Omigapil maleate (CGP3446B maleate) is an orally bioavailable apoptosis inhibitor. Omigapil maleate can be used for the research of congenital muscular dystrophy (CMD)[1]. Omigapil maleate, a GAPDH nitrosylation inhibitor, abrogates Aβ1-42-induced tau acetylation, memory impairment, and locomotor dysfunction in mice, suggesting that Omigapil maleate has the potential for the research of Alzheimer's disease[2].
Evogliptin tartrate is a potent, orally bioavailable and selective dipeptidyl peptidase-4 (DPP-4) inhibitor, with antidiabetic activity. Evogliptin tartrate has potential for anti-atherosclerosis therapy that targets arterial inflammation[1].
Torachrysone-8-O-b-D-glucoside could be isolated from root of Polygonum multiflorum. Torachrysone-8-O-b-D-glucoside increases the proliferation of DPCs (dermal papilla cells)[1].
Prepro-von Willebrand factor (641-650) (bovine) is a fragment of Prepro-von Willebrand factor, which binds to type I collagen[1].
P32/98 is a potent inhibitor of dipeptidyl peptidase IV. P32/98 improves glucose tolerance, insulin sensitivity and β-cell responsiveness in preclinical studies using the fatty Zucker rat, an animal model for IGT (impaired glucose tolerance)[1].
PCSK9-IN-10 is a potent and orally active PCSK9 inhibitor with an IC50 value of 6.4 µM. PCSK9-IN-10 increases the expression of LDLR protein and decreases the expression of PCSK9. PCSK9-IN-10 reduces atherosclerosis progression. PCSK9-IN-10 has the potential for the research of hyperlipidemia[1].
CP-640186 is an isozyme-nonselective acetyl-CoA carboxylase (ACCase) inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively; with improved metabolic stability vs CP-610431.IC50 value: 53 nM/61 nM (rat liver ACC1/skeletal muscle ACC2) [1]Target: acetyl-CoA carboxylasein vitro: CP-640186, also inhibited both isozymes with IC50s of ~55 nM but was 2–3 times more potent than CP-610431 in inhibiting HepG2 cell fatty acid and TG synthesis. CP-640186 also stimulated fatty acid oxidation in C2C12 cells (ACC2) and in rat epitrochlearis muscle strips with EC50s of 57 nM and 1.3 uM [1]. in vivo: In rats, CP-640186 lowered hepatic, soleus muscle,quadriceps muscle, and cardiac muscle malonyl-CoAwith ED50s of 55, 6, 15, and 8 mg/kg. Consequently, CP-640186 inhibited fatty acid synthesis in rats, CD1 mice,and ob/ob mice with ED50s of 13, 11, and 4 mg/kg, andstimulated rat whole body fatty acid oxidation with anED50 of ~30 mg/kg [1].
25-O-Methylalisol A is a protostane triterpenoids isolated from Alisma orientale. The dried rhizomes of the aquatic plant Alisma orientale known as Rhizoma Alismatis is a common traditional Chinese medicine used for diuretic, anti-inflammatory, and hypolipidemic purposes, as well as the treatment of diabetes[1].
Glucagon receptor antagonists-3 is a highly potent glucagon receptor antagonist.
Vildagliptin carboxylic acid metabolite (M20.7) TFA is a potent P450 enzyme activity inhibitor[1].
WM-662 is a WDR5-MYC interaction inhibitor, with an IC50 of 18 μM. WM-662 has potential for the research of cancer, aging, and neurodegenerative disorders[1].
Pegbelfermin (BMS-986036) is a polyethylene glycol-modified (PEGylated) analogue of human fibroblast growth factor 21 (FGF21). Pegbelfermin can be used for the research of nonalcoholic steatohepatitis (NASH)[1][2].
Glibornuride is a blocker of ATP-sensitive K+ channels (KATP channel) with a pKi of 5.75[1]. Antidiabetic agent[2].
Nicotinamide riboside malate, an orally active NAD+ precursor, increases NAD+ levels and activates SIRT1 and SIRT3. Nicotinamide riboside malate is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities[1]. Nicotinamide riboside malate reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease[2].
VIP (1-12), human, porcine, rat, ovine is a vasoactive intestinal peptide (VIP) fragment. VIP (1-12), human, porcine, rat, ovine is a ligand for the CD4 (T4)/human immunodeficiency virus receptor[1][2].
L-Ornithine L-aspartate is a stable salt of two natural nonessential L-amino acids: ornithine and aspartic acid. L-Ornithine L-aspartate lowers blood ammonia concentration and to eliminate symptoms of hepatic encephalopathy associated with liver cirrhosis[1].
Cytidine 5′-monophosphate-13C9,15N3 (5'-Cytidylic acid-13C9,15N3 dilithium; 5'-CMP-13C9,15N3) dilithium is 13C and 15N-labeled Cytidine 5'-monophosphate (HY-W009162). Cytidine 5'-monophosphate (5'-Cytidylic acid) is a nucleotide which is used as a monomer in RNA. Cytidine 5'-monophosphate consists of the nucleobase cytosine, the pentose sugar ribose, and the phosphate group.
3-Methylpyrazole is used as a nitrification inhibitor of nitrification in soil[1].
AZ-Dyrk1B-33 is a potent and selective Dyrk1B kinase inhibitor, with an IC50 of 7 nM[1].
Platycodin D is a saponin isolated from Platycodi Radix, acts as an activator of AMPKα, with anti-obesity property[1].
Trometamol hydrochloride (Tromethamine hydrochloride) is a biologically inert amino alcohol of low toxicity, which buffers carbon dioxide and acids in vitro and in vivo. Trometamol hydrochloride is an effective amine compound for pH control in the physiological range[1].
Hydroxocobalamin acetate is an injectable naturally occurring form of vitamin B12 with a favorable adverse effect profile, used as a dietary supplement in the treatment of vitamin B12 deficiency including pernicious anemia[1][2].
KY-226 (KY226) is a potent, allosteric, orally active inhibitor of protein tyrosine phosphatase 1B (PTP1B) with IC50 of 0.28 uM (human PTP1B), does not exhibit PPARγ agonist activity; shows no effects on adipocyte differentiation in rodent preadipocytes at 10 uM, bot not the PPARγ agonist pioglitazone; increases the phosphorylated insulin receptor (pIR) produced by insulin in human hepatoma-derived cells (HepG2) at 0.310 uM, significantly reduces plasma glucose and triglyceride levels as well as hemoglobin A1c values without increasing body weight gain in db/db mice, exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling.
cis-Ferulic acid 4-O-β-D-glucopyranoside (compound 7) is a phenolic glycosid, which can be isolated from Nitraria sibirica.. cis-Ferulic acid 4-O-β-D-glucopyranoside exhibits antioxidant activity and potent inhibitory effect on Phosphatase PTP1B[1].
(Ser8)-GLP-1 (7-36) amide, human is a glucagon-like peptide 1 amide derived from glucagonogen, a cleavage product of the GLP-1 (1-36) amide peptide. (Ser8)-GLP-1 (7-36) amide, human is an entero-insulinotropic hormone that causes glucose-dependent release of insulin from pancreatic β-cells and affects gastrointestinal motility and secretion[1].
L-Glyceric acid sodium is a mainly urinary metabolite accumulating in rare inherited metabolic disease L-glyceric aciduria. L-Glyceric acid sodium can be used to diagnose primary hyperoxaluria type 2 (PH2). L-Glyceric acid sodium excretion to distinguish PH1 from PH2[1][2].
SB-435495 is a potent, orally active inhibitor of Lp-PLA2 with IC50 of 0.06 nM; inhibits the enzyme in whole human plasma with IC50 of 3 nM; shows little interaction with other CYP450 enzymes (CYP450 IC50: 1A2>100 mM, 2C9>100 uM, 2C19>40 uM, 2D6=37 uM); effectively suppresses BRB breakdown in streptozotocin-diabetic Brown Norway rats,. Atherosclerosis Phase 2 Discontinued
Witepsol is a selective lipid-based vehicle for use in drug delivery systems[1].
Monoethylglycinexylidide is a metabolite of Lidocain (HY-B0185) via oxidative N-deethylation of Lignocaine by liver cytochrome P-450 enzymes in the liver[1].