Chemical Structure : hCES2A inhibitor C3
CAS No.:
2396634-07-2
hCES2A inhibitor C3
Catalog No.: PC-25706Not For Human Use, Lab Use Only.
hCES2A inhibitor C3 is a highly potent, orally active and serine-targeting covalent inhibitor of hCES2A (human carboxylesterase 2A) with IC50 of 0.56 nM, Ki of 1.58 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
hCES2A inhibitor C3 is a highly potent, orally active and serine-targeting covalent inhibitor of hCES2A (human carboxylesterase 2A) with IC50 of 0.56 nM, Ki of 1.58 nM.
hCES2A inhibitor C3 shows dose-dependent inhibition against intracellular hCES2A with IC50 of 2.35 nM in living HepG2 cells.
hCES2A inhibitor C3 dose-dependently inhibits CES2A-catalyzed irinotecan hydrolysis in mouse intestinal S9 and human intestinal S9with IC50 of 90.35 nM and 32.79 nM respectively.
hCES2A inhibitor C3 shows exceptional selectivity towards hCES2A, with no activity against other human serine hydrolases at 10 uM, including hCES1A, hNotum, hPL, hThrombin, hDPP-IV, and hAChE.
hCES2A inhibitor C3 (25 and 50 mg/kg) significantly ameliorates ITGT in tumor-bearing mice, effectively reverses the morphological damage of irinotecan-challenged colon tissues.
Physicochemical Properties
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M.Wt
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381.43
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Formula
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C22H23NO5
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-((5,6-dimethoxy-1-oxo-1,3-dihydro-2H-inden-2-ylidene)methyl)phenyl ethyl(methyl)carbamate
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References
1. Zhang Y, et al. Acta Pharm Sin B. 2025 Oct;15(10):5312-5326.
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