4β-Hydroxywithanolide E, isolated from Physalis peruviana L., inhibits adipocyte differentiation of 3T3-L1 cells through modulation of mitotic clonal expansion. 4β-Hydroxywithanolide E is an adipogenesis inhibitor and inhibits PPARγ, C/EBPα, and the adipocyte-specific molecule aP2 mRNA expression[1].
Tetracosanoyl-sulfatide is an endogenous metabolite present in Urine that can be used for the research of Mild Metachromatic Leukodystrophy[1][2].
Elastase from porcine pancreas is a single polypeptide chain of 240 amino acid residues. Elastase from porcine pancreas is a serine protease that can hydrolyze proteins and polypeptide. Elastase from porcine pancreas can induce emphysema in hamsters[1][2][3].
4β-hydroxy Cholesterol is a major oxysterol cholesterol metabolite and a precursor in the synthesis of bile acids that is found in human circulation[1].
6-O-Caffeoylarbutin (Robustaside B) possesses antioxidant activity[1].
Fasitibant (free base) is a potent, selective, high affinity, and long-lasting nonpeptide bradykinin B2 (BK2) receptor antagonist. Fasitibant (free base) has proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis[1].
Tetrahydro-11-dehydrocorticosterone is a 11β-HSD inhibitor[1].
α-Glucosidase-IN-10 (compound 13) is a potent α-glucosidase inhibitor, with an IC50 of 92.7 μM. α-Glucosidase-IN-10 can be used for type II diabetes research[1].
(+)-Magnoflorine iodide (Magnoflorine iodide), an aporphine alkaloid found in Acoruscalamus, reduces the formation of C. albicans biofilm[1]. (+)-Magnoflorine iodide has anti-fungal, anti-antidiabetic and anti-oxidative activity[2].
Galactosylhydroxylysine is a component of bone collagen produced by post-translational glycosylation of hydroxylysine. Galactosylhydroxylysine is released during bone resorption and has been shown to be elevated in metabolic bone loss[1].
3'-Hydroxy Repaglinide is a main CYP2C8 metabolite of Repaglinide. Repaglinide is a carbamoylmethyl benzoic acid (CMBA) derivative, which recently has become available for the treatment of type II diabetes[1][2].
PF-06815345 (PF 6815345) is a potent prodrug PCSK9 modulator that inhibits PCSK9 secretion in vitro translation assay; PF-06815345is identified after optimization of the prodrug moiety to maximize intestinal stability achieving liver targeting of the active compound after prodrug turnover by carboxylesterase (CES1). Hypercholesterolemia Phase 1 Discontinued
Cholecystokinin Octapeptide, desulfated TFA is a synthetic desulfated octapeptides of Cholecystokinin (CCK)[1].
Malonyl CoA is a substrate for fatty acid biosynthesis and an inhibitor of fatty acid oxidation. Malonyl CoA is also a reversible inhibitor of mitochondrial carnitine palmitoyltransferase (CPT) 1[1][2].
Falecalcitriol(Fulstan; Hornel) is an analog of calcitriol; has a higher potency both in vivo and in vitro systems, and longer duration of action in vivo.
Minoxidil sulfate, a potent and ATP-sensitive K+ channel opener, is the sulfated metabolite of minoxidil. Minoxidil sulfate is considered as a vasodilator to promote hair growth in vivo[1][3].
tert-OMe-byakangelicin is a coumarin that can enhances the adrenaline-induced lipolytic effect and inhibits insulin-stimulated triglyceride synthesis from glucose in fat cells[1].
HIF-2α-IN-1 is a HIF-2α inhibitor has an IC50 of less than 500 nM in HIF-2α scintillation proximity assay.IC50 value: ＜ 500 nMTarget: HIF-2α
Desmopressin(DDAVP) is the synthetic analogue of the antidiuretic hormone arginine vasopressin. IC50 Value:Target: Vasopressin ReceptorThe antidiuretic properties of desmopressin have led to its use in polyuric conditions including primary nocturnal enuresis, nocturia, and diabetes insipidus. Desmopressin works by limiting the amount of water that is eliminated in the urine. Desmopressin binds to V2 receptors in renal collecting ducts, increasing water reabsorption. It also stimulates release of von Willebrand factor from endothelial cells by acting on the V2 receptor.
VIP(6-28)(human, rat, porcine, bovine) is an effective antagonist of the actions of exogenous vasoactive intestinal peptide (VIP) on cAMP.
GPR40 agonist 1 is a potent and novel GPR40 full agonist with an EC50 of 2 nM and 17 nM for hGPR40 and rGPR40, respectively.
Ex26 (S1P1-IN-Ex26) is a potent and selective Sphingosine 1-phosphate receptor 1 (S1P1) antagonist (IC50=0.93 nM). Ex26 shows >3,000-fold selectivity for S1P1 over other Sphingosine 1-phosphate receptors. Ex26 can be used in experimental autoimmune encephalomyelitis reseach[1].
Roxatidine acetate is a potent, selective, competitive and orally active histamine H2-receptor antagonist. Roxatidine acetate has antisecretory potency against gastric acid secretion. Roxatidine acetate can also suppress inflammatory responses and can be used for gastric and duodenal ulcers research. Roxatidine acetate has antitumor activity[1][2][3].
Isoformononetin is an analog of Daidzein (HY-N0019) and has immunoprotective effects. Isoformononetin inhibits the differentiation of Th17 and B-cells lymphopoesis to promote osteogenesis in estrogen-deficient bone loss conditions[1].
KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction.
Aldose reductase-IN-6 (Compound 3) is a competitive aldose reductase (AR) inhibitor with an IC50 of 3.164 μM and a Ki of 0.018 μM. Aldose reductase-IN-6 exhibits no cytotoxicity against healthy cells[1].
Rhodionin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.761 μM and a Ki of 0.769 μM[1]. Rhodionin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL[2]. Rhodionin exhibits potent DPPH free radical scavenging activities, with an IC50 of 19.49 μM[3].
GNF2133 hydrochloride is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 µM for DYRK1A and GSK3β, respectively. GNF2133 hydrochloride shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 hydrochloride significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 hydrochloride has the potential for the research of type 1 diabetes[1].
st-Ht31 is a membrane-permeable peptide inhibitor of protein kinase A (PKA) anchoring. st-Ht31 induces robust cholesterol/phospholipid efflux. st-Ht31 completely reverses foam cell formation and restores the metabolic health of macrophage[1][2].
Chinese gallotannin is a non-specific promiscuous α-amylase inhibitor with a Ki of 0.82 μg/mL for human salivary α-amylase. Chinese gallotannin can be used for the research of diabetes[1].