Tolimidone is a potent and selective allosteric activator of Lyn kinase with an EC50 of 63 nM.
SKF 100398 (d(CH2)5Tyr(Et)VAVP) is an arginine vasopressin (AVP) analogue, and acts as a specific antagonist of the antidiuretic effect of exogenous and endogenous AVP[1].
MAP4K4-IN-17 is a potent and highly selective MAP4K4 inhibitor with IC50 of 14.9 nM, showes improved overall drug-like properties compared to PF-06260933; a lead compound for advanced preclinical development.
GLP-1 receptor agonist 11 (compound 3) is an agonist of GLP Receptor. GLP-1 receptor agonist 11 can be used in the study of diseases such as diabetes and non-alc. fatty liver disease[1].
Phanginin A is a potent and orally active SIK1 (salt-induced kinase 1) activator. Phanginin A inhibited gluconeogenesis. Phanginin A increases the expression of p-SIK1 and decreases the expression of p-CREB. Phanginin A reduces blood glucose levels and improves glucose tolerance and dyslipidemia. Phanginin A has the potential for the research of type 2 diabetes[1].
KT-172 is a potent, selective inhibitor of DAGLβ with IC50 of 60 nM; displays selectivity over DAGLα, and negligible activity against other key enzymes involved in endocannabinoid signaling, including FAAH, MAGL, and ABHD11; disrupts the lipid network involved in macrophage inflammatory responses, lowering 2-AG, as well as arachidonic acid and eicosanoids in mouse peritoneal macrophages; possesses one remaining off-target ABHD6 (IC50=5 nM).
1,5-Anhydrosorbitol is a short-term marker for glycemic control.
Efruxifermin is an Fc-FGF21 fusion protein (human IgG1 Fc domain linked to a modified human FGF21). Efruxifermin has prolonged half-life and enhanced receptor affinity compared with native human FGF21. Efruxifermin can be used for the research of non-alcoholic steatohepatitis[1].
Riboflavin tetrabutyrate is a lipophilic flavin derivative with antioxidative and lipid peroxide-removing activity.
NPP1-IN-1 is a potent NPP inhibitor with IC50s of 0.15 μM and 40 μM for NPP1 and NPP3, respectively[1].
2,3,4'-Trihydroxy-3',5'-dimethoxypropiophenone, isolated from Parinari hypochrysea (Chrysobalanaceae), exhibits antioxidant and lipoxygenase inhibition[1].
EMD638683 R-Form is the R-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM.
PI3KC2α-IN-1 is a potent PI3KC2α inhibitor (IC50: 95 nM). PI3KC2α-IN-1 interacts with the ATP-binding site of PI3KC2α. PI3KC2α-IN-1 can be used in the research of thrombosis, diabetes and cancers[1].
Benalfocin is a novel selective alpha-2 adrenergic receptor antagonist. Benalfocin reduces blood pressure and heart rate. Benalfocin can be used in the study of cardiovascular effects [1].
Epoetin zeta is a derivative of the endogenous protein erythropoietin, acting as an erythropoiesis-stimulating agent. Epoetin zeta can be used for researching symptomatic anemia of renal origin, symptomatic renal anemia[1].
Ibiglustat (Venglustat) is an inhibitor of glucosylceramide synthase extracted from patent WO 2015089067 A1, compound example 64.
Achyranthoside C is a saponin from Achyranthes bidentata. The derivative of Achyranthoside C has inhibitory activity on osteoclast formation[1].
Coproporphyrin I is an endogenous metabolite present in Urine and Blood that can be used for the research of Liver Disease and Porphyria[1][2][3][4].
Zingibroside R1 is dammaranae-type triterpenoid saponin, isolated from rhizomes, taproots, and lateral roots of Panax japonicas C. A. Meyer, shows excellent anti-tumor effects as well as anti-angiogenic activity[1].Zingibroside R1 possesses some anti-HIV-1 activity.Zingibroside R1 has inhibitory effects on the 2-deoxy-D-glucose (2-DG) uptake by EAT cells (IC50=91.3 μM)[2].
MA-0204 is a potent, highly selective and orally available peroxisome proliferator activated receptor δ (PPARδ) modulator with EC50s of 0.4 nM, 7.9 nM and 10 nM for human, mouse and rat PPARδ, respectively. Potential treatment for Duchene Muscular Dystrophy (DMD)[1].
Triiodothyronine sulfate is the main metabolite of thyroid hormone triiodothyronine (T3). Triiodothyronine is an active form of thyroid hormone, which binds to β1 thyroid hormone receptor (TRβ1), and activates its activity[1][2].
SY-640 is an Acetamide derivative and has potent hepatoprotective effect. SY-640 reduces Propionibacterium acnes and Lipopolysaccharide-induced liver injury in mice[1][2].
Leptin (22-56), human is the fragment of leptin, mediated via several isoforms of receptors (Ob-Rs).
Pancreatic Polypeptide, human is a C-terminally amidated 36 amino acid peptide, which acts as a neuropeptide Y (NPY) Y4/Y5 receptor agonist.
Relamorelin (RM-131) acetate, a Ghrelin analog, is a potent ghrelin receptor agonist, with a Ki of 0.42 nM for GHS-1a. Relamorelin acetate can promote food intake and adiposity in mice. Relamorelin acetate can be used for the research of cachexia, gastroparesis, and gastric/intestinal dysmobility disorders[1][2][3].
M8-B is a potent transient receptor potential melastatin-8 (TRPM8) antagonist. M8-B blocks cold-induced and TRPM8-agonist-induced activation TRPM8 channels. M8-B decreases deep body temperature (Tb)[1].
Chrysin 6-C-arabinoside 8-C-glucoside is a α±-glucosidase inhibitors which are widely used in the study for type 2 diabetes[1].
Zamifenacin (UK-76654) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome[1].
CCX140 is a potent CCR2 antagonist.
2,5-Anhydro-D-glucitol-1,6-diphosphate is a limited stimulator of yeast Pyruvate Kinase. 2,5-Anhydro-D-glucitol-1,6-diphosphate is used as an analogue of the a-form, 2,5-anhydro-D-mannitol 1,6-bisphosphate, while is an excellent allosteric activator of Pyruvate Kinase[1].