Disulfamide, an orally active diuretic, is a carbonic anhydrase inhibitor with the IC50 value of 0.07 μM. Disulfamide leads to diuresis by inhibiting carbonic anhydrase and preventing the reabsorption of sodium and bicarbonate in the proximal tubule[1].
3-O-(2-Aminoethyl)-25-hydroxyvitamin D3 is a Vitamin D3 derivative.
3-Phenoxybenzoic acid-13C6 is the 13C6 labeled 3-Phenoxybenzoic acid. 3-Phenoxybenzoic acid is an endogenous metabolite.
Asp-AMS, an analogue of aspartyl-adenylate, is an aspartyl-tRNA synthetase inhibitor and also a strong competitive inhibitor of the mitochondrial enzyme.
Probucol is an anti-hyperlipidemic drug by lowering the level of cholesterol in the bloodstream by increasing the rate of LDL catabolism.Target: OthersProbucol is a drug used to lower LDL and HDL cholesterol yet has little effect on serum-triglyceride or VLDL cholesterol. Probucol inhibited cholesterol efflux up to 80% in J774 macrophages expressing ABCA1. probucol is an effective inhibitor of ABCA1-mediated cholesterol efflux without influencing scavenger receptor class B type I-mediated efflux. The inhibition of ABCA1 translocation to the plasma membrane may in part explain the reported in vivo high-density lipoprotein-lowering action of probucol [1].
L-Leucine-d7 is the deuterium labeled L-Leucine. L-Leucine is an essential branched-chain amino acid (BCAA), which activates the mTOR signaling pathway[1].
Oxonic acid potassium salt is an inhibitor of uricase, oxonic inhibits the phosphorylation of 5-FU to 5-fluorouridine-5'-monophosphate catalyzed by pyrimidine phosphoribosyl-transferase in a different manner from allopurinol in cell-free extracts and intact cells in vitro.IC50 value: Target: On p.o. administration of 5-FU (2 mg/kg) and a potent inhibitor of 5-FU degradation to Yoshida sarcoma-bearing rats, oxonic acid (10 mg/kg) was found to inhibit the formation of 5-fluorouridine-5'-monophosphate from 5-FU and its subsequent incorporation into the RNA fractions of small and large intestine but not of tumor and bone marrow tissues [1]. Oxonic acid diet increased plasma uric acid by 80-90 micromol/l, while blood pressure was elevated only in hyperuricemic 5/6 nephrectomy rats (18 mmHg) [2].
UK-157147 is a substrate for UDP-glucuronosyltransferases (UGT1A1) with a Km value of 105 μM.
Probucol Disuccinate is a derivative of Probucol, a lipid-regulating agent and can reduce LDL-cholesterol levels[1].
GPR120 Agonist 2 is a GPR120 agonist extracted from patent US 20110313003 A1, example 209.
Enclomiphene ((E)-Clomiphene) is a potent and orally active non-steroidal estrogen receptor antagonist, with antioestrogenic property. Enclomiphene can be used for the research of ovarian dysfunction, testosterone deficiency, male hypogonadism and type 2 diabetes[1].
Glucose-6-phosphate dehydrogenase is the rate-limiting enzyme of the pentose phosphate pathway. Glucose-6-phosphate dehydrogenase is a major source of NADPH that is required by many essential cellular systems including the antioxidant pathways, nitric oxide synthase, NADPH oxidase, cytochrome p450 system, and others. Glucose-6-phosphate dehydrogenase can be used for the research of diabetes, aldosterone-induced endothelial dysfunction, and cancer[1].
TfR-T12 is a BBB-penetrated transferrin receptor (TfR) binding peptide, displaying a binding affinity in the nM range[1][2].
EN884 is a BRD4 degrader via a SKP1- and proteasome-dependent manner. EN884 can be used in synthetic proteolysis targeting chimeras (PROTACs)[1].
HM30181 is a potent and selective inhibitor of P-glycoprotein.
5-Heptadecylresorcinol (AR-C17), a phenolic lipid component, is also an orally active mitochondrial protector. 5-Heptadecylresorcinol improves mitochondrial function via sirtuin3 signaling pathway, thus alleviates endothelial cell damage and apoptosis. 5-Heptadecylresorcinol induces sirtuin3-mediated autophagy. 5-Heptadecylresorcinol reduces the atherosclerotic plaques in the aortic root region of mice heart. 5-Heptadecylresorcinol can be used for research of atherosclerosis prevention and obesity[1][2].
Cinnamtannin A2, a tetrameric procyanidin, can increases GLP-1 and insulin secretion in mice. Cinnamtannin A2 could upregulate the expression of corticotrophin releasing hormone. Cinnamtannin A2 exhibits antioxidant, anti-diabetic and nephroprotective effect[1][2].
Amylin (8-37), rat is a truncated analog of native Amylin that selectively inhibits insulin-related glucose uptake and glycogen deposition in muscle tissue. Amylin (8-37), rat is a weak amylin receptor (AMY) antagonist.
Velusetrag (TD-5108) is an orally active, potent and selective agonist of serotonin 5-HT4 receptor (5-HT4R), with a pKi of 7.7. Velusetrag exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2B receptors. Velusetrag can be used for the research of gastrointestinal diseases and Parkinson's disease[1][2][3][4][5].
Tofogliflozin(CSG-452) hydrate is a potent and highly specific sodium/glucose cotransporter 2(SGLT2) inhibitor with Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouse SGLT2.IC50 value: 2.9/14.9/6.4 nM(human/rat/mouse SGLT2) [1]Target: SGLT2 inhibitorin vitro: Tofogliflozin competitively inhibited SGLT2 in cells overexpressing SGLT2, and K(i) values for human, rat, and mouse SGLT2 inhibition were 2.9, 14.9, and 6.4 nM, respectively. The selectivity of tofogliflozin toward human SGLT2 versus human SGLT1, SGLT6, and sodium/myo-inositol transporter 1 was the highest among the tested SGLT2 inhibitors under clinical development [1]. tofogliflozin was catalyzed to the primary hydroxylated derivative (M4) by CYP2C18, CYP4A11 and CYP4F3B, then M4 was oxidized to M1. 3. Tofogliflozin had no induction potential on CYP1A2 and CYP3A4 [4].in vivo: A single oral gavage of tofogliflozin increased renal glucose clearance and lowered the blood glucose level in Zucker diabetic fatty rats. Tofogliflozin also improved postprandial glucose excursion in a meal tolerance test with GK rats. In db/db mice, 4-week tofogliflozin treatment reduced glycated hemoglobin and improved glucose tolerance in the oral glucose tolerance test 4 days after the final administration [1]. Tofogliflozin (400 ng/ml) induced UGE of about 2 mg/kg per min and increased EGP by 1-2 mg/kg per min, resulting in PG in the normal range [2]. Tofogliflozin suppressed plasma glucose and glycated Hb and preserved pancreatic beta-cell mass and plasma insulin levels. No improvement of glycaemic conditions or insulin level was observed with losartan treatment [3].
H-D-MeAla-EtVaI-VaI-MeLeu-AIa-D-AIa-MeLeu-MeLeu-MeVaI-MeBmt(OAc)-Abu-O-CH2-CH2-NHMe is a nonimmunosuppressive cyclosporin A derivative. H-D-MeAla-EtVaI-VaI-MeLeu-AIa-D-AIa-MeLeu-MeLeu-MeVaI-MeBmt(OAc)-Abu-O-CH2-CH2-NHMe has the potential for the research of congenital muscular dystrophy[1].
Lumasiran sodium, an investigational RNA interference (RNAi) therapeutic agent, reduces hepatic oxalate production by targeting glycolate oxidase. Lumasiran sodium reduces urinary oxalate excretion, the cause of progressive kidney failure in primary hyperoxaluria type 1 (PH1) [1][2].
Charantin is a steroidal saponin isolated from Momordica charantia, and has insulin-like activity, by increasing the release of insulin and slowing down gluconeogenesis. Charantin can against GSK-3[1].
Sodium 2-oxopropanoate-13C is the 13C labeled Sodium 2-oxopropanoate[1]. Sodium 2-oxopropanoate (Sodium pyruvate), a three-carbon metabolite of Glucose, is a compound produced in the glycolytic pathway. Sodium 2-oxopropanoate is a free radical scavenger that can scavenge ROS[2][3].
Eliglustat hemitartrate is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM.
H2-003 is a selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2).
4β-Hydroxycholesterol-d4 is the deuterium labeled 4β-Hydroxycholesterol. 4β-hydroxy Cholesterol is a major oxysterol cholesterol metabolite and a precursor in the synthesis of bile acids that is found in human circulation[1][2].
Forsythoside F (Arenarioside) is a xanthine oxidase inhibitor and possesses antihyperuricemic effects in vivo[1].
Gastric Inhibitory Polypeptide (6-30) amide (human) is an incretin hormone. Gastric Inhibitory Polypeptide (6-30) amide (human) can be used for the research of diabete[1].
Stearoyl-L-carnitine chloride is an endogenous long-chain acylcarnitine. Stearoyl-L-carnitine chloride is a less potent inhibitor of GlyT2. Stearoyl-L-carnitine chloride inhibits glycine responses by 16.8% at concentrations up 3 μM[1][2].