| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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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 |
Purity: ≥98%
| Targets |
Diclofensine HCl targets the dopamine transporter (DAT), noradrenaline transporter (NAT), and serotonin transporter (SERT). IC50 values for inhibition of uptake into rat brain synaptosomes: DA = 0.74 nM, NA = 2.3 nM, 5-HT = 3.7 nM [1].
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| ln Vitro |
Diclofensine HCl potently inhibited the synaptosomal uptake of [3H]dopamine (DA), [3H]noradrenaline (NA), and [3H]serotonin (5-HT) in rat brain. IC50 values were 0.74 nM for DA (striatal synaptosomes), 2.3 nM for NA (frontotemporal cortex synaptosomes), and 3.7 nM for 5-HT (whole brain minus cerebellum, pons, and medulla oblongata synaptosomes) [1].
In receptor binding assays, Diclofensine showed weak or no affinity for dopamine D-2 receptors, α1-adrenoceptors, α2-adrenoceptors, histamine receptors, and 5-HT2 receptors. IC50 values (μM) were: >13,000 for α1, >13,000 for α2, 10,000 for histamine, 11,000 for 5-HT2, and 6,500 for muscarinic receptors (acetylcholine) in isolated organ studies [1]. |
| ln Vivo |
Diclofensine HCl had an effect only in the 6-hydroxydopamine (6-OHDA) circling model in unilaterally lesioned rats, but no specific in vivo data on depletion reversal were presented in this paper. In the 6-OHDA-induced depletion model in mouse brain, no quantitative data were provided for diclofensine [1].
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| Cell Assay |
Synaptosomal uptake inhibition assay: Rat brain synaptosomes were prepared from corpus striatum (DA), frontotemporal cortex (NA), or whole brain minus cerebellum, pons, and medulla oblongata (5-HT). Synaptosomes were incubated with [3H]amine (final concentration: 10 nM for DA, 10 nM for NA, 10 nM for 5-HT) and various concentrations of Diclofensine for 30 min at 37°C, then filtered. Unspecific binding was determined in the presence of 100 μM benzotriene (DA), 10 μM citalopram (5-HT), or 10 μM talsupram (NA). IC50 values were calculated from concentration-response curves [1].
Receptor binding assays: Tissues were homogenized and centrifuged. For D-2, α1, 5-HT2, and muscarinic binding, specific radioligands ([3H]spiroperidol, [3H]prazosin, [3H]spiroperidol with sulpiride, [3H]PrBCM) were used. Incubation conditions varied (see Table 1). Bound radioactivity was measured by filtration. Diclofensine was tested at multiple concentrations [1]. Functional organ assays: Isolated guinea pig ileum (muscarinic, histaminergic, α2-adrenergic), rabbit pulmonary artery (α1-adrenergic), and rat fundus (5-HT2) were used to measure antagonist activity against agonist-induced contractions. IC50 values were determined [1]. |
| References | |
| Additional Infomation |
Diclofensine HCl (Ro 8-4650) is a potent and equipotent inhibitor of DA, NA, and 5-HT uptake. It was developed by Hoffmann‑La Roche. In this study, it was used as a comparator to the novel compound Lu 19-005. Diclofensine showed weak receptor binding affinities, indicating selectivity for monoamine transporters over neurotransmitter receptors. Its profile resembles that of Lu 19-005 but with slightly lower potency [1].
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| Molecular Formula |
C17H17NOCL2.HCL
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|---|---|
| Molecular Weight |
358.68992
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| Exact Mass |
357.045
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| CAS # |
34041-84-4
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| Related CAS # |
Diclofensine;67165-56-4
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| PubChem CID |
157489
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| Appearance |
White to off-white solid powder
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| LogP |
5.319
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
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| Complexity |
354
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1CC2=C(C=CC(OC)=C2)C(C3=CC=C(Cl)C(Cl)=C3)C1.[H]Cl
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| InChi Key |
PEHOXCSPLOXNOK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H17Cl2NO.ClH/c1-20-9-12-7-13(21-2)4-5-14(12)15(10-20)11-3-6-16(18)17(19)8-11;/h3-8,15H,9-10H2,1-2H3;1H
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| Chemical Name |
4-(3,4-dichlorophenyl)-7-methoxy-2-methyl-3,4-dihydro-1H-isoquinoline;hydrochloride
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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, avoid exposure to moisture. |
| 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) |
H2O : ≥ 52 mg/mL (~144.97 mM)
DMSO : ~6.67 mg/mL (~18.60 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.67 mg/mL (1.87 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 6.7 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 | 2.7879 mL | 13.9396 mL | 27.8792 mL | |
| 5 mM | 0.5576 mL | 2.7879 mL | 5.5758 mL | |
| 10 mM | 0.2788 mL | 1.3940 mL | 2.7879 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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