Thioquinapiperifil dihydrochloride (KF31327), a potent, selective and non-competitive phosphodiesterase-5 (PDE-5, IC50 of 0.074 nM) inhibitor, is used for sexual enhancement study[1][2].
Elobixibat is a potent ileal bile acid transporter (IBAT) inhibitor with IC50 values of 0.53 ± 0.17 nM, 0.13 ± 0.03 nM, and 5.8 ± 1.6 nM for human IBAT, mouse IBAT, and canine IBAT.
SRI-37330 is an orally active TXNIP inhibitor. SRI-37330 decreases glucagon secretion and action and blocks hepatic glucose output. SRI-37330 can be used in the research of obesity and diabetes[1].
2-Mercaptobenzothiazole is an endogenous metabolite.
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[1][2].
Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC50 of 6 nM and a Ki of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC50 value of 200 nM). Lintitript increases plasma concentration of leptin and food intake as well as plasma concentration of insulin[1][2][3].
Phosphoenolpyruvic acid (potassium)-13C2 is the 13C labeled Phosphoenolpyruvic acid (potassium)[1]. Potassium 1-carboxyvinyl hydrogenphosphate is an endogenous metabolite.
Lafutidine, a newly developed histamine H(2)-receptor antagonist, inhibits gastric acid secretion.Target: histamine H(2)-receptorLafutidine, a newly developed histamine H(2)-receptor antagonist, inhibits gastric acid secretion.It is currently marketed in Japan (Stogar) China (Lemeiting) and India (Lafaxid). It not only suppresses gastric acid secretion, but also has cytoprotective properties by the virtue of its property to induce the collagen synthesis in the gastric mucosa. It has a novel mechanism of action in addition to blocking the H2 receptors, it decreases inflammation by modulating calcitonin gene-related peptide (CGRP) and vanilloid receptors. It is also found to stimulate mucin biosynthesis and promote the restitution of damaged mucosa.Lafutidine is absorbed in the small intestine, reaches gastric cells via the systemic circulation, and then directly and rapidly binds to gastric cell histamine H2 receptors, thereby inhibiting the stimulation of cAMP and a resultant decrease in acid production (antisecretory action). It causes a sustained increase in intracellular Ca2+ ion concentration in endothelial cells resulting in the release of Calcitonin Gene Related Peptide (CGRP), which causes acid suppression by decreasing the vagal tone. Lafutidine also increases plasma somatostatin levels which decreases secretion of gastrin from G cells. This decrease in gastrin causes inhibition of parietal cells, resulting in decrease in gastric acid secretion.
PDE11-IN-1 is a PDE11 inhibitor and can be used for adrenal insufficiency research[1].
D-Threonine (H-D-Thr-OH) is an enantiomer of L-threonine. D-Threonine is a metabolite of Saccharomyces cerevisiae.
CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1), with IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively.
Pascolizumab (SB-240683) is a humanized anti-IL-4 monoclonal antibody. Pascolizumab has the potential for the research of asthma[1].
ASP3662 is a potent, selective, CNS-penetrable and orally active inhibitor of 11β-HSD1 with Ki of 5.3, 2.6 and 23 nM for human, mouse and rat 11β-HSD1, does not inhibit human 11β-HSD2 at 30 uM; demonstrates no appreciable binding affinity to or inhibition against 87 off-targets (adenosine receptors, adrenergic receptors, angiotensin receptors, calcium channels, 5-HT receptors etc.); inhibits the in vitro conversion of glucocorticoid from its inactive to active form in the brain and spinal cord; ameliorates mechanical allodynia in spinal nerve ligation (SNL) and streptozotocin-induced diabetic rats and thermal hyperalgesia in chronic constriction nerve injury rats. Alzheimer Disease Phase 2 Discontinued
DiIC16(3) is the lipid-mimetic dialkylindocarbocyanine (DiI) derivative. DiIC16(3) is a lipophilic red-orange fluorescent. DiIC16(3) is weakly fluorescent in water but highly fluorescent and quite photostable when incorporated into membranes. DiIC16(3) preferentially enters late endosomes/lysosomes[1].
(R)-Tegoprazan (example 3), a benzimidazole derivative, is a potent kidney H+/K+-ATPase inhibitor with an IC50 of 98 nM of canine kidney Na+/K+-ATPase. (R)-Tegoprazan has the potential for gastrointestinal diseases research[1].
Methylswertianin is an active constituent in Swertia punicea Hemsl, with anti-diabetic effect. Methylswertianin could be useful for treating type-2 diabetes, likely via the improvement of insulin resistance (IR)[1].
MK-8245 trifluoroacetate is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy.IC50 value: 1 nM (hSCD1) [1]Target: SCD1in vitro: MK-8245, a phenoxy piperidine isoxazole derivative, has been identified as a potent and liver-specific SCD inhibitor. It contains a tetrazole acetic acid moiety, which is the key molecule for OATPs recognition and liver-targeting. MK-8245 displays similar potencies against human, rat and mouse SCD1 with IC50 values of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1. MK-8245 exhibits a significant SCD inhibition in the rat hepatocyte assay which contains functional, active OATPs with IC50 of 68 nM, while being only weakly active in the HepG2 cell assay which is devoid of active OATPs with IC50 of ~1 μM. MK-8245 displays highly selective activity for the Δ-5 and Δ-6 desaturases (i.e., >100000 μM vs rat and human Δ5D and Δ6D as assessed in the HepG assay [1].in vivo: Administration of MK-8245 at 10 mg/kg in mice exhibits a tissue distribution profile concentrated in the liver. It shows a liver-to-Harderian gland ratio of 21, suggesting a high degree of liver-targeting compared to a systemically distributed compound with liver-to-Harderian gland ratio of 1.5. Oral dosing of MK-8245 in mice, rats, dogs, and rhesus monkeys demonstrates that MK-8245 is distributed mainly to the liver, with low exposure in tissues associated with potential adverse events. The liver-to-skin ratios are >30:1 in all four species. Administration of MK-8245 to eDIO mice before the glucose challenge improves glucose clearance in a dose-dependent manner with ED50 of 7 mg/kg.
Lesinurad sodium is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with Km values of 0.85 and 2 µM, respectively.
PSTAIR is a monoclonal antibody that recognizes the PSTAIR sequence in Cdc28, PSTAIR can be used as loading control[1].
TA 0910 acid-type is a metabolite of TA 0910. TA-0910 is a metabolically stable analogue of thyrotropin releasing hormone (TRH)[1].
Neuropeptide Y, porcine, a peptide in porcine brain, is capable of inhibiting secretin-stimulated pancreatic secretion[1].
A6770 is an orally active, potent sphingosine 1-phosphate (S1P) lyase (S1PL) inhibitor. A6770 is phosphorylated and the phosphorylated form directly inhibits S1P lyased.A6770, a potential key metabolite of THI, induces a [3H]dhS1P increase[1][2].
L-Alanine-2-13C (L-2-Aminopropionic acid-2-13C) is the 13C-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
Rimonabant-d10 (SR 141716A-d10) hydrochloride is the deuterium labeled Rimonabant hydrochloride. Rimonabant hydrochloride (SR 141716A hydrochloride) is a highly potent and selective central cannabinoid receptor (CB1) antagonist with an Ki of 1.8 nM. Rimonabant hHydrochloride (SR 141716A Hydrochloride) also inhibits Mycobacterial membrane protein Large 3 (MMPL3)[1][2].
Adenosine-13C10 (Adenine riboside-13C10; D-Adenosine-13C10) is 13C-labeled Adenosine (HY-B0228). Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation.
VIP Guinea pig (Vasoactive intestinal peptide), a trophic and mitogenic factor, stimulates growth in whole cultured embryos. VIP Guinea pig functions as a simple gastrointestinal hormone and suggest a possible neurotransmitter function[1][2].
2-Naphthoxyacetic acid is an endogenous metabolite.
Disodium succinate-d4 is the deuterium labeled Disodium succinate[1]. Disodium succinate is the?disodium?salt of?Succinic acid. Succinic acid is an intermediate product of the tricarboxylic acid cycle, as well as one of fermentation products of anaerobic metabolism[2].
EML425 is a potent and selective CREB binding protein (CBP)/p300 inhibitor with IC50s of 2.9 and 1.1 μM, respectively.
β-casomorphin, bovine (β-casomorphin-7) is a opioid peptide with an IC50 of 14 μM in an Opioid receptors binding assay.