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Terfenadine (BRN5857899; Seldane; Terfen) is a novel and potent antihistamine drug used to treat allergies. With an IC50 of 204 nM, it is also an open-channel blocker of hERG.
Targets |
Caspase-4; Caspase-2; Caspase-9; Ca2+ homeostasis; H1 histamine receptor
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ln Vitro |
Terfenadine ((±)-Terfenadine) (4-20 μM; 24 hours) causes A375 melanoma cells to undergo dose- and time-dependent apoptosis. After 24 hours of TEF treatment in complete medium, the IC50 for A375 cells, Hs294T cells, and HT144 cells was 10.4, 9.9, and 9.6, respectively[2].Terfenadine (2–10 μM; 8 h) causes dose-dependent cytotoxicity[2].
Terfenadine (10 M; 8 hours) significantly increases the number of autophagic vacuoles in the cytoplasm of cells with double and multiple membranes. Inducing autophagy with terfenadine involves both ROS-dependent and -independent mechanisms[2].
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ln Vivo |
In chemo-resistant NSCLC xenograft models, terfenadine (p.o.; 40 mg/kg; for 16 days) significantly slows the rate at which tumors grow while also enhancing the anti-cancer effect of EPI[3].
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References |
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Molecular Formula |
C32H41NO2
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Molecular Weight |
471.685
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Exact Mass |
471.3137
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Elemental Analysis |
C, 81.48; H, 8.76; N, 2.97; O, 6.78
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CAS # |
50679-08-8
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Related CAS # |
50679-08-8
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Appearance |
Solid powder
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SMILES |
CC(C)(C)C1=CC=C(C=C1)C(CCCN2CCC(CC2)C(C3=CC=CC=C3)(C4=CC=CC=C4)O)O
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InChi Key |
GUGOEEXESWIERI-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C32H41NO2/c1-31(2,3)26-18-16-25(17-19-26)30(34)15-10-22-33-23-20-29(21-24-33)32(35,27-11-6-4-7-12-27)28-13-8-5-9-14-28/h4-9,11-14,16-19,29-30,34-35H,10,15,20-24H2,1-3H3
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Chemical Name |
1-(4-tert-butylphenyl)-4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]butan-1-ol
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Synonyms |
BRN 5857899; BRN-5857899; BRN5857899; Terfen; Seldane; Terfenadine
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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) |
DMSO: ~94 mg/mL (199.3 mM)
Ethanol: ~27 mg/mL (~57.2 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: ≥ 2.5 mg/mL (5.30 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: ≥ 2.5 mg/mL (5.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1200 mL | 10.6002 mL | 21.2004 mL | |
5 mM | 0.4240 mL | 2.1200 mL | 4.2401 mL | |
10 mM | 0.2120 mL | 1.0600 mL | 2.1200 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.