Size | Price | |
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500mg | ||
1g | ||
Other Sizes |
ln Vitro |
Cremophor EL exhibited time- and concentration-dependent cytotoxicity in human umbilical vein endothelial cells (HUVECs) and HeLa epithelial cells. After 1-hour exposure, viability remained >80% at 0.01–0.1 mg/mL but dropped to <20% at 1 mg/mL. After 24 hours, IC50 values were 0.025 mg/mL for HUVECs and 0.035 mg/mL for HeLa cells. Cytotoxicity was attributed to plasma membrane disruption, observed via microscopy. [1]
Cremophor EL is a common excipient. Cremophor EL at 5 mg/mL raises the impedance for the first 10 hours, then lowers it. Epithelial cell death is observed after 20 hours of treatment. More so than RH40, cremophor EL reduces cell viability and enhances cell toxicity. At doses of 10 to 50 mg/mL of Cremophor EL, both epithelial viability and monolayer integrity are significantly compromised after a 24-hour treatment. Moreover, cell dissociation is improved with cremophor EL[1]. |
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Cell Assay |
Cytotoxicity was assessed using the MTT assay. Cells were seeded in 96-well plates (5,000 cells/well) and incubated overnight. Cremophor EL was dissolved in culture medium and serially diluted. Cells were exposed for 1, 4, or 24 hours. After treatment, MTT reagent was added and incubated for 4 hours. Formazan crystals were dissolved in DMSO, and absorbance was measured at 570 nm. Viability was normalized to untreated controls. [1]
Live-cell imaging tracked morphological changes during exposure. Cells were treated with 0.05–0.5 mg/mL Cremophor EL and imaged every 5 minutes for 4 hours using phase-contrast microscopy. Membrane blebbing and lysis were documented. [1] |
Toxicity/Toxicokinetics |
Cremophor EL caused acute cytotoxicity via direct membrane damage, evidenced by rapid lactate dehydrogenase (LDH) release. LDH levels increased 3-fold within 15 minutes at 0.5 mg/mL. Cytotoxicity was partially reversible: cells washed after 1-hour exposure recovered 60–70% viability after 24 hours. No apoptosis or necrosis pathways were activated. [1]
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References | |
Additional Infomation |
Cremophor EL caused acute cytotoxicity via direct membrane damage, evidenced by rapid lactate dehydrogenase (LDH) release. LDH levels increased 3-fold within 15 minutes at 0.5 mg/mL. Cytotoxicity was partially reversible: cells washed after 1-hour exposure recovered 60–70% viability after 24 hours. No apoptosis or necrosis pathways were activated. [1]
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Molecular Formula |
C4H7CL2NO2
|
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Molecular Weight |
172.0099
|
Exact Mass |
170.985
|
CAS # |
61791-12-6
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PubChem CID |
154733643
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Appearance |
Light yellow to brow liquid
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Density |
1.4±0.1 g/cm3
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Boiling Point |
305.7±32.0 °C at 760 mmHg
|
Melting Point |
4°C
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Flash Point |
138.7±25.1 °C
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Vapour Pressure |
0.0±0.6 mmHg at 25°C
|
Index of Refraction |
1.481
|
LogP |
0.62
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Hydrogen Bond Donor Count |
3
|
Hydrogen Bond Acceptor Count |
15
|
Rotatable Bond Count |
65
|
Heavy Atom Count |
78
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Complexity |
1310
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Defined Atom Stereocenter Count |
0
|
SMILES |
ClC([H])([H])C([H])(C([H])([H])Cl)OC(N([H])[H])=O
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InChi Key |
LXZHFNATOMRESM-AAKVHIHISA-N
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InChi Code |
InChI=1S/C63H116O15/c1-4-7-10-31-40-57(64)43-34-25-19-13-16-22-28-37-46-73-61(67)76-51-49-70-55-60(72-53-54-78-63(69)75-48-39-30-24-18-15-21-27-36-45-59(66)42-33-12-9-6-3)56-71-50-52-77-62(68)74-47-38-29-23-17-14-20-26-35-44-58(65)41-32-11-8-5-2/h25-27,34-36,57-60,64-66H,4-24,28-33,37-56H2,1-3H3/b34-25-,35-26-,36-27-
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Chemical Name |
2-[1,3-bis[2-[(Z)-11-hydroxyheptadec-8-enoxy]carbonyloxyethoxy]propan-2-yloxy]ethyl [(Z)-11-hydroxyheptadec-8-enyl] carbonate
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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) |
Ethanol : ~50 mg/mL
H2O : ~25 mg/mL |
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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 | 5.8136 mL | 29.0681 mL | 58.1362 mL | |
5 mM | 1.1627 mL | 5.8136 mL | 11.6272 mL | |
10 mM | 0.5814 mL | 2.9068 mL | 5.8136 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.