Cholyl-Lys-fluorescein disodium
Cholyl-Lys-fluorescein sodium is a fluorescein-labeled bile acid analog. Cholyl-Lys-fluorescein sodium mimics the physiological hepatobiliary properties of glycocholic acid. Cholyl-Lys-fluorescein sodium is efficiently taken up by the liver and rapidly excreted into bile in intact form in rats. Cholyl-Lys-fluorescein sodium can serve as a liver function assessment agent, bile salt transport probe, and liver-targeted carrier.
For research use only. We do not sell to patients.
- CAS No.: 397841-89-3
- Formula: C51H62N3Na2O11S
- Molecular Weight:971.10
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Cholyl-Lys-fluorescein (0.21 μM; intravenous injection; single dose) sodium achieves a cumulative biliary excretion rate of 94.4% within 20 minutes in healthy biliary fistula Wistar rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:FVB wild-type, Abcc2(-/-), Abcc3(-/-) (male)[1]
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Dosage:200 nM (plasma clearance, intestinal uptake studies); 100 nM (biliary secretion studies)
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Administration:i.v.
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Result:Showed strongly impaired clearance in Abcc2(-/-) mice compared with wild-type mice, but no impairment in Abcc3(-/-) mice.
Excreted ~70% of dose into bile within 20 minutes in wild-type mice, while <2% was excreted in Abcc2(-/-) mice.
Reached cumulative biliary excretion of 85% (wild-type) versus 32% (Abcc2(-/-)) of the administered dose at 120 minutes.
Had hepatic retention of 64% (Abcc2(-/-)) versus 1% (wild-type) of the administered dose at 120 minutes.
Reached blood levels of 1306 nM (Abcc2(-/-)) versus 83 nM (wild-type) at 120 minutes.
Showed no difference in biliary output between Abcc3(-/-) and wild-type mice.
Recovered only 2% of ileally administered dose in bile at 4.5 hours, compared with 68% of co-administered taurocholate.
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Animal Model:Wistar (male, 250 g)[2]
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Dosage:0.21 μM
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Administration:i.v.; single dose
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Result:Reached 50% retention time (time for half the dose to be excreted into bile) of 6.5 minutes.
Excreted 71.1% of the administered dose in bile over the initial 10 minutes.
Achieved 94.4% cumulative biliary excretion over 20 minutes.
Confirmed intact excretion into bile via TLC analysis.
Chemical Information
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CAS No. 397841-89-3
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Molecular Weight 971.10
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Formula C51H62N3Na2O11S
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SMILES
O=C1OC2(C3=CC=C(O)C=C3OC4=CC(O)=CC=C42)C5=CC=C(NC(NCCCC[C@@H](C(O[Na])=O)NC(CC[C@H]([C@]6([H])[C@@]7([C@@]([C@@]8([H])[C@]([C@@]9([C@](C[C@@H](CC9)O)([H])C[C@H]8O)C)([H])C[C@@H]7O)([H])CC6)C)C)=O)=S)C=C51.[Na]
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Synonyms
Fluorescein lisicol disodium; NRL972 disodium
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. de Waart DR, et al. Hepatic transport mechanisms of cholyl-L-lysyl-fluorescein. J Pharmacol Exp Ther. 2010;334(1):78-86. [Content Brief]
[2]. Mills CO, et al. Cholyl-lysylfluorescein: synthesis, biliary excretion in vivo and during single-pass perfusion of isolated perfused rat liver. Biochim Biophys Acta. 1991;1115(2):151-156. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)