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DOV-216,303 Free Base

Cat No.:V29724 Purity: ≥98%
DOV-216,303 (Free Base) is a potent triple inhibitor of serotonin, norepinephrine, and dopamine reuptake, with IC50s of 14 nM, 20 nM, and 78 nM for hSERT, hNET, and hDAT, respectively.
DOV-216,303 Free Base
DOV-216,303 Free Base Chemical Structure CAS No.: 66504-40-3
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
Other Sizes

Other Forms of DOV-216,303 Free Base:

  • Amitifadine HCl
  • CL-216303 HCl
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
DOV-216,303 (Free Base) is a potent triple inhibitor of serotonin, norepinephrine, and dopamine reuptake, with IC50s of 14 nM, 20 nM, and 78 nM for hSERT, hNET, and hDAT, respectively. In the olfactory bulbectomy rat model, it can increase the release of monoamines in the prefrontal cortex and have antidepressant effects.
Biological Activity I Assay Protocols (From Reference)
ln Vivo
In OBX and Sham animals, acute administration of DOV-216,303 (20 mg/kg, i.p.) dramatically raises dopamine, norepinephrine, and serotonin levels [2]. In the medial prefrontal cortex of OBX and Sham mice, chronic administration of DOV 216,303 (20 mg/kg, i.p., for 17 days) raises extracellular concentrations of dopamine, norepinephrine, and serotonin and significantly increases extracellular baseline serum concentration [2].
Animal Protocol
Animal/Disease Models: Male Sprague Dawley rats weighing 290 to 350 grams at the time of OBX or sham surgery [2].
Doses: 20 mg/kg. Management: IP one time/day for 17 days.
Experimental Results: Extracellular concentrations of dopamine, norepinephrine, and serotonin were increased in the medial prefrontal cortex of OBX and Sham animals, and extracellular baseline serotonin concentrations were Dramatically increased.

Animal/Disease Models: Male Sprague Dawley rats weighing 290 to 350 grams at the time of OBX or sham surgery [2].
Doses: 20 mg/kg. Management: IP once.
Experimental Results: Dopamine, norepinephrine, and serotonin levels were Dramatically increased in OBX and Sham animals.
References

[1]. Discovery of N-methyl-1-(1-phenylcyclohexyl)methanamine, a novel triple serotonin, norepinephrine, and dopamine reuptake inhibitor. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1438-41.

[2]. The putative antidepressant DOV 216,303, a triple reuptake inhibitor, increases monoamine release in the prefrontal cortex of olfactory bulbectomized rats. Eur J Pharmacol. 2010 May 10;633(1-3):55-61.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C11H11NCL2
Molecular Weight
228.11774
Exact Mass
227.027
CAS #
66504-40-3
Related CAS #
Amitifadine hydrochloride;410074-74-7;DOV-216,303;86215-36-3
PubChem CID
9795276
Appearance
Colorless to light yellow ointment
LogP
3.183
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
1
Rotatable Bond Count
1
Heavy Atom Count
14
Complexity
245
Defined Atom Stereocenter Count
0
SMILES
C1=CC(=C(C=C1C23CC3CNC2)Cl)Cl
InChi Key
BSMNRYCSBFHEMQ-UHFFFAOYSA-N
InChi Code
InChI=1S/C11H11Cl2N/c12-9-2-1-7(3-10(9)13)11-4-8(11)5-14-6-11/h1-3,8,14H,4-6H2
Chemical Name
1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO : ≥ 125 mg/mL (~547.96 mM)
Ethanol : ~100 mg/mL (~438.37 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (9.12 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 (9.12 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 4.3837 mL 21.9183 mL 43.8366 mL
5 mM 0.8767 mL 4.3837 mL 8.7673 mL
10 mM 0.4384 mL 2.1918 mL 4.3837 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.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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.
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