PKR activator 4 (example 7A) is a potent pyruvate kinase R (PKR) activator. PKR activator 4 has the potential for the research of blood disorders[1].
Clorgyline hydrochloride is an irreversible and selective inhibitor of monoamine oxidase A (MAO-A) that is used in scientific research; structurally related to Pargyline.
4-Chlorophenylacetic acid is a compound belongs to a family of small aromatic fatty acids with anticancer properties. 4-Chlorophenylacetic acid can provide carbon and energy for Pseudomonas sp[1][2].
α-Eleostearic acid (cis-Eleostearic acid), a conjugated linolenic acid, is an apoptosis inducer. α-Eleostearic acid is also a ferroptosis inducer. α-Eleostearic acid exhibits antioxidant and antitumor activity[1][2][3].
Dexloxiglumide is a selective cholecystokinin type A (CCKA) receptor antagonist[1]. Dexloxiglumide, the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8)[2].
Pantothenate kinase-IN-2 is a potent Pantothenate kinase 1/3 (PanK1/3) inhibitor with an IC50 of 0.14 μM and 0.36 μM. Pantothenate kinase-IN-2 is a promising agent for PKAN (PanK-associated neurodegeneration) and diabetes research[1].
CB1R Allosteric modulator 5, a novel1-sulfonyl-4-acylpiperazines as selective cannabinoid-1 receptor (CB1R) inverse agonist with an IC50 value of 4.2 μM and EC50 value of ＞10 μM. CB1R Allosteric modulator 5 can be used for the research of metabolic and obesity[1].
Tyrosinase-IN-11 is a potent tyrosinase inhibitor with IC50s of 50 nM and 64 nM for L-tyrosinase and L-dopa, respectively. Tyrosinase-IN-11 has significant antioxidant activity and low cytotoxicity. Tyrosinase-IN-11 has the potential for skin hyperpigmentation research[1].
Dapagliflozin (BMS-512148) is a sodium-glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes.
O-Desmethylangolensin is a metabolite of soy isoflavone, daidzein metabolized by gut microbiota. O-Desmethylangolensin possesses antioxidant activity[1][2].
Ethylenediaminetetraacetic acid (EDTA) disodium dihydrate is a chelating agent used as a protease inhibitor and metal ion scavenger. Ethylenediaminetetraacetic acid disodium dihydrate is used extensively during protein purification. Ethylenediaminetetraacetic acid disodium dihydrate has been shown to be a noneffective molecule on cellulase activity. Ethylenediaminetetraacetic acid disodium dihydrate binds to metals including calcium and facilitates their excretion[1][2].
N-Arachidonyl maleimide is a potent, irreversible inhibitor of monoacylglycerol lipase (MAGL) with an IC50 value of 140 nM[1].
Rubrofusarin 6-O-β-D-glucopyranoside, the glycoside of Rubrofusarin, is a protein tyrosine phosphatase 1B (PTP1B) inhibitor with the IC50 of 87.36 μM. Rubrofusarin 6-O-β-D-glucopyranoside can be used for the research of comorbid diabetes and depression[1].
Arzoxifene (LY353381) is an orally active selective estrogen receptor modulator with a fixed ring structure similar to raloxifene. Arzoxifene has minimal side effects with powerful antiestrogenic effects on breast cancer and endometrium, with equally strong favorable estrogenic effects on bone and lipid profile[1].
Phenylglyoxylic acid (Benzoylformic acid) is a metabolite of ethylbenzene and styrene (EB/S) and can be used as a biomarker of exposure to EB/S in human[1].
(R)-(-)-1,2-Propanediol is a (R)-enantiomer of 1,2-Propanediol that produced from glucose in Escherichia coli expressing NADH-linked glycerol dehydrogenase genes[1].
Senecionine is a pyrrolizidine alkaloid isolated from Senecio vulgaris. Senecionine is toxic to animals and humans.
Linoleic Acid-d2 is the deuterium labeled Linoleic acid. Linoleic acid is a common polyunsaturated (PUFA) found in plant-based oils, nuts and seeds. Linoleic acid is a part of membrane phospholipids, and functions as a structural component to maintain a certain level of membrane fluidity of the transdermal water barrier of the epidermis. Linoleic acid induces red blood cells and hemoglobin damage via oxidative mechanism[1][2].
Ertugliflozin-d5 is the deuterium labeled Ertugliflozin[1]. Ertugliflozin (PF-04971729) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2[2]. Has the potential for the treatment of type 2 diabetes mellitus[3].
Alvimopan(LY 246736; ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery. IC50 Value: 1.7 nM (Mu-type opioid receptor) [1]Target: mu-opioid receptorin vitro: The dissociation rate of alvimopan from the micro opioid receptor (t(1/2)=30--44 min) was comparable to that of the long acting partial agonist buprenorphine (t(1/2)=44 min), but was slower than those of the antagonists naloxone (t(1/2)=0.82 min) and N-methylnaltrexone (t(1/2)=0.46 min) [2].in vivo: Alvimopan did not significantly accelerate GI-3 compared with placebo [6 mg: hazard ratio (HR) = 1.20, p = 0.080; 12 mg: HR = 1.24, p = 0.038). However, after adjustment for significant covariates (sex/surgical duration), benefits were significant for both doses (6 mg: HR = 1.24, p = 0.037; 12 mg: HR = 1.26, p = 0.028). Alvimopan also significantly accelerated time to GI-2 (6 mg: HR = 1.37, p = 0.008; 12 mg: HR = 1.33, p = 0.018) and DCO (6 mg: HR = 1.31, p = 0.008; 12 mg: HR = 1.28, p = 0.015) [3]. Alvimopan (1 and 3 mg/kg) significantly reversed this delayed GI transit when administered 45 min prior to surgery. However, the effects of alvimopan were less pronounced when administered following surgery [4].Toxicity:The most common treatment-emergent adverse events across all treatment groups were nausea, vomiting, and hypotension; the incidence of nausea and vomiting was reduced by 53 percent in thealvimopan 12-mg group [5].Clinical trial: Intercostal Nerve Block With Liposome Bupivacaine in Subjects Undergoing Posterolateral Thoracotomy. Phase 3
Indole-d7 is the deuterium labeled Indole[1]. Indole is an endogenous metabolite.
Picoprazole is a specific inhibitor of H+/K+-ATPase with IC50 of 3.1±0.4 μM.
Monobutyl phthalate, a major metabolite of dibutyl phthalate (DBP), possesses antiandrogenic effects. Monobutyl phthalate is an embryotoxicant[1][2].
Thiamine pyrophosphate is the coenzyme form of Vitamin B1 and is a required intermediate in the pyruvate dehydrogenase complex and the ketoglutarate dehydrogenase complex.
2-Ethylpyrazine-d5 is the deuterium labeled 2-Ethylpyrazine[1]. 2-Ethylpyrazine is an endogenous metabolite.
2,4,6-Trihydroxybenzaldehyde is an orally active NF-ĸB inhibitor. 2,4,6-Trihydroxybenzaldehyde shows anti-tumor activity, anti-cancer cell proliferative activity and anti-obesity activity[1][2][3].
(R)-Etomoxir sodium salt is the R-form of Etomoxir sodium salt, acts as an inhibitorof carnitine palmitoyltransferase I (CPT-I), and inhibits palmitate β-oxidation in human, rat and guinea pig.
Desmethyl Sibutramine hydrochloride, the secondary metabolite of Sibutramine, is an orally active norepinephrine transporter (NET) and serotonin transporter (SERT) inhibitor. Desmethyl Sibutramine hydrochloride can be used in the research of obesity and appetite suppressant[1][2][3][4].
SIRT1 activator 3 is a potent activator of Sirt1 and suppresses TNF-α in a dose-dependent manner. SIRT1 activator 3 has the potential for anti-obesity or anti-diabetic researches[1].
Fulvine is a pyrrolizidine alkaloid isolated from the seeds of Crotalaria fulva. Fulvine is hepatotoxic and can be used to induce hypertensive pulmonary vascular disease in vivo[1].