Size | Price | Stock | Qty |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Astemizole (formerly R-43512; Hismanal) is a novel, potent and second-generation antihistamine drug with a long duration of action and is used to diminish allergic symptomsby acting as a histamine H1-receptor antagonist (IC50 = 4 nM).
Targets |
H1 Receptor
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ln Vivo |
Astemizole (po, 10 and 30 mg/kg) and (iv, 1 and 3 mg/kg) had no effect on respiratory rate, heart rate, or blood glucose, even at the high doses of 30 mg/kg and 3 mg/kg. It also had no effect on breast cancer and exercise capacity in marmosets of average weight. However, astemizole at 30 mg/kg (po) and 1 mg/kg (iv) can prolong the QT interval and induce premature ventricular contractions [3]. Astemizole (po, 3) and 30 mg/kg) at a dose of 3 mg/kg, preperfume control values (C) for ventricular rate, QT interval, and QTcF were 31 beats/min, 319 ms, and 256, whereas these were 31 beats/min, 331 ms, and 270 respectively at a dose of 30 mg/kg in mice. In addition, astemizole at a dose of 30 mg/kg (po) may cause torsade de pointes ventricular tachycardia by inhibiting hERG K+ channels [4].
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References |
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Molecular Formula |
C28H31FN4O
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Molecular Weight |
458.57034
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Exact Mass |
458.25
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Elemental Analysis |
C, 73.34; H, 6.81; F, 4.14; N, 12.22; O, 3.49
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CAS # |
68844-77-9
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Appearance |
Solid powder
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SMILES |
COC1=CC=C(C=C1)CCN2CCC(CC2)NC3=NC4=CC=CC=C4N3CC5=CC=C(C=C5)F
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InChi Key |
GXDALQBWZGODGZ-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C28H31FN4O/c1-34-25-12-8-21(9-13-25)14-17-32-18-15-24(16-19-32)30-28-31-26-4-2-3-5-27(26)33(28)20-22-6-10-23(29)11-7-22/h2-13,24H,14-20H2,1H3,(H,30,31)
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Chemical Name |
1-[(4-fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]piperidin-4-yl]benzimidazol-2-amine
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Synonyms |
R 43512; Hismanal; R43512; Paralergin; R-43512; Astemizole; Histaminos; Laridal; Retolen
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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: ~125 mg/mL (~272.6 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (13.63 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 62.5 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: ≥ 6.25 mg/mL (13.63 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 62.5 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1807 mL | 10.9035 mL | 21.8069 mL | |
5 mM | 0.4361 mL | 2.1807 mL | 4.3614 mL | |
10 mM | 0.2181 mL | 1.0903 mL | 2.1807 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.
The time courses of the changes in the idioventricular rate (top), QT interval (middle), and QTcF and the number of surviving animals (bottom) before and after the oral administration of astemizole of 3 (left) and 30 (right) mg/kg (n = 4 for each dose). J Pharmacol Sci . 2016 Jun;131(2):150-3. td> |
Proarrhythmic effects of the oral administration of 30 kg/kg of astemizole. J Pharmacol Sci . 2016 Jun;131(2):150-3 td> |