Ezurpimtrostat (compound 2-2) is used for the study of fibrosis, cancer, autophagy and cathepsins B (CTSB), L (CTSL) and D (CTSD) related diseases (extracted from patent WO2020048694 A1)[1].
LY3104607 (LY-3104607) is a potent, selective, orally available GPR40 agonist with Ki of 15 nM, β-arrestin EC50 of 108 nM; demonstrates functional potency and glucose dependent insulin secretion in primary islets from rats; dose-dependently reduces glucose levels in vivo.
Rhodiosin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.420 μM and a Ki of 0.535 μM[1]. Rhodiosin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL[2]. Rhodiosin exhibits potent DPPH free radical scavenging activities, with an IC50 of 27.77 μM[3].
L-CCG-I is an extended isomer of conformationally restricted glutamate analog. L-CCG-I also is a potent agonist for mGluR2 with an EC50 value of 0.3 nM. L-CCG-I can be used for the research of mGluR family[1].
URAT1&XO inhibitor 1 (compound 29) is a dual inhibitor of both URAT1 (IC50=~10 μM) and Xanthine Oxidase (IC50=1.01 μM). URAT1&XO inhibitor 1 results hypouricemic effect in potassium oxonate-induced hyperuricemia rat model. URAT1&XO inhibitor 1 is used for hyperuricemia research[1].
IM176OUT05 is a high solubility biguanide. IM176OUT05 activates stem cell metabolism, promotes hair regrowth and increases stemness induction and maintenance during the pluripotent stem cell generation process. IM176OUT0 inhibits mitochondrial electron transport chain (ETC) activity with an IC50 of 3.2 μM[1].
D-Glucose-13C2,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 si
Tigogenin, one of steroidal sapogenins, is widely used for synthesizing steroid drugs. Tigogenin inhibits adipocytic differentiation and induces osteoblastic differentiation in mouse bone marrow stromal cells[1].
Acts on β-galactosyl-1,4-N-acetylglucosaminyl termini on asialo-α1-acid glycoprotein and N-acetyllactosamine (β-D-galactosyl-1,4-N-acetyl-β-D-glucosamine), but not on 2'-fucosylated-N-acetyllactosamine. The non-reducing terminal N-acetyllactosamine residues of glycoproteins can also act as acceptor. Now includes EC 2.4.1.124 and EC 2.4.1.151. Reaction: UDP-α-D-galactose + β-D-galactosyl-(1→4)-β-N-acetyl-D-glucosaminyl-R = UDP + α-D-galactosyl-(1→3)-β-D-galactosyl-(1→4)-β-N-acetylglucosaminyl-R (where R can be OH, an oligosaccharide or a glycoconjugate)
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].
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].
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].
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].
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].
Mildronate (Meldonium) functions as a cardioprotective drug by cpmpetetively inhibiting BBOX1 and OCTN2. Mildronate (Meldonium) exhibits IC50 values of 34-62 μM for human recombinant BBOX and an EC50 of 21 μM for human OCTN2. Mildronate (Meldonium) treatment-induced redirection of long-chain FA metabolism from mitochondria to peroxisomes[1].
IGF-I (30-41) is amino acids 30 to 41 fragment of Insulin-like Growth Factor I (IGF-I). IGF-I is partly responsible for systemic GH activities although it possesses a wide number of own properties (anabolic, antioxidant, anti-inflammatory and cytoprotective actions)[1].
(R)-3-Hydroxybutanoic acid-13C (sodium) is the 13C labeled (R)-3-Hydroxybutanoic acid sodium[1]. (R)-3-Hydroxybutanoic acid sodium ((R)-3-Hydroxybutyric acid) is a metabolite converted from acetoacetic acid catalyzed by 3-hydroxybutyrate dehydrogenase. (R)-3-Hydroxybutanoic acid sodium can function as a nutrition source, and as a precursor for vitamins, antibiotics and pheromones[2][3].
D-Thyroxine (D-T4) is a thyroid hormone that can inhibit TSH secretion. D-Thyroxine can be used for the research of hypercholesterolemia[1][2].
OHM 11638 (Atilmotin), an analogue of the (1-14) fragment of porcine motilin, is a motilin receptor agonist with a pKd of 8.94 for the motilin receptor. OHM 11638 affects esophageal, lower esophageal sphincter (LES), and gastric motility. OHM 11638 increases LES and gastric pressures, OHM 11638 can be used as prokinetic agents[1][2].
Nebicapone (BIA 3-202), a reversible catechol-O-methyltransferase (COMT) inhibitor, is mainly metabolized by glucuronidation. Nebicapone is mainly peripherally acting inhibitor that decreases the biotransformation of L-DOPA to 3-O-methyl-DOPA by inhibition of COMT, and it is potential for the treatment of Parkinson's disease.[1].
PPARγ/δ modulator 1 (compound 3e) is a potent PPAR modulator. PPARγ/δ modulator 1 is a PPARδ antagonist and a PPARγ partial agonist , with Ki values of 14.4 nM and 5.31 μM, respectively. PPARγ/δ modulator 1 has the EC50 of 7.3 and 12.6 μM for PPARδ corepression and adiponectin production, respectively[1].
L-Carnitine hydrochloride ((R)-Carnitine hydrochloride), a highly polar, small zwitterion, is an essential co-factor for the mitochondrial β-oxidation pathway. L-Carnitine hydrochloride functions to transport long chain fatty acyl-CoAs into the mitochondria for degradation by β-oxidation. L-Carnitine hydrochloride is an antioxidant. L-Carnitine hydrochloride can ameliorate metabolic imbalances in many inborn errors of metabolism[1][2][3].
Desacetyl bisacodyl is the active metabolite of the laxative bisacodyl. Desacetyl bisacodyl induces epithelial Cl(-) secretion in rat colon and rectum. Desacetyl bisacodyl evokes several effects at the colon or rectum, including increased mucus and chloride secretion[1].
Famotidine is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.Target: Histamine H2 ReceptorFamotidine is a histamine H2-receptor antagonist that inhibits stomach acid production, and it is commonly used in the treatment of peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD/GORD). Famotidine Group(2 mg/kg/day) were significantly lower than the equivalent parameters for the Control Group on both the third and seventh days post-surgery. famotidine exerts detrimental effects on the anastomotic bursting pressure and hydroxyproline content of perianastomotic tissues in the colon of rats [1]. famotidine increased the transgastric potential difference (PD) and promoted the recovery of decreased transgastric PD induced by acidified ethanol in rats. The preventive effect of famotidine on gastric lesions is attributable not only to suppression of acid secretion but to activation of the gastric mucosal defensive mechanisms [2].
trans-trans-Muconic acid-d4 is the deuterium labeled trans-trans-Muconic acid[1]. trans-trans-Muconic acid is a urinary metabolite of benzene and has been used as a biomarker of exposure to benzene in human[2].
Ezurpimtrostat hydrochloride (compound 2-3) is a potent and orally active anti-fibrotic agent. Ezurpimtrostat hydrochloride reduces significantly the liver fibrosis in DEN (diethyl nitrosamine) cirrhotic rat model. Ezurpimtrostat hydrochloride can be used for the research of fibrosis, cancer, autophagy and cathepsins B (CTSB), L (CTSL) and D (CTSD) related diseases [1].
ML 10302 hydrochloride is a potent and selective 5-HT4 receptor agonist, with an EC50 of 4 nM。ML 10302 hydrochloride displays more than 680-fold selectivity over 5-HT3 receptor in binding assay[1][2].
Hexokinase is a glycolytic enzyme hexokinase that is inhibited by n-acetylglucosamine. Inhibition of hexokinase by n-acetylglucosamine leads to its separation from the mitochondrial outer membrane, resulting in activation of NLRP3 inflammasome[1].