performance

Sodium laureth sulfate (Sodium lauryl polyoxyethylene ether sulfate) is an anionic surfactant, with excellent decontamination, wetting, emulsification, dispersion, solubilizing performance and foaming property.

Fipexide (Attentil, Vigilor), a psychoactive drug of the piperazine chemical class, was developed in Italy in 1983. It was served as a nootropic drug in France and Italy, mainly for the therapy of senile dementia, but is no longer in common use because of the occurrence of rare drug side-effects including hepatitis and fever.

N-Methylsarcosine (Dimethylglycine) is used as an athletic performance enhancer and immunostimulant. It is also used in the treatment of autism, epilepsy and mitochondrial disease. It is also employed as a biomarker of protein degradation in chronic obstructive lung disease (COPD) patients. Further, it is used as a substrate to identify, differentiate and characterize amino acid methyltransferase. It plays an important role in the development of glycine-based ionic liquids and emulsifiers.

Benzophenonetetracarboxylic acid (3,3',4,4'-Benzophenonetetracarboxylic acid) is utilized in the preparation of high-performance polyimides and serves as a curing agent for epoxy resins.

1. Nootkatone can provide effective tick control. 2. (+)-Nootkatone has antiallergic, anti-inflammatory, and antiplatelet activities. 3. Nootkatone can prevent obesity and improve physical performance through AMPK activation in skeletal muscle and liver.

TC-MCH 7c is an oral, selectable and blood-brain barrier penetrating MCH1R antagonist with IC50 performance of 5.6 nM against hMCH1R, and TC-MCH 7c is a phenylpyridone derivative with MCH1R Ki of 3.4 nM against human. In mice, MCH1R Ki was 3.0 nM.

BD-AcAc 2 (Ketone Ester) is a ketone monoester and can be used as a source of oral nutritional ketones. BD-AcAc 2 can elevate plasma levels of acetoacetate and β-hydroxybutyrate, blood Na+, blood glucose levels and blood creatinine levels after oral administration in mice. BD-AcAc 2 can partly prevent muscle weakness in septic mice. BD-AcAc 2 exhibits potential to improve endurance and exercise performance in animal body. BD-AcAc 2 can also be used to research diabetes or Parkinson’s disease.

Pridopidine (FR310826), a dopamine (DA) stabilizer, acts as a low affinity dopamine D2 receptor (D2R) antagonist, improves motor performance and shows neuroprotective effects in Huntington disease R6 2 mouse model.

O-desmethyl Brinzolamide is an active metabolite of the carbonic anhydrase (CA) inhibitor brinzolamide .1,2It inhibits CAII and CAIV (IC50s = 0.136 and 165 nM, respectively).1 1.Huang, Q., Rui, E.Y., Cobbs, M., et al.Design, synthesis, and evaluation of NO-donor containing carbonic anhydrase inhibitors to lower intraocular pressureJ. Med. Chem.58(6)2821-2833(2015) 2.Lo Faro, A.F., Tini, A., Gottardi, M., et al.Development and validation of a fast ultra-high-performance liquid chromatography tandem mass spectrometry method for determining carbonic anhydrase inhibitors and their metabolites in urine and hairDrug Test Anal.13(8)1552-1560(2021)

QM-FN-SO3 is a blood-brain barrier (BBB)-penetrable, near-infrared (NIR) probe with aggregation-induced emission (AIE) activity, specifically designed for the detection of Aβ plaques. It exhibits ultra-high signal-to-noise (S/N) ratio, binding affinity, and high-performance NIR emission, making it suitable for in vivo detection of Aβ plaques [1].

BAY-747 (BAY 1165747) is an orally administered, brain-penetrant compound that stimulates soluble guanylate cyclase (sGC). It effectively counteracts memory impairments induced by L-NAME, improves cognitive performance in rats during the object location task (OLT), reduces blood pressure in conscious normotensive and spontaneously hypertensive rats (SHR), and enhances skeletal muscle function in the mdx mTRG2 mouse model of Duchenne muscular dystrophy (DMD) [1] [2] [3].

ELND006 is a novel gamma secretase inhibitor previously under investigation for the oral treatment of Alzheimer's disease. ELND006 shows poor solubility and has moderate to high permeability. The in vivo performance of the ELND006 nanosuspension was tested in fed and fasted beagle dogs and compared with a gelatin capsule containing reference API. The results show that nanosizing ELND006 profoundly improved the oral bioavailability and virtually eliminated variation resulting from food intake.

Myoregulin (MLN peptide) TFA, belonging to the regulin family, is a regulator of muscle performance through modulation of intracellular calcium dynamics. It specifically interacts with sarcoplasmic reticulum Ca2+-ATPase (SERCA) and impedes Ca2+ uptake into the sarcoplasmic reticulum [1] [2].

Methyl brevifolincarboxylate (Brevifolincarboxylic acid methyl ester) is a potent influenza virus PB2 cap-binding inhibitor, exhibiting inhibitory activity against influenza virus A Puerto Rico 8 34 (H1N1) and A Aichi 2 68 (H3N2) with IC50s of 27.16 μM and 33.41 μM, respectively, and possessing anti-oxidant activity[1][2].

TMTD (Tetramethylthiuram disulfide) reduces the growth performance of chickens by reducing liver index, while increasing kidney, heart and spleen index. In addition, TMTD also induces tibial chondrodysplasia (TD) by regulating the expression of VEGF, HIF-1α and WNT4. As a super accelerator in rubber processing, TMTD plays an important role in the low-temperature vulcanization process and is a key pesticide in agriculture.

Suffruticosol A, a neuroprotective compound isolated from the seeds of P. lactiflora [1], mitigates scopolamine-induced neurodegenerative cellular damage and improves hippocampal cholinergic function. Additionally, it partially boosts BDNF signaling and has neuromodulatory effects, leading to the restoration of memory and cognitive performance in a scopolamine-induced mouse model.

Olmesartan medoxomil impurity C is an impurity of Olmesartan medoxomil, a potent and selective angiotensin (AT1 receptor) inhibitor with an IC50 of 66.2 μM.

C26 Sphingomyelin is a sphingolipid that has been found in serum and cell or brain extracts.1,2,3C26 sphingomyelin levels are increased in the serum of patients with hemophagocytic lymphohistiocytosis, an inflammatory condition characterized by excessive immune activation.3C26 sphingomyelin has been used a component of monolayers to study the influence of sphingomyelin acyl chain length on sphingomyelin-sterol interactions.4[Matreya, LLC.] 1.Wang, J.-R., Zhang, H., Yau, L.D., et al.Improved sphingolipidomic approach based on ultra-high performance liquid chromatography and multiple mass spectrometries with application to cellular neurotoxicityAnal. Chem.86(12)5688-5696(2014) 2.Willmann, J., Mahlstedt, K., Leibfritz, D., et al.Characterization of sphingomyelins in lipid extracts using a HPLC-MS-offline-NMR methodAnal. Chem.79(11)4188-4191(2007) 3.Jenkins, R.W., Clarke, C.J., Lucas, J.T., Jr., et al.Evaluation of the role of secretory sphingomyelinase and bioactive sphingolipids as biomarkers in hemophagocytic lymphohistiocytosisAm. J. Hematol.88(11)E265-E272(2013) 4.Li, X.M., Momsen, M.M., Brockman, H.L., et al.Sterol structure and sphingomyelin acyl chain length modulate lateral packing elasticity and detergent solubility in model membranesBiophys. J.85(6)3788-3801(2003)

Hydroxydehydro nifedipine carboxylate is a metabolite of nifedipine .1 1.Roosemalen, M.C.M., Soons, P.A., Funaki, T., et al.High-performance liquid chromatographic determination of the polar metabolites of nifedipine in plasma, blood and urineJ. Chromatogr.565(1-2)516-522(1991)

DL-AP7, a competitive NMDA antagonist and anticonvulsant, blocks NMDA-induced convulsions and impairs learning performance in mice during a passive avoidance task [1].

Mandipropamid exhibits remarkable performance in controlling late blight diseases in potatoes and tomatoes, while also proving highly effective against downy mildew diseases in grapes and cucumbers [1].

GBR 12783 can improve memory performance and increase hippocampal acetylcholine release in rats. GBR 12783 is a specific, potent and selective dopamine uptake inhibitor that inhibits the [3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively.

Reldesemtiv (CK-2127107) is a selective fast skeletal muscle troponin activator with an EC50 of 3.4 μM, enhancing exercise performance in heart failure models.

Antidepressant agent 4, an orally active compound, demonstrates efficacy as an antidepressant with additional anxiolytic, performance-enhancing, and nootropic activities [1].

Avermectin B1a aglycone is an aglycone form of the anthelmintic and insecticide avermectin B1a . It hyperpolarizes P. crassipes muscle fibers with a minimum active concentration (MAC) value of 0.1 μM. Avermectin B1a aglycone decreases survival of C. elegans (MAC = 0.1 μM). In vivo, avermectin B1a aglycone prevents seizures induced by pentylenetetrazole in mice (ED50 = 43.9 mg/kg) without inducing deficits in rotarod performance.

Dityrosine, an oxidation product of protein formed through the intermolecular cross-linking of tyrosyl radicals from the reactive oxygen species (ROS) and tyrosine interaction, is associated with decreased hippocampal expression of NMDA receptor subunits Nr1, Nr2a, and Nr2b when administered intragastrically at 320 µg/kg per day, leading to memory impairments in mice as evidenced by their performance in a novel object recognition test. Additionally, it raises fasting blood glucose levels while reducing plasma insulin levels and the pancreatic expression of insulin synthesis-related genes Ins2, Pdx1, and MafA. Increased dityrosine levels have been positively linked to a range of diseases, including autism spectrum disorder, cataracts, Alzheimer’s disease, Parkinson’s disease, atherosclerosis, and cystic fibrosis.

Positive allosteric modulator of AMPA receptors (pEC50 = 5.2 for potentiation of AMPA-mediated currents in vitro). Also potentiates AMPA-mediated synaptic responses in vivo. Improves performance of rats in various learning and memory paradigms Ward et al (2010) Discovery of N-[(2S)-5-(6-fluoro-3-pyridinyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfonamide, a novel clinical AMPA receptor positive modulator. J.Med.Chem. 53 5801 PMID:20614889 |Ward et al (2017) Pharmacological characterization of N-[(2S)-5-(6-fluoro-3-pyridinyl)-2, 3-dihydro-1H-inden-2-yl]-2-propanesulfonamide: a novel, clinical AMPA receptor positive allosteric modulator. Br.J.Pharmacol. 174 370 PMID:28009436

TRK-IN-12 (Compound 9e), a macrocyclic derivative, is a potent TRK inhibitor, with efficacy against TRK G595R (IC 50 = 13.1 nM). It demonstrates significant antiproliferative activity in the Ba/F3-LMNA-NTRK1 cell line (IC 50 = 0.080 μM) and exhibits superior inhibitory performance (IC 50 = 0.646 μM) compared to the control agent LOXO-101 in the Ba/F3-LMNA-NTRK1-G595R cell line [1].

Antidepressant agent 3, an orally active compound, showcases multifaceted pharmacological properties including antidepressant, anxiolytic, performance-enhancing, and nootropic activities [1].

Follicle-stimulating hormone (FSH), a heterodimeric glycoprotein synthesized by gonadotrophs in the anterior pituitary gland, influences animal fertility and reproductive performance [1] [2].

(±)10-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro.[1][2] It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes.[3][4][5] (±)10-HDHA is a potential marker of oxidative stress in brain and retina where DHA is an abundant polyunsaturated fatty acid. Reference：[1]. VanRollins, M., and Murphy, R.C. Autooxidation of docosahexaenoic acid: Analysis of ten isomers of hydroxydocosahexaenoate. J. Lipid Res. 25(5), 507-517 (1984).[2]. Reynaud, D., Thickitt, C.P., and Pace-Asciak, C.R. Facile preparation and structural determination of monohydroxy derivatives of docosahexaenoic acid (HDoHE) by α-tocopherol-directed autoxidation. Anal. Biochem. 214(1), 165-170 (1993).[3]. VanRollins, M., Baker, R.C., Sprecher, H., et al. Oxidation of docosahexaenoic acid by rat liver microsomes. J. Biol. Chem. 259(9), 5776-5783 (1984).[4]. Yamane, M., Abe, A., and Yamane, S. High-performance liquid chromatography-thermospray mass spectrometry of epoxy polyunsaturated fatty acids and epoxyhydroxy polyunsaturated fatty acids from an incubation mixture of rat tissue homogenate. J. Chromatogr. 652(2), 123-136 (1994).[5]. Kim, H.Y., Karanian, J.W., Shingu, T., et al. Sterochemical analysis of hydroxylated docosahexaenoates produced by human platelets and rat brain homogenate. Prostaglandins 40(5), 473-490 (1990).

1,3,6,8-Pyrenetetrasulfonic acid is an intermediate in the synthesis of the color additive pyranine.1It has been used to stabilize intermolecular interactions for the crystallization ofL. mexicanapyruvate kinase.2 1.Jitian, S., White, S.R., Yang, H.-H.W., et al.Conventional high-performance liquid chromatography versus derivative spectrophotometry for the determination of 1,3,6-pyrenetrisulfonic acid trisodium salt and 1,3,6,8-pyrenetetrasulfonic acid tetrasodium salt in the color additive D&C Green No. 8 (Pyranine)J. Chromatogr. A1324238-241(2014) 2.Morgan, H.P., McNae, I.W., Hsin, K.-Y., et al.An improved strategy for the crystallization of Leishmania mexicana pyruvate kinaseActa Crystallogr. Sect. F Struct. Biol. Cryst. Commun.66(Pt 3)215-218(2010)

1,4-Anthraquinone is an anticancer drug that blocks nucleoside transport, inhibits macromolecule synthesis, induces DNA fragmentation, and decreases the growth and viability of L1210 leukemic cells in the same nanomolar range as daunorubicin in vitro.1,4-

Tat-NTS peptide, a cell-penetrating compound, comprises the HIV-1 Tat protein transduction domain fused with a 10-amino acid sequence (residues 228-237) from the repeat III domain of annexin A1, serving as a nuclear translocation signal (NTS). This peptide hinders the interaction between annexin A1 and importin β, obstructing annexin A1's nuclear entry in primary mouse hippocampal neurons. Tat-NTS effectively prevents apoptosis triggered by glucose-oxygen deprivation and reperfusion in these neurons. When administered in vivo at a dosage of 10 mg/kg, it significantly reduces infarct size, minimizes neuronal apoptosis, and improves navigation performance in the Morris water maze test for mice subjected to ischemia-reperfusion injury via middle cerebral artery occlusion (MCAO).

4-Amino-6-chloro-1,3-benzenedisulfonamide is a carbonic anhydrase inhibitor.1 Formulations containing this compound are diuretics.2 4-Amino-6-chloro-1,3-benzenedisulfonamide is detected as a hydrolysis product of chlorothiazide in the urine.2 Diuretics, including chlorothiazide, have been abused as performance-enhancing drugs and masking agents in sports doping.3References1. Nishimori, I., Vullo, D., Minakuchi, T., et al. Carbonic anhydrase inhibitors: Cloning and sulfonamide inhibition studies of a carboxyterminal truncated α-carbonic anhydrase from Helicobacter pylori. Bioorg. Med. Chem. Lett. 16(8), 2182-2188 (2006).2. Deventer, K., Pozo, O.J., Van Eenoo, P., et al. Detection of urinary markers for thiazide diuretics after oral administration of hydrochlorothiazide and altizide-relevance to doping control analysis. J. Chromatogr. A 1216(12), 2466-2473 (2009).3. Cadwallader, A.B., de la Torre, X., Tieri, A., et al. The abuse of diuretics as performance-enhancing drugs and masking agents in sport doping: Pharmacology, toxicology and analysis. Br. J. Pharmacol. 161(1), 1-16 (2010). 4-Amino-6-chloro-1,3-benzenedisulfonamide is a carbonic anhydrase inhibitor.1 Formulations containing this compound are diuretics.2 4-Amino-6-chloro-1,3-benzenedisulfonamide is detected as a hydrolysis product of chlorothiazide in the urine.2 Diuretics, including chlorothiazide, have been abused as performance-enhancing drugs and masking agents in sports doping.3 References1. Nishimori, I., Vullo, D., Minakuchi, T., et al. Carbonic anhydrase inhibitors: Cloning and sulfonamide inhibition studies of a carboxyterminal truncated α-carbonic anhydrase from Helicobacter pylori. Bioorg. Med. Chem. Lett. 16(8), 2182-2188 (2006).2. Deventer, K., Pozo, O.J., Van Eenoo, P., et al. Detection of urinary markers for thiazide diuretics after oral administration of hydrochlorothiazide and altizide-relevance to doping control analysis. J. Chromatogr. A 1216(12), 2466-2473 (2009).3. Cadwallader, A.B., de la Torre, X., Tieri, A., et al. The abuse of diuretics as performance-enhancing drugs and masking agents in sport doping: Pharmacology, toxicology and analysis. Br. J. Pharmacol. 161(1), 1-16 (2010).

SK609 is a selective dopamine D3 receptor agonist which significantly improves the performance of the impaired paw and normalizes the bilateral asymmetry associated with the hemiparkinson rat.

N-3-hydroxydecanoyl-DL-Homoserine lactone is a bacterial quorum-sensing molecule.1It activates SdiA (EC50= 0.6 μM), a transcription factor that detects N-acyl homoserine lactones (AHLs), in the 14028/pJNS25 strain ofS. enterica.2 1.Fekete, A., Frommberger, M., Rothballer, M., et al.Identification of bacterial N-acylhomoserine lactones (AHLs) with a combination of ultra-performance liquid chromatography (UPLC), ultra-high-resolution mass spectrometry, and in-situ biosensorsAnal. Bioanal. Chem.387455-467(2007) 2.Janssens, J.C.A., Metzger, K., Daniels, R., et al.Synthesis of N-acyl homoserine lactone analogues reveals strong activators of SdiA, the Salmonella enterica serovar Typhimurium LuxR homologueAppl. Environ. Microb.73(2)535-544(2007)

Isophthalic acid is an intermediate for a modifier of polyethylene terephthalate for bottles, gel coats, high solids paints, resins for coatings, and high-performance unsaturated polyesters.

AMPA Receptor Modulator-4, a 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide (BTD), serves as an orally active positive allosteric modulator of the AMPA receptors (AMPAR PAMs). This compound is capable of crossing the blood-brain barrier and has been found to enhance cognitive performance and working memory in mice [1].

GBR 12783 dihydrochloride (GBR12783 2HCl) is a specific, potent and selective dopamine uptake inhibitor. GBR 12783 dihydrochloride inhibits the [3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively.GBR 12783 dihydrochloride can improve memory performance and increase hippocampal acetylcholine release in rats.

C2-8 is an inhibitor of polyglutamine (polyQ) aggregation with IC50s of 25 and 0.05 μM for recombinant HDQ51 and in PC12 cells, respectively. It also limits polyQ aggregation in organotypic hippocampal slice cultures from R6 2 transgenic mice and reduces neurodegeneration dose-dependently in a Drosophila model of Huntington's disease. C2-8 (100 and 200 mg kg) decreases huntingtin aggregate size, reduces neuronal atrophy, and enhances motor performance in a rotarod test in the R6 2 transgenic mouse model of Huntington's disease.

WLSEAGPVVTVRALRGTGSW TFA, a cardiomyocyte-specific peptide, exhibits enhanced performance through its expression in exosomes, which notably improves uptake by cardiomyocytes, reduces apoptosis within these cells, and increases cardiac retention after intramyocardial injection in vivo [1] [2].

Stick Insect Hypertrehalosaemic Factor II, a synthetic peptide, exhibits identical FAB spectra, reversed-phase high-performance liquid chromatographic profiles (behavior), and biological activity (behavior) as its natural counterpart and is utilized in researching the hypertrehalosaemic effect [1].

PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor (IC50= 22 nM).1It is selective for PDE9A over PDE1C (IC50= >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 μM but does inhibit the human dopamine transporter (DAT; Ki= 293 nM). PF-04449613 (0.1-100 mg/kg, s.c.) increases cerebrospinal fluid (CSF) levels of cyclic GMP (cGMP) in rats. Subcutaneous administration of PF-04449613 (10 mg/kg) increases the rate of dendritic spine formation and elimination in mouse primary motor cortex pyramidal neuronsin vivo.2It increases the average running speed of mice in an accelerating rotarod task, indicating improved motor learning, at the same dose. 1.Claffey, M.M., Helal, C.J., Verhoest, P.R., et al.Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitorsJ. Med. Chem.55(21)9055-9068(2012) 2.Lai, B., Li, M., Hu, A., et al.The phosphodiesterase 9 inhibitor PF-04449613 promotes dendritic spine formation and performance improvement after motor learningDev. Neurobiol.78(9)859-872(2018)

Q134R, a neuroprotective derivative of hydroxyquinoline, effectively inhibits nuclear factor of activated T-cell (NFAT) signaling and possesses the ability to cross the blood-brain barrier. This compound shows promise for research into Alzheimer’s disease (AD) and aging-related disorders[1].

0 [1]. Fan Z, Jia S, Ding N, et al. Determination of Fosetyl-Aluminium by Ion-Pair Reversed Phase-High Performance Liquid Chromatography With Evaporative Light Scattering Detection. Se Pu. 2009;27(6):849‐851. [2]. TüRK LMEZ , et al. Activity of metalaxyl-M+mancozeb, fosetyl-Al, and phosphorous acid against Phytophthora crown and root rot of apricot and cherry caused by Phytophthora palmivora. Plant Protect. Sci., 53: 216-225.

Bibn 99, a lipophilic and selective muscarinic M2 receptor antagonist, has applications in cognitive performance and Alzheimer's Disease.

Cytidine-5’-O-(2-thiodiphosphate) (CDP-β-S), a non-hydrolyzable derivative of CDP exhibiting antioxidant activity, effectively scavenges free radicals as evidenced by its performance in the Trolox equivalent absorbance capacity (TEAC) assay at concentrations between 5 and 20 µM.

SK1071 is a novel migrastatin analogs, which demonstrated improved performance over migrastatin, with nanomolar IC50 values in chamber cell migration assays with tumor cells and human umbilical vein endothelial cells (HUVECs), and in wound healing assays.

Sildenafil chlorosulfonyl is a synthetic intermediate in the synthesis of the phosphodiesterase 5 (PDE5) inhibitor sildenafil .1It is also a potential impurity found in commercial preparations of sildenafil. 1.Nagaraju, V., Sreenath, D., Rao, J.T., et al.Separation and determination of synthetic impurities of sildenafil (Viagra) by reversed-phase high-performance liquid chromatographyAnal. Sci.19(7)1007-1011(2003)