Beta-glucuronidase is an important lysosomal enzyme involved in the degradation of glucuronate-containing glycosaminoglycan[1].
IMM-H007 is a potent TGFβ1 (transforming growth factor β1) antagonist. IMM-H007 has protective effects in cardiovascular diseases via activation of AMPK (AMP-activated protein kinase). IMM-H007 negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling. IMM-H007 inhibits ABCA1 degradation. IMM-H007 resolves hepatic steatosis in HFD-fed hamsters by the regulation of lipid metabolism. IMM-H007 can be used for the research of nonalcoholic fatty liver disease (NAFLD) and inflammatory atherosclerosis[1][2][3].
Edoxaban M4, an active metabolite of Edoxaban, shows reproducible, but concentration-dependent matrix effects. Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor [1][2].
AVE5688 is an inhibitor of glycogen phosphorylase (GP), with IC50s of 430 nM and 915 nM and Kds of 170 nM and 530 nM for rabbit muscle glycogen phosphorylase (rmGPb and rmGPa, respectively); AVE5688 can be used for the research of type 2 diabetes.
Auriculin B (Atrial natriuretic peptide (126-150)(rat)) is a rat-derived atrial natriuretic peptide. Auriculin B has potent vasodilatory and diuretic properties[1].
Bococizumab (PF-04950615) is an anti-human PCSK9 inhibitory antibody that reduces LDL cholesterol levels. Bococizumab can be used in the research of hypercholesterolemia[1][2].
Gastric Inhibitory Peptide (GIP), human is thought to act as an inhibitor of gastric functions.
4-Hydroxyphenylglyoxylate (4-Hydroxyphenylglyoxylic acid) is an inhibitor of carnitine palmitoyltransferase I (CPT I). 4-Hydroxyphenylglyoxylate can be used to study sensitivity changes in CPT I of liver mitochondria and fatty acid oxidation by isolated hepatocytes. 4-Hydroxyphenylglyoxylate can inhibits fatty acid oxidation[1].
D-Tetrahydropalmatine is an isoquinoline alkaloid, mainly in the genus Corydalis[1]. D-Tetrahydropalmatine is a Dopamine (DA) receptor antagonist with preferential affinity toward the D1 receptors[2]. D-Tetrahydropalmatine is a potent organic cation transporter 1 (OCT1) inhibitor[3].
SMP-028 is an inhibitor of neutral cholesterol esterase (CEase), with an IC50 of 1.01 μM.
A8SGLP-1 is an orally active GLP-1 analogue that the alanine at position 8 substituted with serine. A8SGLP-1 reduces blood glucose in db/db mice without affecting its function[1].
rel-O-2050 (Compound O-2050) is a neutral cannabinoid CB1 receptor antagonist. rel-O-2050 also decreases food intake in mice[1].
Torsemide is a pyridine-sulfonyl urea type loop diuretic.Target: OthersTorasemide is a pyridine-sulfonylurea type loop diuretic mainly used in the management of edema associated with congestive heart failure. It is also used at low doses for the management of hypertension. Torsemide significantly reduced total HF readmissions (relative risk [RR]: 0.41, 95% CI: 0.28-0.61, p < 0.0001) and HF readmissions (RR: 0.53, 95% CI: 0.33-0.84, p = 0.008) as well as CV readmissions (RR: 0.77, 95% CI: 0.60-0.98, p = 0.03) in patients with "at least 1 readmission." Torsemide caused a 14% reduction in all-cause mortality (RR: 0.86 [0.53-1.39], p = 0.54). Torsemide significantly reduces HF and CV-related hospital readmissions in systolic HF. Furthermore, torsemide is associated with a trend in reducing all-cause mortality [1]. Torsemide has several characteristics that make it suitable for treatment of advanced heart failure including longer half-life, increased potency of diuretic action, and anti-aldosterone effects. This case report details the administration of torsemide in 3 dogs with advanced heart failure and apparent furosemide resistance [2].
ZLN024 is an AMPK allosteric activator. ZLN024 directly activates recombinant AMPK α1β1γ1, AMPK α2β1γ1, AMPK α1β2γ1 and AMPK α2β2γ1 heterotrimer with EC50s of 0.42 µM, 0.95 µM, 1.1 µM and 0.13 µM, respectively.
Aflibercept (VEGF Trap) is a soluble decoy VEGFR constructed by fusing the Ig domains of VEGFR1 and VEGFR2 with the Fc region of human IgG1. Aflibercept inhibits VEGF signaling by reducing VEGF-regulated processes. Aflibercept can be used for thr research of age-related macular degeneration (AMD) and cardiovascular disease[1][2][3].
Demethylcantharidate disodium, an endogenous metabolite, induces apoptosis in hepatocellular carcinoma cells via ER stress. Demethylcantharidate disodium shows excellent anticancer activity against multiple types of cancer[1].
Glutarylcarnitine is the diagnostic metabolite for malonic aciduria and glutaric aciduria type I monitored in most tandem mass spectrometry newborn screening programmes.
Mipomersen (sodium) is a second-generation 20-base phosphorothioate ASO targeted to human apoB-100[1][2].
Afegostat was previously in phase II clinical trials for the treatment of Gaucher's disease. The experiment was discontinued.
Exisulind is an inactive metabolite of the nonsteroidal, anti-inflammatory agent sulindac[1]. Exisulind inhibits aldose reductase with an IC50 of 367 nM in vitro and may contribute to the beneficial pharmacological effects of sulindac on type 2 diabetic complications[2].
4-Methoxybenzimidamide is a reagent used for the determination of reducing carbohydrates and glycoproteins.
Bisindolylmaleimide I (GF109203X) hydrochloride is a cell-permeable and reversible PKC inhibitor (IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I hydrochloride is also a GSK-3 inhibitor[1][2][3].
Sitagliptin phosphate monohydrate is a potent inhibitor of DPP4 with IC50 of 19 nM in Caco-2 cell extracts
Artemisinic acid (Qing Hao acid), an amorphane sesquiterpene isolated from Artemisia annua L., possesses a variety of pharmacological activity, such as antimalarial activity, anti-tumor activity, antipyretic effect, antibacterial activity, allelopathy effect and anti-adipogenesis effect[1].
A71623, a CCK-4-based peptide, is a potent and highly selective CCK-A full agonist. The IC50s for A-71623 are 3.7 nM in guinea pig pancreas (CCK-A) and 4500 nM in cerebral cortex (CCK-B) in radioligand binding assays, respectively[1].
Methocarbamol is a central muscle relaxant used to treat skeletal muscle spasms.Target: Carbonic AnhydraseMethocarbamol is the carbamate of guaifenesin, but does not produce guaifenesin as a metabolite, because the carbamate bond is not hydrolyzed metabolically; metabolism is by Phase I ring hydroxylation and O-demethylation, followed by Phase II conjugation. All the major metabolites are unhydrolyzed carbamates. Methocarbamol is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm [1, 2].
DL-Mevalonolactone ((±)-Mevalonolactone;Mevalolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrial membrane potential (∆Ψm), NAD(P)H content and the capacity to retain Ca2+ in the brain, besides inducing mitochondrial swelling[1][2].
D-Glucose-13C,d-1 is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical si
DMAPP (Dimethylallyl pyrophosphate) is an isoprenoid precursor. DMAPP, as an isomer of isopentenyl pyrophosphate (IPP), exists in virtually all life forms[1].
Enclomiphene ((E)-Clomiphene) hydrochloride is a potent and orally active non-steroidal estrogen receptor antagonist, with antioestrogenic property. Enclomiphene hydrochloride can be used for the research of ovarian dysfunction, testosterone deficiency, male hypogonadism and type 2 diabetes[1].