| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vivo |
In mice, the main transporter responsible for bile excretion of choyllysine fluorescein sodium (100-200 nM; intravenous injection) is Abcc2[1]. In healthy Wistar rats with bile fistula, choyllysine fluorescein sodium (0.21 μM; intravenous injection; single dose) achieved a cumulative bile excretion rate of 94.4% within 20 minutes[2].
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|---|---|
| Animal Protocol |
Animal/Disease Models: FVB wild-type, Abcc2(-/-), Abcc3(-/-) (male) [1]
Doses: 200 nM (plasma clearance, intestinal absorption study); 100 nM (bile secretion study) Route of Administration: Intravenous injection Experimental Results: Compared with wild-type mice, the clearance rate of Abcc2(-/-) mice was significantly reduced, while the clearance rate of Abcc3(-/-) mice was not reduced. In wild-type mice, about 70% of the dose was excreted in bile within 20 minutes, while in Abcc2(-/-) mice, the bile excretion was less than 2%. 120 minutes after administration, the cumulative bile excretion of Abcc2(-/-) mice reached 85% of the administered dose, while that of Abcc2(-/-) mice was only 32%. 120 minutes post-administration, the liver retention in Abcc2(-/-) mice was 64% of the administered dose, compared to only 1% in wild-type mice. At the same time, the plasma concentration in Abcc2(-/-) mice reached 1306 nM, while that in wild-type mice was 83 nM. There was no difference in bile excretion between Abcc3(-/-) and wild-type mice. After 4.5 hours, the recovery rate of the ileally administered dose in bile was only 2%, while the recovery rate of concurrently administered sodium taurocholate was 68%. Animal/Disease Models:Wistar (male, 250 g) [2] Doses: 0.21 μM Route of Administration: Intravenous injection; single dose Experimental Results: The 50% retention time (time required for half the dose to be excreted into bile) was 6.5 minutes. Within the first 10 minutes, 71.1% of the administered dose was excreted into bile. Within 20 minutes, the cumulative bile excretion rate reached 94.4%. Thin-layer chromatography confirmed complete excretion of the drug into bile. |
| References |
| Molecular Formula |
C51H61N3NA2O12
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|---|---|
| Molecular Weight |
954.02
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| Appearance |
Typically exists as solids at room temperature
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| 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]
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0482 mL | 5.2410 mL | 10.4820 mL | |
| 5 mM | 0.2096 mL | 1.0482 mL | 2.0964 mL | |
| 10 mM | 0.1048 mL | 0.5241 mL | 1.0482 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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