Diclofenac acyl glucuronide
Based on 1 Customer Validation
Diclofenac acyl glucuronide (D-1-O-G) is an orally active glucuronide metabolite of Diclofenac (HY-15036). Diclofenac acyl glucuronide exhibits SOD inhibitory activity, COX-1 inhibitory activity (IC50 = 0.620 μM), and COX-2 inhibitory activity (IC50 = 2.91 μM). Diclofenac acyl glucuronide induces reactive oxygen species (ROS) production and acts as a substrate of OATP2B1. Diclofenac acyl glucuronide induces small intestinal ulcers. Diclofenac acyl glucuronide can be used in research related to intestinal diseases and small intestinal ulcers.
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- Pureté: 98.34%
- CAS No.: 64118-81-6
- Formule: C20H19Cl2NO8
- Masse moléculaire:472.27
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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COX-1 0.620 μM (IC50) |
COX-2 2.91 μM (IC50) |
Diclofenac acyl glucuronide (1-300 μM; 0.1-2 min) serves as a substrate of OATP2B1 in HEK-OATP2B1 cells, with higher uptake activity at pH 6.0; its Vmax is 27.8 pmol/min/mg and Km is 15.2 μM under pH 6.0 conditions, while its Vmax is 17.6 pmol/min/mg and Km is 14.3 μM under pH 7.4 conditions[1].
Diclofenac acyl glucuronide (100-1000 μM; 3-12 h) exhibits higher cytotoxicity against HEK-OATP2B1 cells than diclofenac (HY-15036)[1].
Diclofenac acyl glucuronide (100-1000 μM; 1-3 h) induces time-dependent reactive oxygen species production in HEK-OATP2B1 cells, increasing reactive oxygen species levels by 5.5-fold after 3 h of treatment at 1000 μM and by 1.8-fold after 3 h of treatment at 500 μM[1].
Diclofenac acyl glucuronide (50-1000 μM; 30 min) dose-dependently inhibits the activity of copper/zinc superoxide dismutase. After incubation at room temperature for 30 minutes, the inhibition rate reaches 27% at 250 μM and 100% at 1000 μM[1].
Diclofenac acyl glucuronide (2 min) inhibits purified COX-1 and COX-2 enzymes. After incubation at 37℃ for 2 minutes, its IC50 against COX-1 is 0.620 μM, and that against COX-2 is 2.91 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK-OATP2B1
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Concentration:100-1000 μM
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Incubation Time:3-12 h
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Result:Induced greater cytotoxicity than diclofenac.
Caused approximately 61% cell death at 1000 μM after 3 hours.
Increased to 85% cell death at 1000 μM by 12 hours.
Showed a >2-fold increase in EthD-1 fluorescence for 1000 μM at 12 hours compared to vehicle controls.
Diclofenac acyl glucuronide (bile containing Diclofenac acyl glucuronide; molar amount equivalent to 4 mg/kg diclofenac; p.o.; single dose) significantly exacerbates small intestinal ulcers in Wistar rats and TR2 rats compared to equimolar free diclofenac, with the total ulcer length significantly increased in both strains[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CRL:(Wi)BR Wistar (female, 10-12 weeks of age); TR2 (female, 10-12 weeks of age, derived from Wistar)[2]
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Dosage:Part of 4 mg/kg total dose (free diclofenac plus diclofenac acyl glucuronide)
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Administration:p.o.; single dose
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Result:Increased total ulcer length significantly compared to control rats receiving equimolar free diclofenac in Wistar rats.
Caused development of large ulcers and shifted lesions to more proximal intestinal areas (relative location 0.52-0.90) in Wistar rats.
Increased total ulcer length significantly compared to controls in TR2 rats.
Induced development of large ulcers not seen with free diclofenac (even at 8 mg/kg) and shifted lesions to more proximal intestinal areas (relative location 0.52-0.90) in TR2 rats.
Chemical Information
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CAS No. 64118-81-6
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Appearance Solid
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Masse moléculaire 472.27
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Formule C20H19Cl2NO8
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Color White to off-white
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SMILES
O[C@H]1[C@H](OC(CC2=CC=CC=C2NC3=C(Cl)C=CC=C3Cl)=O)O[C@H](C(O)=O)[C@@H](O)[C@@H]1O
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Synonyms
D-1-O-G
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Pureté et documentation
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Fiche technique (277 KB)
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SDS (420 KB)
- English - EN (420 KB)
- Français - FR (420 KB)
- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Korean - KR (420 KB)
- Portuguese - PT (420 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Scialis RJ, et al. Elucidation of the Mechanisms through Which the Reactive Metabolite Diclofenac Acyl Glucuronide Can Mediate Toxicity. J Pharmacol Exp Ther. 2016;357(1):167-176. [Content Brief]
[2]. Seitz S, et al. Diclofenac acyl glucuronide, a major biliary metabolite, is directly involved in small intestinal injury in rats. Gastroenterology. 1998;115(6):1476-1482. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Diclofenac acyl glucuronide Related Classifications
HY-126848 Related Classifications
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