7-Methylguanine, a metabolite of DNA methylation, is generated by methylating agents. It is utilized as a probe for DNA–protein interactions and serves as a crucial component in DNA sequencing methods.
Octanophenone can be analyzed by reverse phase (RP) HPLC method with simple conditions. The phosphoric acid needs to be replaced with formic acid for Mass-Spec (MS) compatible applications. For fast UPLC applications, smaller 3 µm particles columns is av
FR-186054 is a new, potent inhibitor of acyl-CoA:cholesterol O-acyltransferase (ACAT) and has oral activity. Compared to other ACAT inhibitors, this compound displayed excellent in vitro efficacy, irrespective of dosing method, indicating superior charact
DA 3505 is one of feprazone metabolite. Limits of detection are 0.1 microgram feprazone per ml plasma and 0.2 microgram of its metabolite per ml plasma using the HPLC method. Concentration down to about 0.5 microgram/ml plasma of both compounds can be det
β-D-Ribofuranose 1,2,3,4-tetraacetate is a precursor in the synthesis of nucleosides with antiproliferative activity against cancer cells.1,2 1.Furukawa, Y., and Honjo, M.A novel method for the synthesis of purine nucleosides using Friedel-Crafts catalystsChem. Pharm. Bull. (Tokyo)16(6)1076-1080(1968) 2.Wicke, L., Engels, J.W., Gambari, R., et al.Synthesis and antiproliferative activity of quinolone nucleosides against the human myelogenous leukemia k-562 cell lineArch. Pharm. (Weinheim)346(10)757-765(2013)
BODIPY-aminoacetaldehyde diethyl acetal (BAAA-DA) is a stable precursor to BODIPY-aminoacetaldehyde, a cell-permeable fluorescent substrate for aldehyde dehydrogenase (ALDH).1,2BODIPY-aminoacetaldehyde diethyl acetal is converted under acidic conditions to BODIPY-aminoacetaldehyde (BAAA).2BAAA is cell-permeant and is converted intracellularly by ALDH to BODIPY aminoacetate (BAA), which is retained by cells and can be used to identify cells with high ALDH activity.1BAA is a substrate for the efflux pump P-glycoprotein (P-gp) but co-application of BAAA with a P-gp inhibitor, such as verapamil , inhibits BAA efflux.2BAAA-DA has been used to isolate human hematopoietic progenitor cells, which have high ALDH activity, andviaflow cytometry to sort cancer stem cells that contain high levels of ALDH.1,3BAA used in cells can be excited at 488 nm and displays an emission maximum of 512 nm.4 1.Storms, R.W., Trujillo, A.P., Springer, J.B., et al.Isolation of primitive human hematopoietic progenitors on the basis of aldehyde dehydrogenase activityProceedings of the National Academy of Sciences of the United States of America96(16)9118-9123(1999) 2.Smith, C.A., Colvin, M., Storms, R.W., et al.BODIPY aminoacetaldehyde diethyl acetal08010501.81-15(2010) 3.Leng, Z., Yang, Z., Li, L., et al.A reliable method for the sorting and identification of ALDHhigh cancer stem cells by flow cytometryExp. Ther. Med.(2017) 4.Pomper, M.G., Wang, H., Minn, I., et al.Red fluorescent aldehyde dehydrogenase (ALDH) substrate(2015)
O-Des[2-aminoethyl]-O-carboxymethyl dehydroamlodipine is a major metabolite of the calcium channel inhibitor amlodipine .1 1.Taguchi, R., Naito, T., Sato, H., et al.Validated LC-MS/MS method for the simultaneous determination of amlodipine and its major metabolites in human plasma of hypertensive patientsTher. Drug Monit.39(6)625-631(2017)
O-Demethyl apremilast is an active metabolite of the phosphodiesterase 4 (PDE4) inhibitor apremilast .1It inhibits the activity of PDE4 isolated from U937 cells and LPS-induced TNF-α production in isolated human peripheral blood mononuclear cells (PBMCs; IC50s = 8.3 and 5.6 μM, respectively). O-Demethyl apremilast is also an oxidative degradation product of apremilast.2,3 1.Hoffmann, M., Kumar, G., Schafer, P., et al.Disposition, metabolism and mass balance of [14C]apremilast following oral administrationXenobiotica41(12)1063-1075(2011) 2.Lu, Y., Shen, X., Hang, T., et al.Identification and characterization of process-related substances and degradation products in apremilast: Process optimization and degradation pathway elucidationJ. Pharm. Biomed. Anal.14170-78(2017) 3.Bhole, R.P., Naksakhare, S.R., and Bonde, C.G.A stability indicating HPTLC method for apremilast and identification of degradation products using MS MSJ. Pharm. Sci. & Res.11(5)1861-1869(2019)
DEPMPO is a nitrone that is used to spin trap reactive O-, N-, S-, and C-centered radicals and allow their characterization when used in association with electron spin resonance. It is noted for the stability of adducts formed. DEPMPO can be used in vitro or in vivo, as it crosses lipid bilayer membranes and is a good trapping agent in biological systems. DEPMPO-biotin is a biotinylated form of DEPMPO which retains the outstanding persistency of its adducts. The biotin moiety offers an effective means for monitoring biodistribution in cells, tissues, and organs when used with an avidin-conjugated reporter. Importantly, DEPMPO-biotin binds free radicals, such as S-nitroso groups, on proteins, producing adducts that can be analyzed via the biotin tag. This direct labeling of S-nitrosothiols (SNO) thus serves as an effective alternative to the more cumbersome biotin-switch method for monitoring SNO formation.
Pal-KTTKS is a lipidated pentapeptide consisting of a fragment of the type I collagen C-terminal propeptide conjugated to palmitic acid .1 It increases collagen production in human corneal and dermal fibroblasts when used at concentrations of 0.002, 0.004, and 0.008 wt%.2 Following topical administration, pal-KTTKS (50 μg/cm2) is found in the stratum corneum, epidermis, and dermis of isolated hairless mouse skin.1 It can self-assemble into flat tapes and extended fibrillar structures.3 Pal-KTTKS has been detected in anti-wrinkle creams.4 |1. Choi, Y.L., Park, E.J., Kim, E., et al. Dermal stability and in vitro skin permeation of collagen pentapeptides (KTTKS and palmitoyl-KTTKS). Biomol. Ther. (Seoul) 22(4), 321-327 (2014).|2. Jones, R.R., Castelletto, V., Connon, C.J., et al. Collagen stimulating effect of peptide amphiphile C16-KTTKS on human fibroblasts. Mol. Pharm. 10(3), 1063-1069 (2013).|3. Castelletto, V., Hamley, I.W., Whitehouse, C., et al. Self-assembly of palmitoyl lipopeptides used in skin care products. Langmuir 29(29), 9149-9155 (2013).|4. Chirita, R.-I., Chaimbbault, P., Archambault, J.-C., et al. Development of a LC-MS/MS method to monitor palmitoyl peptides content in anti-wrinkle cosmetics. Anal. Chim. Acta 641(1-2), 95-100 (2009).
8-hydroxy Amoxapine is a metabolite of the tetracyclic antidepressant amoxapine .1,2 1.Johnson, S.M., Nygard, G., and Khalil, S.K.Isocratic liquid chromatographic method for the determination of amoxapine and its metabolitesJ. Pharm. Sci.73(5)696-699(1984) 2.Tasset, J.J., and Pesce, A.J.Amoxapine in human overdoseJ. Anal. Toxicol.8(3)124-128(1984)
Palonosetron N-oxide is a metabolite of the serotonin (5-HT) receptor subtype 5-HT3antagonist palonosetron .1It is also a potential impurity in palonosetron preparations.2Palonosetron N-oxide is a degradation product formed by exposure to oxidative stress. 1.Stoltz, R.A., Cyong, J.-C., Shah, A., et al.Pharmacokinetic and safety evaluation of palonosetron, a 5-hydroxytryptamine-3 receptor antagonist, in U.S. and Japanese healthy subjectsJ. Clin. Pharmacol.44(5)520-531(2004) 2.Vishnu Murthy, M., Srinivas, K., Kumar, R., et al.Development and validation of a stability-indicating LC method for determining palonosetron hydrochloride, its related compounds and degradation products using naphthalethyl stationary phaseJ. Pharm. Biomed. Anal.56(2)429-435(2011)
5,6-dimethyl-2-Thiouracil is a heterocyclic building block that has been used in the synthesis of anti-HIV-1 pyrimidinones.1 It has also been used as an internal standard for the quantification of thyreostats, including 2-thiouracil, in bovine plasma.2 |1. Navrotskii, M.B. Synthesis and anti-HIV-1 activity of new 2-[(2-phthalimidoethyl)thio]-4(3H)-pyrimidinone derivatives. Pharm. Chem. J. 39(9), 466-467 (2005).|2. Schmidt, K.S. In-house validation and factorial effect analysis of a liquid chromatography-tandem mass spectrometry method for the determination of thyreostats in bovine blood plasma. Anal. Bioanal. Chem. 406(3), 735-743 (2014).