| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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| ln Vitro |
Pizotifen malate (BC-105 malate) is a strong antagonist of the 5-HT2 receptor that has a high affinity for the binding region of the 5-HT1C [1]. Pizotifen is an anti-5-HT2A receptor antagonist that prevents platelet aggregation generated by ADP that is increased by serotonin [2].
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| ln Vivo |
Fetal weight was considerably lowered by all doses of pethidine and benzofen malate (BC-105 malate); placental weight was only significantly reduced at the intermediate level and only after 0.6 and 1.2 mg/kg of pethidine. It didn't drastically drop until after bentifen malate. There was no difference observed between the treated and control groups in terms of implantation, viable pregnancies, stillbirths, resorptions, and external, skeletal, and visceral abnormalities. There was no discernible difference between the treatment group's and the negative control group's number of chromosomal abnormalities in the mice's bone marrow cells. Testing for micronuclei revealed no rise in micronucleus frequency as compared to controls. Following two increased dosages of benzofen maleate and pipethiazide, the mitotic index was comparatively lower in the experimental group [3].
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| References |
[1]. Mylecharane EJ, et al. 5-HT2 receptor antagonists and migraine therapy. J Neurol. 1991;238 Suppl 1:S45-52.
[2]. Lin OA, et al. The antidepressant 5-HT2A receptor antagonists pizotifen and cyproheptadine inhibit serotonin-enhanced platelet function. PLoS One. 2014 Jan 23;9(1):e87026. [3]. Ujházy E, et al. Teratological and cytogenetical evaluation of two antihistamines (pipethiadene and pizotifen maleate) in mice. Agents Actions. 1988 Apr;23(3-4):376-8 |
| Additional Infomation |
Pizotifen malate is a malate salt resulting from the reaction of equimolar amounts of pizotifen and malic acid. A sedating antihistamine with strong serotonin antagonist and weak antimuscarinic activity, it is used for the treatment of migraine and the prevention of headache attacks during cluster periods. It has a role as a histamine antagonist, a muscarinic antagonist and a serotonergic antagonist. It contains a pizotifen(1+).
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| Molecular Formula |
C23H27NO5S
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|---|---|
| Molecular Weight |
429.5292
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| Exact Mass |
429.16
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| CAS # |
5189-11-7
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| Related CAS # |
Pizotifen;15574-96-6
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| PubChem CID |
168993
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| Appearance |
Typically exists as solid at room temperature
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| Boiling Point |
436.7ºC at 760 mmHg
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| Melting Point |
185-186° (dec)
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| Flash Point |
217.9ºC
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| LogP |
4.023
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
535
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C([H])=C([H])C2=C1C([H])([H])C([H])([H])C1=C([H])C([H])=C([H])C([H])=C1/C/2=C1\C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C\1([H])[H].O([H])C([H])(C(=O)O[H])C([H])([H])C(=O)O[H]
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| InChi Key |
IWAWCPZVTXCFKD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H21NS.C4H6O5/c1-20-11-8-15(9-12-20)19-16-5-3-2-4-14(16)6-7-18-17(19)10-13-21-18;5-2(4(8)9)1-3(6)7/h2-5,10,13H,6-9,11-12H2,1H3;2,5H,1H2,(H,6,7)(H,8,9)
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| Chemical Name |
2-hydroxybutanedioic acid;1-methyl-4-(6-thiatricyclo[8.4.0.03,7]tetradeca-1(14),3(7),4,10,12-pentaen-2-ylidene)piperidine
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~50 mg/mL (~116.41 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.82 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 (5.82 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 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 | 2.3281 mL | 11.6406 mL | 23.2813 mL | |
| 5 mM | 0.4656 mL | 2.3281 mL | 4.6563 mL | |
| 10 mM | 0.2328 mL | 1.1641 mL | 2.3281 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.
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