| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
Seco Rapamycin's Disposition in Caco-2 Cell Monolayers and Human Tissue Homogenates. Human liver, jejunal mucosal, and Caco-2 homogenates are treated with 20μM Seco Rapamycin to see if it can be converted to dihydro Sirolimus(M2). These homogenates all generated M2 in a way that was dependent on NADPH. Even at 100μM concentration, ketoconazole has no effect on M2 production in any of the homogenates tested. 20μM Seco Rapamycin is applied to Caco-2 cell monolayers to test if Seco Rapamycin may be converted to M2 in intact cells. After four hours, very little Seco Rapamycin is found in the cellular fraction and the basolateral compartment following application to the apical compartment. Furthermore, not much M2 is found. After an apical dosage, LY335979 has minimal effect on the distribution of Seco Rapamycin, even if M2 is now detectable in the apical compartment. LY335679 reduces the flux of Seco Rapamycin to the apical compartment and increases the amount of M2 in both the apical and basolateral compartments[1]. In contrast, when Seco Rapamycin is applied to the basolateral compartment, both Seco Rapamycin and M2 are easily detected in the apical compartment.
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| References |
| Molecular Formula |
C53H83NO13
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| Appearance |
Light yellow to yellow ointment
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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) |
DMSO :~100 mg/mL (~106.13 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (5.31 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 5 mg/mL (5.31 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (5.31 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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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