocks growth of SK-N-SH neuroblastoma xenografts in mice, and synergizes the effect of doxorubicin in vivo.
6-O-Caffeoylarbutin (Robustaside B) possesses antioxidant activity[1].
L-Cystine-3,3'-13C2 is the 13C labeled L-Cystine[1]. L-Cystine is an amino acid and intracellular thiol, which plays a critical role in the regulation of cellular processes[2].
VU0810464 (VU 0810464, VU464) is a selective neuronal GIRK channels activator, displays nanomolar potency for GIRK1/2 (EC50=163 nM) and improved brain penetration; exhibits comparable efficacy and potency compared with ML297, but VU0810464 is more selective for neuronal GIRK channels (GIRK1/4 EC50>500 nM); displays >3-fold more potent on GIRK1/2-expressing HEK293 cells compared to GIRK1/4-expressing cells, as measured using a Tl+ flux assay; reduced stress-induced hyperthermia in a GIRK-dependent manner in mice, ML297, but not VU0810464, decreased anxiety-related behavior as assessed with the elevated plus maze test.