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.
PBI 51 is an (+)-abscisic acid (ABA) antagonist that blocks the induction of napin and oleosin gene expression by ABA. PBI 51 acts as a weak ABA agonist at high concentration[1].
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].
Atorvastatin lactone is a prodrug form of atorvastatin. Atorvastatin is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor[1].
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].
CP-610431 is a reversible, ATP-uncompetitive, isozyme-nonselective acetyl-CoA carboxylase (ACC) inhibitor. CP-610431 inhibits ACC1 and ACC2 with IC50s of ~50 nM. CP-610431 can be used for the research of metabolic syndrome[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].
LysoPC 20:3(5Z,8Z,11Z) is a lysophosphatidylcholine. LysoPC 20:3(5Z,8Z,11Z) can be used as a biomarker for acute aortic dissection[1].
Cholecystokinin Precursor (24-32) (rat) is a cholecystokinin precursor that can be expressed in the heart, lungs, and kidneys as well as in the gastrointestinal tract and brain. Cholecystokinin is a brain-gut peptide that stimulates gallbladder contraction and pancreatic exocrine secretion and also acts as a neurotransmitter[1].
Aldicarb sulfoxide-d3 is the deuterium labled Aldicarb sulfoxide (HY-124104). Aldicarb sulfoxide is a metabolite of Aldicarb. Aldicarb sulfoxide affects the glutathione-linked enzymes in CHO-K1 cells. Aldicarb sulfoxide inhibits cholinesterase (ChE) and carboxylesterase (CaE) with IC50 of 10 μM for both in zebrafish[1][2].
Chrysophanol triglucoside is an anthraquinone isolated from Cassia obtusifolia, inhibits protein tyrosine phosphatases 1B (PTP1B) and α-glucosidase with IC50s of 80.17 and 197.06 µM, respectively. Chrysophanol triglucoside has the potential for diabetes research[1].
DS-3801b is a potent and non-macrolide agonist of GPR38. DS-3801b is expected to be novel gastrointestinal prokinetic agents for the research of functional gastrointestinal disorders such as gastroparesis and chronic constipation[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].
Terazosin is a selective alpha1-antagonist used for treatment of symptoms of benign prostatic hyperplasia (BPH).Target: Alpha-1 Adrenergic ReceptorTerazosin is selective for alpha 1A-adrenoceptors which appear to dominate in the human prostate; the therapeutic relevance of this selectivity remains to be assessed in clinical studies [1]. Administration of terazosin 1 mg orally for 28 d. Terazosin initially shifted the dose-response curve of phenylephrine to the right, with a significant increase in ED50 for phenylephrine from a control value of 102 to 759 ng/min on day 1 of terazosin (P < 0.001). The mean Kd of terazosin was estimated as 11 +/- 15 nM in the first few days of treatment. This study demonstrates that pharmacological tolerance to the alpha 1-adrenoceptor blocking action of terazosin occurs in man and may be responsible for loss in efficacy with chronic therapy [2].
BIM 23042, a certain somatostatin (SS) octapeptide analogue, is a selective neuropeptide neuromedin B receptor (NMB-R, BB1) antagonist. BIM 23042 has 100-fold lower affinity for gastrin-releasing peptide (GRP) receptor (BB2). BIM 23042 inhibits Neuromedin B (HY-P0241), ICI 216140 and DPDM-bombesin ethylamide-induced Ca2+ release[1][2][3].
Firuglipel (DS-8500a) is an orally available, potent and selective GPR119 agonist.
Mitoquinone is a mitochondria-targeted antioxidant designed to accumulate within mitochondria in vivo in order to protect against oxidative damage.
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.
Methyl deacetylasperulosidate is an iridoid isolated from Borreria and Spermacoce species.
Cy5.5 (Sulfo-Cyanine5.5) is a near-infrared fluorescent dye (Ex=673 nm, Em=707 nm) used to label biological molecules, such as peptides, proteins, and oligonucleotides[1].
4-Hydroxyisoleucine (4-Hydroxy-L-isoleucine) is an amino acid which can be extracted and purified from fenugreek seeds. 4-Hydroxyisoleucine (4-Hydroxy-L-isoleucine) displays an insulinotropic activity of great interest[1].
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].
1-Methylhistamine-d3 (dihydrochloride) is the deuterium labeled 1-Methylhistamine (dihydrochloride)[1]. 1-Methylhistamine dihydrochloride is a histamine metabolite[2].
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].