Clofibride is an orally active hypolipaemic agent of pchlorophenoxyisobutyric type. Clofibride has weak toxicity and marked hypocholesterolaemic and hypotriglyceridaemic activity. Clofibride is converted into 4-chlorophenoxyisobutyric acid (CPIB) and 4-hydroxy-N-dimethylbutyramide (HMB) in vivo[1].
25-Hydroxy VD2-D6 is a labelled metabolite of Vitamin D2.
Syringetin, a flavonoid derivative, is associated with increased BMP-2 production. Syringetin stimulates osteoblast differentiation at various stages, from maturation to terminally differentiated osteoblasts[1].
Tricosanoic acid is a long-chain fatty acid and shown to be a hair growth stimulant.
TUG-1375 is an agonist of free fatty acid receptor 2 (FFA2/GPR43), with a pKi of 6.69. TUG-1375 is inactive on FFA3, FFA4, PPARα, PPARγ, PPARδ, LXRα or LXRβ[1].
N-Acetyl-D-glucosamine-13C is the 13C labeled N-Acetyl-D-glucosamine. N-Acetyl-D-Glucosamine (N-Acetyl-2-amino-2-deoxy-D-glucose) is a monosaccharide derivative of gluc[1][2].
PF-02575799 is a microsomal triglyceride transfer protein (MTP) inhibitor with an IC50 of 0.77±0.29 nM.
Hydrocortisone phosphate is the pharmaceutical term for cortisol, which is a steroid hormone, in the glucocorticoid class of hormones, increases blood sugar through gluconeogenesis, to suppress the immune system, and to aid in the metabolism of fat, protein, and carbohydrate.
Rasburicase is a recombinant urate oxidase and a hyperuricemia inhibitor. Rasburicase converts uric acid into allantoin, making it easier to be cleared by the kidneys and improving the elevated level of uric acid in the blood[1].
Galanin-Like Peptide (rat) is a 60 amino acid neuropeptide. Galanin-Like Peptide (rat) plays an important role in the regulation of feeding, body weight and energy metabolism[1].
Chitosan oligosaccharide (COS) is an oligomer of β-(1→4)-linked D-glucosamine. Chitosan oligosaccharide (COS) activates AMPK and inhibits inflammatory signaling pathways including NF-κB and MAPK pathways.
Sograzepide (Netazepide;YF476) is a gastrin/cholecystokinin 2 receptor (CCK2) antagonist.
4-Methyl-2-oxopentanoic acid, an abnormal metabolite, is both a neurotoxin and a metabotoxin.
PCSK9-IN-18 (compound 188) is a potent PCSK9 inhibitor with a KD value of <200 nM[1].
Licoisoflavone A, an isoflavone, mainly derived from Glycyrrhiza uralensis Fisch.[1]. Licoisoflavone A inhibits lipid peroxidation with an IC50 of 7.2 μM[1].
P32/98 hemifumarateis a potent inhibitor of dipeptidyl peptidase IV with a Ki value of 130 nM. P32/98 hemifumarate improves glucose tolerance, insulin sensitivity and β-cell responsiveness in fatty Zucker rat model[1][2][3].
D-Glucose-13C,d2 is the deuterium and 13C 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 sig
Trelagliptin(SYR-472) is a long acting dipeptidyl peptidase-4 (DPP-4) inhibitor that is being developed for the treatment of type 2 diabetes (T2D). IC50 value:Target: DPP4Two Phase II clinical studies have been completed with Efficacy and Safety of SYR-472 in Subjects With Type 2 Diabetes Mellitus. Phase III clinical studies with trelagliptin in Japan to evaluate its safety and efficacy in a once-weekly oral treatment regimen. Currently, all available DPP-4 inhibitors are dosed once-daily. A once-weekly treatment, such as trelagliptin, would provide patients with a convenient treatment alternative and has the potential to improve treatment compliance.
Febuxostat(TEI 6720;TMX 67 ) is selective xanthine oxidase inhibitor with Ki of 0.6 nM.IC50 value: 0.6 nM (Ki) [1]Target: xanthine oxidasein vitro: Febuxostat displays potent mixed-type inhibition of the activity of purified bovine milk xanthine oxidase, with Ki and Ki' values of 0.6 nM and 3.1 nM respectively, indicating inhibition of both the oxidized and reduced forms of xanthine oxidase [1]. in vivo: Febuxostat (5–6 mg/kg/day) combined with fructose significantly lowers blood pressure, UA, triglycerides, and insulin in rats compared with fructose alone. Febuxostat (5–6 mg/kg/day) combined with fructose also reduces glomerular pressure, renal vasoconstriction, and afferent arteriolar area in rats compared with fructose alone [2]. Febuxostat prevents hyperuricemia in 5/6 nephrectomy (5/6 Nx)+oxonic acid (OA)+Febuxostat(Fx) rats and ameliorates proteinuria, preserves renal function and prevents glomerular hypertension in both 5/6 nephrectomy (5/6 Nx)+vehicle (V)+Febuxostat(Fx) and 5/6 nephrectomy (5/6 Nx)+oxonic acid (OA)+Febuxostat(Fx) groups [3]. Febuxostat (5 mg/kg/d by gavage for 8 days) treatment after transverse aortic constriction (TAC) attenuates the TAC-induced left ventricular (LV) hypertrophy and dysfunction. Febuxostat blunts the TAC-induced increases in nitrotyrosine (indicating reduced myocardial oxidative stress), p-Erk(Thr202/Tyr204), and p-mTOR(Ser2488), with no effect on total Erk or total mTOR [4].
GLP-1R agonist 15 (Compound 101) is a GLP-1 receptor agonist[1].
2-Oleoylglycerol is a dietary naturally occurring lipid. 2-Oleoylglycerol is a GPR119 agonist, with an EC50 of 2.5 μM for human GPR119 in transiently transfected COS-7 cells. 2-Oleoylglycerol stimulates glucagon-like peptide-1 (GLP-1) secretion in vivo[1][2].
GlcNAcstatin is a selective glucoimidazole-based bacterial O-GlcNAcase inhibitor with a Ki of 4.6 pM. GlcNAcstatin shows 100000-fold selectivity over HexA/B[1].
Insulin lispro is a recombinant human insulin analogue and is one of three rapid-acting insulin analogues available. Insulin lispro can be used for the research of hyperglycaemia in diabetes mellitus[1].
Palmitoyl hexapeptide-14(Palmitoyl hexapeptide-6)isa bioactive peptide withanti-inflammatoryeffect and has been reported used as a cosmetic ingredient[1].
Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation.
PROTAC PTPN2 degrader-2 (example 187B) is a potent PTPN2 degrader with potential for studying cancer or metabolic diseases[1].
(-)-N-methylcoclaurine possesses melanogenesis inhibitory activity[1].
Desmethylazelastine is a main active metabolite of Azelastine that is oxidatively metabolized by the cytochrome P450 enzyme system with a protein binding rate of 97% and an elimination half-life of 54 hours. Azelastine is an orally active, selective and high-affinity histamine H1-receptor antagonist. Azelastine can be used in studies of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2[1][2][3][4][5].
Ipragliflozin (L-Proline) is a highly potent and selective SGLT2 inhibitor with an IC50 of 2.8 nM; little and NO potency for SGLT1/3/4/5/6.
CP742033 is a gut-selective inhibitor of microsomal triglyceride transfer protein (MTP) that reliably produces weight loss in obese dogs.