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Anordrin is predominantly catalyzed by CES1 and CES2 to generate the main active metabolite, anordiol.
genetic association and pharmacogenomic studies in population in Finland: Data suggest that 2 SNPs in CES1 (rs12443580, rs8192935) are associated with variations in expression of CES1 (in whole blood samples but not in liver); these CES1 SNPs do not affect pharmacokinetics or pharmacodynamics of clopidogrel, an inhibitor of platelet aggregation. A missense mutation in CES1 (rs71647871) impairs hydrolysis of clopidogrel.
The frequencies of SNVs with a potential functional impact were below 0.02 suggesting limited pharmacogenetic potential for CES1 genotyping.
none of the selected variations of CES1 had a clinically relevant impact on the metabolism of enalapril
Study revealed that several nsSNPs significantly impaired CES1 activity on the metabolism of the CES1 substrates enalapril, clopidogrel, and sacubitril.
Suggest a primary metabolic role for CES1 in the capacity of skin/keratinocytes to mediated biotransformation of penta-ethyl ester prodrug of DTPA.
These data suggest that infants younger than 3 weeks of age would exhibit significantly lower CES1- and CES2-dependent metabolic clearance compared with older individuals.
The intestinal transport of oseltamivir, a hCE1 (show RNGTT Antibodies) substrate, could be evaluated in subclone #78 cell monolayers.
An association was identified with a genetic variation in CES1 and early-onset capecitabine-related toxicity.
Reduced CES1 expression/activity could promote development of METH-PAH.
Loss of CES1 is associated with the susceptibility to high cholesterol diet-induced liver injury.
Hepatic Ces1g/Es-x plays a critical role in limiting hepatic steatosis, very low-density lipoprotein assembly and in augmenting insulin (show INS Antibodies) sensitivity.
Data indicate that organic anion-transporting polypeptides Oatp1a/1b-null mice had increased levels of carboxylesterase (Ces) enzymes, which caused higher conversion of irinotecan to SN-38 in plasma, potentially complicating pharmacokinetic analyses.
Hepatic CES1 plays a critical role in regulating both lipid and carbohydrate metabolism and FXR (show NR1H4 Antibodies)-controlled lipid homeostasis
One novel isoform termed alternative pig liver esterase (show ESD Antibodies) (APLE) was found to hydrolyze methyl-(2R,4E)-5-chloro-2-isopropyl-4-pentenoate in a highly stereoselective manner (E>200).
The objective of this study is to explore the mechanisms that regulate TGH expression in porcine adipocyte and its role in fasting-induced (show C10orf10 Antibodies) and Isoproterenol-stimulated lipolysis in porcine primary adipocytes.
PMPMEase was purified to apparent homogeneity from porcine liver supernatant.
This gene encodes a member of the carboxylesterase large family. The family members are responsible for the hydrolysis or transesterification of various xenobiotics, such as cocaine and heroin, and endogenous substrates with ester, thioester, or amide bonds. They may participate in fatty acyl and cholesterol ester metabolism, and may play a role in the blood-brain barrier system. This enzyme is the major liver enzyme and functions in liver drug clearance. Mutations of this gene cause carboxylesterase 1 deficiency. Three transcript variants encoding three different isoforms have been found for this gene.
acyl coenzyme A:cholesterol acyltransferase
, acyl-coenzyme A:cholesterol acyltransferase
, brain carboxylesterase hBr1
, carboxylesterase 1 (monocyte/macrophage serine esterase 1)
, carboxylesterase 2 (liver)
, cholesteryl ester hydrolase
, cocaine carboxylesterase
, human monocyte/macrophage serine esterase 1
, liver carboxylesterase 1
, methylumbelliferyl-acetate deacetylase 1
, monocyte/macrophage serine esterase
, retinyl ester hydrolase
, serine esterase 1
, triacylglycerol hydrolase
, carboxylesterase 1
, carboxylesterase D1
, alternative pig liver esterase
, liver carboxylesterase
, prenylated methylated protein methyl esterase