| Size | Price | Stock | Qty |
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| 250mg |
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Purity: ≥98%
Ketanserin (R41468; Vulketan; KJK-945; R-41468), an aprroved antihypertensive drug, is a potent and specific 5-HT2A serotonin receptor antagonist with a Ki of 2.5 nM for rat and human 5-HT2A. Additionally, it can be applied to distinguish between 5-HT1D and 5-HT1B receptor subtypes. When postjunctional alpha adrenergic activation occurs, ketanserin prevents the contraction of the canine saphenous vein and the rat caudal artery.
| Targets |
5-HT2A ( Ki = 2.5 nM ); 5-HT2C (Rat) ( Ki = 50 nM ); 5-HT2C (Human) ( Ki = 100 nM )
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| Cell Assay |
The HEK 293 cell line, which has been established to express hERG channels consistently, is cultivated in Dulbecco's modified Eagle's medium (DMEM) that has been enhanced with 10% foetal bovine serum and 400 μg/mL G418. The HEK 293 cell line is cultured in DMEM supplemented with 10% foetal bovine serum and 100 μg/mL hygromycin, which is responsible for the stable expression of recombinant human cardiac KCNQ1/KCNE1 channel current (IKs). On a glass coverslip, cells are seeded for electrophysiology. HEK 293 cells are used to create the mutant hERG channels, which are then temporarily expressed using 10 μL of Lipofectamine 2000 in combination with 4 μg of hERG mutant cDNA in pCDNA3 vector.
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| References |
| Molecular Formula |
C22H22FN3O3
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| Molecular Weight |
395.43
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| Exact Mass |
395.16
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| Elemental Analysis |
C, 66.82; H, 5.61; F, 4.80; N, 10.63; O, 12.14
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| CAS # |
74050-98-9
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| Related CAS # |
Ketanserin tartrate; 83846-83-7
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| Appearance |
Solid powder
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| SMILES |
C1CN(CCC1C(=O)C2=CC=C(C=C2)F)CCN3C(=O)C4=CC=CC=C4NC3=O
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| InChi Key |
FPCCSQOGAWCVBH-UHFFFAOYSA-
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| InChi Code |
InChI=1S/C22H22FN3O3/c23-17-7-5-15(6-8-17)20(27)16-9-11-25(12-10-16)13-14-26-21(28)18-3-1-2-4-19(18)24-22(26)29/h1-8,16H,9-14H2,(H,24,29)
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| Chemical Name |
3-[2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl]-1H-quinazoline-2,4-dione
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (4.22 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 16.7 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: ≥ 1.67 mg/mL (4.22 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 16.7 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: ≥ 1.67 mg/mL (4.22 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 0.5 mg/mL (1.26 mM) (saturation unknown) in 10% DMF 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: 4%DMSO + 40%PEG300 + 4%Tween 80 + 52%ddH2O: 1.0mg/ml (2.53mM) Solubility in Formulation 6: 6.25 mg/mL (15.81 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5289 mL | 12.6445 mL | 25.2889 mL | |
| 5 mM | 0.5058 mL | 2.5289 mL | 5.0578 mL | |
| 10 mM | 0.2529 mL | 1.2644 mL | 2.5289 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03289949 | Recruiting | Drug: Psilocybine Drug: Ketanserin |
Basic Science | Gitte Moos Knudsen | March 3, 2017 | Phase 1 |
| NCT05964647 | Recruiting | Drug: LSD (150 µg) + placebo Drug: Placebo + placebo |
Healthy | University Hospital, Basel, Switzerland |
January 15, 2024 | Phase 1 |
| NCT04558294 | Completed | Drug: Ketanserin Placebo Drug: Ketanserin |
Healthy | University Hospital, Basel, Switzerland |
October 16, 2020 | Phase 1 |
| NCT02632877 | Completed | Drug: Pirfenidone with MODD Drug: Ketanserin |
Diabetic Foot Ulcer | University of Guadalajara | January 2014 | Phase 1 Phase 2 |
| NCT01329887 | Completed | Drug: ketanserin Septic Shock |
Medical Centre Leeuwarden | Severe Sepsis Septic Shock |
March 2011 | Phase 3 |
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