PI5P4Kα-IN-1 (Compound 13) is a PI5P4Kinhibitor (IC50: 2 and 9.4 μM for PI5P4Kα and PI5P4Kβ). PI5P4Kα-IN-1 can be used for research of cancer, metabolic and immunological disorders[1].
MAFP (Methyl Arachidonyl Fluorophosphonate) is an selective, active-site directed and irreversible inhibitor of cPLA2 and iPLA2. MAFP is also a potent irreversible inhibitor of anandamide amidase.
Pulsatilloside C is a phenolic compound isolated from Pulsatilla koreana. Pulsatilloside C significantly inhibits adipocyte differentiation[1].
3-(3-Methoxyphenyl)propionic acid is an organic acid, naturally occurring human metabolite and excreted in human urine.
ELOVL1-IN-1 is an ELOVL1 inhibitor extracted from patent WO2018107056A1, compound 87. ELOVL1-IN-1 can reduce very long chain fatty acid levels. ELOVL1-IN-1 can be used for the research of adrenoleukodystrophy (ALD)[1].
5'''-O-Feruloyl complanatoside B is isolated from Astragali Semen, the seeds of Astragalus Complanatus. Semen Astragali Complanati (SAC) include fatty acids, amino acids, polysaccharides, flavonoids, triterpene glycosides and trace elements; have been reported to involve in chronic diseases such as cardiovascular diseases, diabetes mellitus and cancers[1][2].
Trimethylammonium chloride-13C3,d9 is the deuterium and 13C labeled Trimethylammonium chloride[1]. Trimethylammonium chloride is an endogenous metabolite.
Spermidine trihydrochloride maintains cell membrane stability, increases antioxidant enzymes activities, improving photosystem II (PSII), and relevant gene expression. Spermidine trihydrochloride significantly decreases the H2O2 and O2.- contents[1].
D-Glucose-d1-4 is the deuterium 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 signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
D-Tyrosine is the D-isomer of tyrosine. D-Tyrosine negatively regulates melanin synthesis by inhibiting tyrosinase activity. D-Tyrosine inhibits biofilm formation and trigger the self-dispersal of biofilms without suppressing bacterial growth[1][2].
Lobeglitazone is a new type of thiazolidinedione. Lobeglitazone can be used to prevent type 2 diabetes mellitus (T2DM)[1].
Glucagon receptor antagonists-4 is a highly potent glucagon receptor antagonist. It displays low in vivo clearance and excellent oral bioavailability in both rats and dogs.
Fosciclopirox suppresses growth of urothelial cancer by targeting the γ-secretase complex. Fosciclopirox selectively delivers the active metabolite, Ciclopirox (CPX), to the entire urinary tract[1][2]. Ciclopirox has anticancer activity in a number of solid and hematologic malignancies.
β-Zearalanol-d4 is a deuterium labeled Beta-Zearalanol (HY-N6740）[1]. Beta-Zearalenol is an mycotoxin produced by Fusarium spp, which causes apoptosis and oxidative stress in mammalian reproductive cells[2]. Beta-Zearalenol is the derivative of zearalenone (ZEA) which can conjugate with glucuronic acid[3].
MK-0674 is a potent, orally bioavailable and selective cathepsin K inhibitor, with an IC50 of 0.4 nM, shows 1156, 1465, 11857 and 243 fold selectivity over Cat B, Cat F, Cat L and Cat S. MK-0674 exhibits long half-lives in rats, rabbits and rhesus monkeys[1].
7-Ketocholesterol, toxic oxysterol, inhibits the rate-limiting step in bile acid biosynthesis cholesterol 7 alpha-hydroxylase, as well as strongly inhibiting HMG-CoA reductase (the rate-limiting enzyme in cholesterol biosynthesis). 7-Ketocholesterol induces cell apoptosis[1].
Allyl methyl trisulfide is a volatile organic compound and a component of garlic (Allium sativum L.) essential oil, which has antibacterial, antioxidant and antitumor activities[1].
L-Cysteine-d3 is the deuterium labeled L-Cysteine. L-Cysteine is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine suppresses ghrelin and reduces appetite in rodents and humans[1].
Firuglipel (DS-8500a) is an orally available, potent and selective GPR119 agonist.
Taurodeoxychloic Acid (sodium hydrate) prevents apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxychloic Acid (sodium hydrate) is investigated for use in several conditions such as Primary Biliary Cirrhosis (PBC), insulin resistance, amyloidosis, Cystic Fibrosis, Cholestasis, and Amyotrophic Lateral Sclerosis[1].
OPC-163493 is an orally active liver-targeted mitochondrial uncoupling agent. OPC-163493 reduces Δψ and mitochondrial ROS production. OPC-163493 has antidiabetic and cardiovascular beneficial effects. OPC-163493 lowers blood pressure, extends survival, and improves renal function in the rat model of stroke/hypertension[1].
Xanthine oxidase-IN-1 is a xanthine oxidase inhibitor extracted from patent WO2008126898A1, page 68, compound example 3, with an IC50 of 6.5 nM.
Rennin, also known as Chymosin, is a pepsin-related proteolytic enzyme synthesized by cells in the stomach of certain animals that efficiently converts liquid milk into a semi-solid, allowing it to remain in the stomach for longer. The natural substrate of Rennin is K-casein, which is specifically cleaved at the peptide bond between amino acid residues 105 and 106, phenylalanine and methionine, and is widely used in cheese production[1].
Saxagliptin(BMS477118) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM and Ki of 1.3 nM.IC50 value: 26 nM [1]Target: DPP4in vitro: Saxagliptin has an inhibition constant Ki of 1.3 nM for DPP4 inhibition, which is 10-fold more potent than either vildagliptin or sitagliptin (another two DPP4 inhibitors) with Ki of 13 and 18 nM. In addition, Saxagliptin demonstrates greater specificity for DPP4 than for either the DPP8 or DPP9 enzymes (400- and 75- fold, respectively). The active metablite of saxagliptin is two-fold less potent than the parent. Both Saxagliptin and its metabolite are highly selective (>4000-fold) for the prevention of DPP4 compared with a range of other proteases (selectivity of sitagliptin and vildagliptin for DPP4 is >2600 and <250-fold, respectively, compared with DPP8 and DPP9) [2]. Saxagliptin reduces the degradation of the incretin hormone glucagon-like peptide-1, thereby enhancing its actions, and is associated with improved β-cell function and suppression of glucagon secretion.in vivo: Saxagliptin is highly effective at eliciting marked dose-dependent enhancements in glucose clearance in the dose range 0.13-1.3 mg/kg in ob/ob mice relative to controls. Saxagliptin dose-dependently elevate plasma insulin significantly at 15 min post-oGTT, with concomitant improvement in the glucose clearance curves at 60 min post-oGTT [4].
SB-435495 hydrochloride is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM[1][3].
1-Palmitoyl-sn-glycerol 3-phosphate (1-P-GPA) is an endogenous metabolite. 1-Palmitoyl-sn-glycerol 3-phosphate can be used for the research of non‐alcoholic fatty liver disease[1].
1,2-Dipalmitoyl-sn-glycero-3-phosphoethanolamine-d62 is deuterium labeled 1,2-Dipalmitoyl-sn-glycero-3-phosphoethanolamine. 1,2-Dipalmitoyl-sn-glycero-3-phosphoethanolamine is an endogenous metabolite.
Sorbinil, is an Aldose reductase inhibitor (ARI).Sorbinil plays therapeutic role in treating diabetes and diabetic complications, decreases AR activity and inhibits polyol pathway, it to be found comparatively safer than other ARIs for human use[1].
Acyl coenzyme A synthetase (ACS), namely acetyl coenzyme A synthetase, is often used in biochemical research. Acyl coenzyme A synthetase can catalyze the activation of fatty acids by coenzyme A through a two-step thioesterification reaction to produce acyl coenzyme A, and then participate in a variety of anabolic and catabolic lipid metabolism pathways, and participate in the TCA cycle in aerobic respiration[1].
PTP1B-IN-3 is a potent and selective PTP1B inhibitor with IC50s of 120 nM (PTP1B) and 120 nM (TCPTP), respectively.