Amitifadine hydrochloride (Synonyms: DOV-21947 hydrochloride; EB-1010 hydrochloride)

Cat. No.: HY-18332A Purity: 99.86%: FAQs
Data Sheet SDS COA Handling Instructions

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Amitifadine hydrochloride is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI), with IC₅₀s of 12, 23, 96 nM for serotonin, norepinephrine and dopamine in HEK 293 cells , respectively.

For research use only. We do not sell to patients.

Amitifadine hydrochloride Chemical Structure

CAS No. : 410074-74-7

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 320	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 320	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 290	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 490	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1090	In-stock	Estimated Time of Arrival: December 31
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Other Forms of Amitifadine hydrochloride:

DOV-216,303 Free Base In-stock

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

IC50: 12 nM (serotonin), 23 nM (norepinephrine), 96 nM (dopamine)^[1].

In Vitro

Amitifadine (DOV 21,947) is an antidepressant drug. K_i values for SERT, NET, and DAT are 99 nM, 262 nM, and 213 nM. The IC₅₀ values for serotonin, norepinephrine and dopamine uptake are 12, 23 and 96 nM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The 30 mg/kg Amitifadine dose significantly reduces nicotine self-administration. The 5 and 10 mg/kg doses reduce nicotine self-administration during the first 15 min. of the session when the greatest amount of nicotine is self-administered. The 30 mg/kg Amitifadine dose, but not the lower doses cause a significant reduction in locomotor activity averaged over the 1-hour session and reduce food motivated responding. The 10 mg/kg dose causes hypoactivity at the beginning of the session, but 5 mg/kg does not cause any hypoactivity. The effect of chronic Amitifadine treatment (10 mg/kg) over the course of 15 sessions is also determined. Amitifadine causes a significant reduction in nicotine self-administration, which is not seen to diminish over two consecutive weeks of treatment and a week after enforced abstinence. Amitifadine significantly reduces nicotine self-administration. This prompts further research to determine if Amitifadine might be an effective treatment for smoking cessation^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

264.58

Formula

C₁₁H₁₂Cl₃N

CAS No.

410074-74-7

Appearance

Solid

Color

White to off-white

SMILES

ClC(C=C1[C@]2(CNC3)[C@@H]3C2)=C(C=C1)Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (377.96 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 50 mg/mL (188.98 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.7796 mL	18.8979 mL	37.7958 mL
5 mM	0.7559 mL	3.7796 mL	7.5592 mL
10 mM	0.3780 mL	1.8898 mL	3.7796 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

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: ≥ 2.75 mg/mL (10.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.75 mg/mL (10.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.75 mg/mL (10.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 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 (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 10 mg/mL (37.80 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

Purity & Documentation

Purity: 99.86%

Select Batch:

Data Sheet (272 KB) SDS (252 KB)

COA (248 KB) LCMS (258 KB)

Handling Instructions (2659 KB)

References

[1]. Skolnick P1, et al. Antidepressant-like actions of DOV 21,947: a "triple" reuptake inhibitor. Eur J Pharmacol. 2003 Feb 14;461(2-3):99-104. [Content Brief]

[2]. Levin ED, et al. Amitifadine, a triple monoamine re-uptake inhibitor, reduces nicotine self-administration in female rats. Eur J Pharmacol. 2015 Jun 20;764:30-37. [Content Brief]

Complete Stock Solution Preparation Table

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

H₂O / DMSO	1 mM	3.7796 mL	18.8979 mL	37.7958 mL	94.4894 mL
	5 mM	0.7559 mL	3.7796 mL	7.5592 mL	18.8979 mL
	10 mM	0.3780 mL	1.8898 mL	3.7796 mL	9.4489 mL
	15 mM	0.2520 mL	1.2599 mL	2.5197 mL	6.2993 mL
	20 mM	0.1890 mL	0.9449 mL	1.8898 mL	4.7245 mL
	25 mM	0.1512 mL	0.7559 mL	1.5118 mL	3.7796 mL
	30 mM	0.1260 mL	0.6299 mL	1.2599 mL	3.1496 mL
	40 mM	0.0945 mL	0.4724 mL	0.9449 mL	2.3622 mL
	50 mM	0.0756 mL	0.3780 mL	0.7559 mL	1.8898 mL
	60 mM	0.0630 mL	0.3150 mL	0.6299 mL	1.5748 mL
	80 mM	0.0472 mL	0.2362 mL	0.4724 mL	1.1811 mL
	100 mM	0.0378 mL	0.1890 mL	0.3780 mL	0.9449 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Amitifadine hydrochloride Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Amitifadine410074-74-7DOV-21947EB-1010DOV21947DOV 21947EB1010EB 1010Serotonin TransporterDopamine Transporter5-HTTSERTSLC6A4DATSLC6A3Inhibitorinhibitorinhibit

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