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  4. Cholyl-Lys-fluorescein sodium

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.

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Cholyl-Lys-fluorescein sodium

Cholyl-Lys-fluorescein sodium Chemical Structure

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Description

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[1][2].

In Vivo

The major transporter responsible for the biliary excretion of cholyl-Lys-fluorescein sodium (100-200 nM; intravenous injection) in mice is Abcc2[1].
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.

Animal Model: FVB wild-type, Abcc2(-/-), Abcc3(-/-) (male)[1]
Dosage: 200 nM (plasma clearance, intestinal uptake studies); 100 nM (biliary secretion studies)
Administration: i.v.
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.
Animal Model: Wistar (male, 250 g)[2]
Dosage: 0.21 μM
Administration: i.v.; single dose
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.
Molecular Weight

954.02

Formula

C51H61N3Na2O12
SMILES

O=C(C1=CC(NC(NCCCC[C@@H](C(O[Na])=O)NC(CC[C@H]([C@]2([H])[C@@]3([C@@]([C@@]4([H])[C@]([C@@]5([C@](C[C@@H](CC5)O)([H])C[C@H]4O)C)([H])C[C@@H]3O)([H])CC2)C)C)=O)=O)=CC=C1C(C6=CC(O)=CC=C6O7)=C(C=C8)C7=CC8=O)O[Na]
Structure Classification
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
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  • Do most proteins show cross-species activity?

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Keywords:

Cholyl-Lys-fluoresceinFluorescent Dyebile acid analogliver function assessment agentbile salt transport probeliver-targeted carrierInhibitorinhibitorinhibit

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