| Size | Price | |
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| 500mg | ||
| 1g | ||
| Other Sizes |
Fluphenazine Decanoate Dihydrochloride is a novel and potent antipsychotic agent acting as a dopamine D2 receptor inhibitor. It is a long-acting phenothiazine neuroleptic used for schizophrenia.
| ln Vitro |
In human fibroblast cell cultures, fluphenazine decanoate dihydrochloride exhibits activity against T. gondii with an IC50 value of 1.7 mM[1].
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|---|---|
| ln Vivo |
As an antipsychotic, fluphenazine decanoate dihydrochloride (0.22 mg/kg and then 0.33 mg/kg; im; 8 times every 3 weeks) enhances dopamine sensitivity in a monkey model after prolonged treatment[2]. A pharmaceutical model of human tardive dyskinesia, fluphenazine decanoate dihydrochloride (25 mg/ kg; im; 6 times every 3 weeks; 24 weeks) causes mouth movements in rats[3]. In adult male rats, fluphenazine decanoate dihydrochloride (1, 2, 3 mg/kg/d; sc; 60 d) reduces fertility and simultaneously suppresses gonadotropin levels by causing hyperprolactinemia[4].
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| Animal Protocol |
Animal/Disease Models: Cebus apella monkey[2]
Doses: 0.22 mg/kg and followed by 0.33 mg/kg Route of Administration: intramuscular (im) injection; 8 times per 3 weeks; 0.22 mg/kg for 63 weeks and 0.33 mg/kg for 6 weeks Experimental Results: diminished the aggressiveness composite behavioral variables (CBV). Resulted stereotypic behavior induced by agonist and diminished prolactin response to AMPH. Animal/Disease Models: Male Sprague- Dawley rats (250 g)[3] Doses: 25 mg/kg Route of Administration: intramuscular (im) injection into the hind limb; 24 weeks Experimental Results: Resulted in spontaneous vacuous chewing mouth movements and jaw tremor. Animal/Disease Models: Adult male rats[4] Doses: 1, 2, 3 mg/kg/d Route of Administration: subcutaneous (sc) injection between 10:00-12:00 h; 60 days Experimental Results: Increased serum prolactin level and suppressed serum LH and FSH levels at day 60. Increased hypothalamic tyrosine hydroxylase levels, enhanced chromatin decondensation, and resulted DNA denaturation. |
| References |
[1]. Goodwin DG, et al. Evaluation of five antischizophrenic agents against Toxoplasma gondii in human cell cultures. J Parasitol. 2011 Feb;97(1):148-51.
[2]. Lifshitz K, et al. Effects of dopamine agonists on Cebus apella monkeys with previous long-term exposure to fluphenazine. Biol Psychiatry. 1997 Mar 15;41(6):657-67. [3]. Stoessl AJ, et al. Chronic neuroleptic-induced mouth movements in the rat: suppression by CCK and selective dopamine D1 and D2 receptor antagonists. Psychopharmacology (Berl). 1989;98(3):372-9. [4]. Gill-Sharma MK, et al. Antifertility effects of fluphenazine in adult male rats. J Endocrinol Invest. 2003 Apr;26(4):316-26. |
| Molecular Formula |
C32H44N3O2F3S.2[HCL]
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|---|---|
| Molecular Weight |
664.69274
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| Exact Mass |
663.263
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| CAS # |
2376-65-0
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| Related CAS # |
Fluphenazine decanoate;5002-47-1
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| PubChem CID |
24745024
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
43
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| Complexity |
765
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.Cl.CCCCCCCCCC(OCCN1CCN(CCCN2C3=CC=CC=C3SC3C=CC(=CC2=3)C(F)(F)F)CC1)=O
|
| InChi Key |
IJIYWOFSPALWMA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H44F3N3O2S.2ClH/c1-2-3-4-5-6-7-8-14-31(39)40-24-23-37-21-19-36(20-22-37)17-11-18-38-27-12-9-10-13-29(27)41-30-16-15-26(25-28(30)38)32(33,34)35;;/h9-10,12-13,15-16,25H,2-8,11,14,17-24H2,1H3;2*1H
|
| Chemical Name |
2-[4-[3-[2-(trifluoromethyl)phenothiazin-10-yl]propyl]piperazin-1-yl]ethyl decanoate;dihydrochloride
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5045 mL | 7.5223 mL | 15.0446 mL | |
| 5 mM | 0.3009 mL | 1.5045 mL | 3.0089 mL | |
| 10 mM | 0.1504 mL | 0.7522 mL | 1.5045 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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