Galantide is a reversible and non-specific galanin receptor antagonist.
Amylin (8-37), human is a fragment of human Amylin. Amylin (8-37), human can direct vasodilator effects in the isolated mesenteric resistance artery of the rat. Human Amylin is a small hormone secreted by pancreatic β-cells that forms aggregates under insulin deficiency metabolic conditions, and it constitutes a pathological hallmark of type II diabetes mellitus[1].
Biotin-TAT (47-57), biotin tagged TAT, is a transactivator of transcription. Biotin-TAT (47-57) is one of the most widely used PTDs into different primary cells is ATP- and temperature-dependent, indicating the involvement of endocytosis[1][2].
PA452, retinoic X receptor (RXR) specific antagonist, inhibits the effect of Retinoic acid (RA) on Th1/Th2 development[1].
Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.
BIBR 1087 SE is an intermediate metabolite of dabigatran etexilate.
Theaflavine-3,3'-digallate, a bioactive black tea phenolic, can be used for the research of gut microbiota composition modulatory effects[1].
Myristoyl tetrapeptide-12 directly activates SMAD2 and induces the linking of SMAD3 with DNA. Myristoyl tetrapeptide-12 is capable of stimulating hair growth, especially at the level of eyelashes[1][2].
FATP1-IN-2, as an arylpiperazine derivative, is an orally active fatty acid transport protein 1 (FATP1) inhibitor (human IC50=0.43 μM, mouse IC50=0.39 μM)[1].
Human enteropeptidase-IN-1 (compound 6b) is a highly potent, orally active and low systemic exposure enteropeptidase inhibitor. Human enteropeptidase-IN-1 boosts the increase in fecal protein output, and exhibits potent body weight loss in diet-induced obese (DIO) rat model. Human enteropeptidase-IN-1 can be used for anti-obesity research[1].
Furosemide (Lasix) is a loop diuretic inhibitor of Na+/2Cl-/K+ (NKCC) cotransporter of which used in the treatment of congestive heart failure and edema.Target: NKCC Furosemide (INN/BAN) or frusemide is a loop diuretic used in the treatment of congestive heart failure and edema. It is most commonly marketed by Sanofi under the brand name Lasix, and also under the brand names Fusid and Frumex. It has also been used to prevent Thoroughbred and Standardbred race horses from bleeding through the nose during races.Along with some other diuretics, furosemide is also included on the World Anti-Doping Agency's banned drug list due to its alleged use as a masking agent for other drugs.Furosemide, like other loop diuretics, acts by inhibiting NKCC2, the luminal Na-K-2Cl symporter in the thick ascending limb of the loop of Henle. The action on the distal tubules is independent of any inhibitory effect on carbonic anhydrase or aldosterone; it also abolishes the corticomedullary osmotic gradient and blocks negative, as well as positive, free water clearance.Because of the large NaCl absorptive capacity of the loop of Henle, diuresis is not limited by development of acidosis, as it is with the carbonic anhydrase inhibitors. Additionally, furosemide is a noncompetitive subtype-specific blocker of GABA-A receptors. Furosemide has been reported to reversibly antagonize GABA-evoked currents of α6β2γ2 receptors at uM concentrations, but not α1β2γ2 receptors. During development, the α6β2γ2 receptor increases in expression in cerebellar granule neurons, corresponding to increased sensitivity to furosemide
4-(Dimethylamino)phenol increases the extracellular lactate dehydrogenase (LDH) without markedly affecting gluconeogenesis. 4-(Dimethylamino)phenol cannot decreases the ATP content until the membrane becomes permeable to LDH[1].
LY255582 is a pan-opioid antagonist and has high affinity for mu, delta, and kappa receptors (Ki: 0.4 nM, 5.2, 2.0 nM respectively). LY255582 can decrease food intake and body weight. LY255582 can be used for the research of obesity[1][2][3][4].
pTH-Related Protein (1-34) amide (human, mouse, rat) (Human PTHrP-(1-34)NH2) is a N-terminal fragments of PTHrP. pTH-Related Protein (1-34) amide (human, mouse, rat) induces hypercalcemia, and can be used for research of humoral hypercalcaemia of malignancy[1].
Carbutamide (BZ-55) is an orally active and first-generation sulfonylurea with hypoglycemic activity[1].
TM-25659 is a TAZ modulator. Anti-osteoporotic and anti-obesity activities[1].
APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119 respectively..IC50 value: 2.7 nM (EC50) [1]Target: GPR119Chronic treatment withAPD668 showed for the first time that blood glucose and glycated hemoglobin (HbA1c) levels could be significantly reduced in Zucker Diabetic Fatty (ZDF) rats over several weeks of dosing. APD668 was the ?rst compound with thismechanism of action to be progressed into clinical development for the treatment of diabetes.
2-Hydroxy-2-methylbutanoic acid, an unusual metabolite, is associated with 2-hydroxyglutaric aciduria and maple syrup urine disease.
Siaresinolic acid 28-O-β-D-glucopyranosyl ester possesses anti-tumor and antidiabetic effect activity[1][2].
(S)-Thalidomide ((S)-(-)-Thalidomide) is the S-enantiomer of Thalidomide. (S)-Thalidomide has immunomodulatory, anti-inflammatory, antiangiogenic and pro-apoptotic effects[1][2][3]. (S)-Thalidomide induces teratogenic effects by binding to cereblon (CRBN) [4].
SR59230A is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist[1] with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively[2].
D-Mannitol-d2 is the deuterium labeled D-Mannitol.
Tripeptide-10 is a bioactive peptide withanti-wrinkleeffect and has been reported used as a cosmetic ingredient[1].
FBPase-IN-1 is a potent FBPase (Fructose-1,6-bisphosphatase) inhibitor for Type 2 diabetes (T2D) study with an IC50 of 0.22 μM. FBPase-IN-1 can reduce blood glucose levels and ameliorate glucose tolerance. FBPase-IN-1 modifies the C128 site, regulates the N125-S124-S123 allosteric pathway of FBPase and affects the catalytic activity of FBPase[1].
D-Glucose-d1-2 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].
Quercetin 3-O-rutinoside-7-O-glucoside (compound 8) is an antioxidant agent that canbe found in Hemerocallis fulva. Quercetin 3-O-rutinoside-7-O-glucoside shows strong lipid peroxidation inhibitory activities[1].
Phosphorylethanolamine-d4 (Monoaminoethyl phosphate-d4; NSC 254167-d4) is a deuterium labeled Phosphorylethanolamine (HY-N5034). Phosphorylethanolamine is an endogenous metabolite.
11-Dehydrocorticosterone is a endogenous corticosteroid. 11-Dehydrocorticosterone can be a source of transcriptionally active glucocorticoid in cardiac myocytes and fibroblasts. 11-Dehydrocorticosterone can increase SGK mRNA expression in cardiac fibroblast[1].
Flaccidoside III is a flavonoid and triterpenoid isolated from the aerial parts of N. sativa (Ranunculaceae). Flaccidoside III inhibits α-Glucosidase (IC50: 256.7 μM) and has potential antioxidant and antidiabetic activities[1].
Nimacimab (RYI-018) is a negative-allosteric modulating monoclonal antibody targeting CB1 receptor. Nimacimab can be used for research of metabolic diseases[1][2].