| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Vesicular monoamine transporter-2 (VMAT2).
|
|---|---|
| ln Vitro |
GZ-793A inhibits VMAT2 with a Ki value of 0.029 µM. It shows 50-fold selectivity for VMAT2 over serotonin or dopamine transporters. The compound inhibits methamphetamine-induced dopamine release and prevents dopamine uptake into synaptic vesicles. These properties make GZ-793A a valuable tool for studying the neurochemical basis of methamphetamine addiction.
|
| ln Vivo |
In a dose-dependent way, GZ-793A (30, 60, 120, or 240 mg/kg; oral; once) lowers the quantity of self-injected methamphetamine infusions each time interval [1]. The release of dopamine produced by METH (5 µM) is inhibited by GZ-793A (1-100 µM; 90 minutes) [2].
In vivo, GZ-793A is orally active and inhibits the neurochemical effects of methamphetamine-induced dopamine release. It has been investigated in animal models of methamphetamine addiction for its ability to reduce drug-seeking behavior and methamphetamine self-administration. Specific dosing regimens and detailed efficacy data are available in preclinical literature. |
| Enzyme Assay |
VMAT2 binding affinity is assessed using in vitro radioligand binding assays with membrane preparations from cells expressing recombinant VMAT2. Competitive binding with [3H]dihydrotetrabenazine is measured. Ki values are calculated from displacement curves. Selectivity over serotonin and dopamine transporters is confirmed by parallel testing.
|
| Cell Assay |
Cellular activity is evaluated in neuronal cell cultures or synaptosomes. Dopamine uptake into synaptic vesicles is measured using radiolabeled dopamine. Methamphetamine-induced dopamine release is assessed by measuring extracellular dopamine levels using HPLC or amperometry. Cells are treated with GZ-793A at various concentrations to determine inhibition potency.
|
| Animal Protocol |
Animal/Disease Models: Adult male SD (SD (Sprague-Dawley)) rat [1].
Doses: 30, 60, 120 or 240 mg/kg Route of Administration: po (po (oral gavage)) once. Experimental Results: The number of self-injections of methamphetamine was diminished in a dose-dependent manner, with a reduction of approximately 85% at the highest dose (240 mg/kg). Reduce meth self-administration that lasts for at least 180 minutes. Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (250-275 g; 9 weeks old; 0.5 mm thick rat coronal striatum sections were used) [2]. Doses: 1-100 µM Administration Time: 90 minutes Experimental Results: Inhibition of methamphetamine-induced dopamine release in a concentration-dependent manner. In vivo efficacy is studied in rodent models of methamphetamine addiction, including self-administration, conditioned place preference, and drug-seeking behavior paradigms. GZ-793A is administered orally at various doses. Methamphetamine-induced dopamine release is measured in brain regions using microdialysis. Drug-seeking behavior is quantified. |
| ADME/Pharmacokinetics |
GZ-793A has a molecular formula of C26H38ClNO4 and molecular weight of 464.04. It is orally active. The compound is typically supplied as the hydrochloride salt. Detailed pharmacokinetic parameters including half-life, oral bioavailability, and plasma protein binding are not extensively characterized in publicly available literature.
|
| Toxicity/Toxicokinetics |
Safety data for GZ-793A indicate it is a research compound for laboratory use only. Specific toxicological profiles including acute toxicity, organ toxicity, and genotoxicity are not extensively published. As a VMAT2 inhibitor, it may affect monoamine neurotransmission. Standard laboratory safety practices should be followed during handling.
|
| References |
|
| Additional Infomation |
GZ-793A is a research tool compound for studying VMAT2 function and methamphetamine addiction. It is not approved for clinical use. The compound has been developed as a potential pharmacotherapy for methamphetamine use disorder by targeting the vesicular monoamine transporter to reduce the rewarding effects of the drug.
|
| Molecular Formula |
C26H38CLNO4
|
|---|---|
| Molecular Weight |
464.04
|
| Exact Mass |
463.248
|
| CAS # |
1356447-90-9
|
| PubChem CID |
49778922
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
11
|
| Heavy Atom Count |
32
|
| Complexity |
438
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
COC1=CC=C(C=C1)CC[C@H]2CCC[C@H](N2C[C@H](CO)O)CCC3=CC=C(C=C3)OC.Cl
|
| InChi Key |
FLFFCQKGCYZDOI-SJUVJREQSA-N
|
| InChi Code |
InChI=1S/C26H37NO4.ClH/c1-30-25-14-8-20(9-15-25)6-12-22-4-3-5-23(27(22)18-24(29)19-28)13-7-21-10-16-26(31-2)17-11-21;/h8-11,14-17,22-24,28-29H,3-7,12-13,18-19H2,1-2H3;1H/t22-,23+,24-;/m1./s1
|
| Chemical Name |
(2R)-3-[(2R,6S)-2,6-bis[2-(4-methoxyphenyl)ethyl]piperidin-1-yl]propane-1,2-diol;hydrochloride
|
| Synonyms |
GZ793A; GZ 793A; GZ-793A
|
| 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 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2155 mL | 1.0775 mL | 2.1550 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
