| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| ln Vivo |
At postsynaptic 5-HT1A receptors, flesinoxan functions as a partial agonist; at presynaptic 5-HT1A receptors, it functions as a full agonist. The way that 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT) counteracts the effects of 5-HT on CA3 pyramidal neurons is comparable to that of blesinoxan [1]. Flesinoxan administered intravenously suppresses the firing activity of dorsal raphe 5-HT neurons and CA3 pyramidal neurons. It was established how permeable the brain is to [3H]Flesinoxan and [3H]8-OH-DPAT. Brain concentrations of [3H]8-OH-DPAT were substantially greater than [3H]Flesinoxan nine minutes after intravenous injection[1]. The administration of Flesinoxan with 8-OH-DPAT subcutaneously induces hypothermia based on the dose. The hypothermia caused by Flesinoxan was considerably reduced by preadministration of the nonselective 5-HT1A antagonist pindolol and the 5-HT1/2 antagonist methysergide. 0.5 mg/kg of 8-OH-DPAT and 3 mg/kg of Flesinoxan produced hypothermia to comparable degrees. Compared to 8-OH-DPAT, the maximal effect of Flesinoxan happens 30 minutes later and dissipates more slowly [1].
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| References |
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| Molecular Formula |
C22H26FN3O
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|---|---|
| Molecular Weight |
415.4654
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| Exact Mass |
415.191
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| CAS # |
98206-10-1
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| Related CAS # |
98205-89-1 (HCl);98206-10-1;
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| PubChem CID |
57347
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.271g/cm3
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| Boiling Point |
635.8ºC at 760mmHg
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| Flash Point |
338.3ºC
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| Index of Refraction |
1.585
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| LogP |
1.903
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
30
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| Complexity |
553
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1CN(CCN1CCNC(=O)C2=CC=C(C=C2)F)C3=C4C(=CC=C3)O[C@H](CO4)CO
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| InChi Key |
NYSDRDDQELAVKP-SFHVURJKSA-N
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| InChi Code |
InChI=1S/C22H26FN3O4/c23-17-6-4-16(5-7-17)22(28)24-8-9-25-10-12-26(13-11-25)19-2-1-3-20-21(19)29-15-18(14-27)30-20/h1-7,18,27H,8-15H2,(H,24,28)/t18-/m0/s1
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| Chemical Name |
4-fluoro-N-[2-[4-[(2S)-2-(hydroxymethyl)-2,3-dihydro-1,4-benzodioxin-5-yl]piperazin-1-yl]ethyl]benzamide
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| Synonyms |
DU29373; DU-29373; Flesinoxan
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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 : ~31.25 mg/mL (~75.22 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.01 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 20.8 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: ≥ 2.08 mg/mL (5.01 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 20.8 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 | 2.4069 mL | 12.0346 mL | 24.0691 mL | |
| 5 mM | 0.4814 mL | 2.4069 mL | 4.8138 mL | |
| 10 mM | 0.2407 mL | 1.2035 mL | 2.4069 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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