2. Membrane Transporter/Ion Channel
  3. Monoamine Transporter
  4. GZ-793A

GZ-793A is an orally active and selective vesicular monoamine transporter-2 (VMAT2) inhibitor, with an Ki of 0.029 µM. GZ-793A inhibits the neurochemical effects of methamphetamine (METH)-induced dopamine release. GZ-793A can be used for research of METH addiction.

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GZ-793A Chemical Structure

GZ-793A Chemical Structure

CAS No. : 1356447-90-9

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5 mg USD 350 In-stock
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Description

GZ-793A is an orally active and selective vesicular monoamine transporter-2 (VMAT2) inhibitor, with an Ki of 0.029 µM. GZ-793A inhibits the neurochemical effects of methamphetamine (METH)-induced dopamine release. GZ-793A can be used for research of METH addiction[1][2][3].

IC50 & Target

Ki: 0.029 µM (VMAT2)[1].
In Vivo

GZ-793A (30, 60, 120 or 240 mg/kg; p.o.; once) decreases the number of METH infusions self-administered across each time interval evaluats in a dose-dependent manner[1].
GZ-793A (1-100 µM; 90 min) inhibits METH (5 µM)-evoked fractional dopamine releases[2].

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

Animal Model: Adult male Sprague-Dawley rats[1].
Dosage: 30, 60, 120 or 240 mg/kg
Administration: Oral administration; once.
Result: Decreased the number of METH infusions self-administered in a dose-dependent manner, and with an ~85% reduction at the highest dose (240 mg/kg).
Decreased the METH self-administration produced by lasted at least 180 min.
Animal Model: Male Sprague-Dawley rats (250–275 g; 9-week-old; 0.5 mm thick rats coronal striatal slices are used)[2].
Dosage: 1-100 µM
Administration: 90 min
Result: Inhibited methamphetamine-evoked dopamine released in a concentration-dependent manner.
Molecular Weight

464.04

Formula

C26H38ClNO4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC[C@H](O)CN1[C@H](CCC[C@H]1CCC2=CC=C(C=C2)OC)CCC3=CC=C(C=C3)OC.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: 

H2O : 3 mg/mL (6.46 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1550 mL 10.7749 mL 21.5499 mL
5 mM 0.4310 mL 2.1550 mL 4.3100 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.

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  • Dilution Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working 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).
Purity & Documentation

Purity: 99.50%

COA (250 KB) LCMS (88 KB)

Handling Instructions (2659 KB)
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 2.1550 mL 10.7749 mL 21.5499 mL 53.8747 mL
5 mM 0.4310 mL 2.1550 mL 4.3100 mL 10.7749 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.

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  • 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:

GZ-793A1356447-90-9Monoamine TransporterMETHdopamineCPPaddictionInhibitorinhibitorinhibit

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