DOV-216,303 Free Base

Name: DOV-216,303 Free Base
Brand: MedChemExpress
SKU: HY-18332C
Rating: 4.5 (0 reviews)

製品番号: HY-18332C 純度: 98.17%: Data Sheet SDS COA 取扱説明書
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DOV-216,303 (Free Base) is a potent triple serotonin, norepinephrine, and dopamine reuptake inhibitor, with IC₅₀ values of 14 nM, 20 nM and 78 nM for hSERT, hNET and hDAT, respectively. Has antidepressant-like effects and increases monoamine release in the prefrontal cortex of olfactory bulbectomized (OBX) rats.

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DOV-216,303 Free Base 構造式

CAS 番号 : 66504-40-3

容量	価格（税別）	在庫状況	数量
Oil + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 82	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 82	在庫あり	Estimated Time of Arrival: December 31
Oil
5 mg	$75	在庫あり	Estimated Time of Arrival: December 31
10 mg	$120	在庫あり	Estimated Time of Arrival: December 31
50 mg		お問い合わせ
100 mg		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 0 publication(s) in Google Scholar

Other Forms of DOV-216,303 Free Base:

Amitifadine hydrochloride 在庫あり
Amitifadine お問い合わせ
DOV-102,677 お問い合わせ
DOV-216,303 お問い合わせ

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製品説明

IC₅₀ & Target

IC50: 14 nM (serotonin), 20 nM (norepinephrine), 78 nM (dopamine)^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	78 nM Compound: DOV-216, 303	Inhibition of [3H]dopamine reuptake at human DAT expressed in CHOK1 cells by scintillation counting Inhibition of [3H]dopamine reuptake at human DAT expressed in CHOK1 cells by scintillation counting	[PMID: 21093273]
CHO-K1	IC₅₀	96 nM Compound: DOV-21, 947	Inhibition of [3H]dopamine reuptake at human DAT expressed in CHOK1 cells by scintillation counting Inhibition of [3H]dopamine reuptake at human DAT expressed in CHOK1 cells by scintillation counting	[PMID: 21093273]
HEK293	IC₅₀	12 nM Compound: DOV-21, 947	Inhibition of [3H]serotonin reuptake at human SERT expressed in HEK293 cells by scintillation counting Inhibition of [3H]serotonin reuptake at human SERT expressed in HEK293 cells by scintillation counting	[PMID: 21093273]
HEK293	IC₅₀	14 nM Compound: DOV-216, 303	Inhibition of [3H]serotonin reuptake at human SERT expressed in HEK293 cells by scintillation counting Inhibition of [3H]serotonin reuptake at human SERT expressed in HEK293 cells by scintillation counting	[PMID: 21093273]
HEK293	IC₅₀	143 nM Compound: DOV216,303	Inhibition of norepinephrine reuptake at human NET expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay Inhibition of norepinephrine reuptake at human NET expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay	[PMID: 24974340]
HEK293	IC₅₀	394 nM Compound: DOV216,303	Inhibition of DA reuptake at human DAT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay Inhibition of DA reuptake at human DAT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay	[PMID: 24974340]
HEK293	IC₅₀	723 nM Compound: DOV216,303	Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay	[PMID: 24974340]
MDCK	IC₅₀	20 nM Compound: DOV-216, 303	Inhibition of [3H]norepinephrine reuptake at human NET expressed in MDCK cells by scintillation counting Inhibition of [3H]norepinephrine reuptake at human NET expressed in MDCK cells by scintillation counting	[PMID: 21093273]
MDCK	IC₅₀	23 nM Compound: DOV-21, 947	Inhibition of [3H]norepinephrine reuptake at human NET expressed in MDCK cells by scintillation counting Inhibition of [3H]norepinephrine reuptake at human NET expressed in MDCK cells by scintillation counting	[PMID: 21093273]

体内実験

Animal Model:	Male Sprague Dawley rats weighing between 290 and 350 g at time of OBX or Sham surgery^[2].
Dosage:	20 mg/kg.
Administration:	I.P. daily for 17days.
Result:	Increased extracellular concentrations of dopamine, norepinephrine and serotonin in the medial prefrontal cortex of both OBX and Sham animals and significantly increased extracellular baseline serotonin concentrations.

Animal Model:	Male Sprague Dawley rats weighing between 290 and 350 g at time of OBX or Sham surgery^[2].
Dosage:	20 mg/kg.
Administration:	I.P. once.
Result:	Significant increases in dopamine, norepinephrine and serotonin levels were measured in both OBX and Sham animals.

分子量

228.12

分子式

C₁₁H₁₁Cl₂N

CAS 番号

66504-40-3

Appearance

Oil

Color

Colorless to light yellow

SMILES

ClC1=C(Cl)C=C(C=C1)C12CC1CNC2

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : ≥ 125 mg/mL (547.96 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 100 mg/mL (438.37 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (9.12 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (9.12 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 98.17%

Select Batch:

データシート (276 KB) SDS (393 KB)

COA (254 KB) LCMS (90 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Popik P, et al. Pharmacological profile of the "triple" monoamine neurotransmitter uptake inhibitor, DOV 102,677. Cell Mol Neurobiol. 2006 Jul-Aug;26(4-6):857-73. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

Ethanol / DMSO	1 mM	4.3837 mL	21.9183 mL	43.8366 mL	109.5914 mL
	5 mM	0.8767 mL	4.3837 mL	8.7673 mL	21.9183 mL
	10 mM	0.4384 mL	2.1918 mL	4.3837 mL	10.9591 mL
	15 mM	0.2922 mL	1.4612 mL	2.9224 mL	7.3061 mL
	20 mM	0.2192 mL	1.0959 mL	2.1918 mL	5.4796 mL
	25 mM	0.1753 mL	0.8767 mL	1.7535 mL	4.3837 mL
	30 mM	0.1461 mL	0.7306 mL	1.4612 mL	3.6530 mL
	40 mM	0.1096 mL	0.5480 mL	1.0959 mL	2.7398 mL
	50 mM	0.0877 mL	0.4384 mL	0.8767 mL	2.1918 mL
	60 mM	0.0731 mL	0.3653 mL	0.7306 mL	1.8265 mL
	80 mM	0.0548 mL	0.2740 mL	0.5480 mL	1.3699 mL
	100 mM	0.0438 mL	0.2192 mL	0.4384 mL	1.0959 mL