| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| ln Vitro |
A number of N-hydroxyguanidine analogs of Guanoxabenz as well as a number of metabolic inhibitors, such as allopurinol, 1-chloro-2,4-dinitrobenzene, 5,59-dithiobis-(2-nitrobenzoic acid), cibacron blue, phenyl-p-benzoquinone, didox, and trimidox, appear to inhibit the formation of high-affinity Guanoxabenz binding. Preincubating the membranes with the Guanoxabenz analogue LW03 N-hydroxyguanidine inhibits the production of Guanoxabenz high-affinity binding in a manner that is dependent on both time and concentration[1]. Guanoxabenz is reduced to guanabenz by the cytosolic portion of the spleen, and guanabenz has an almost 100-fold greater affinity for rat alpha2A-adrenoceptors than does guanoxabenz[2].
|
|---|---|
| ln Vivo |
The names "guanoxabenz" and "guanabenz" refer to centrally acting antihypertensive medications. Rat brain membranes exhibit high affinity Guanoxabenz binding upon the presence of NADPH or NADH cofactors. A metabolite with a strong affinity for alpha 2-adrenoceptors can be formed by activating Guanoxabenz through an enzymatic activity seen in the cerebral cortex of rats[3]. A dose of 1 mg/kg is chosen because it creates a noticeable and long-lasting behavioral hypoactivity. Guanoxabenz (0.1-3 mg/kg, ip) causes a dose-related reduction in locomotor activity[4].
|
| Animal Protocol |
Animal/Disease Models: Rats[4].
Doses: 0.5 mg/kg (RX 781094 or saline vehicle was injected intravenously (iv) (tail vein) at the time of peak effect of the agonist (20min for clonidine and 30 min for Guanoxabenz). Route of Administration: IP. Experimental Results: RX 781094 (0.1-1.0 mg/kg, iv) produces a rapid (< 5 set) and complete antagonism of the EEG and behavioral effects induced by clonidine and Guanoxabenz. |
| References |
[1]. Uhlén S, et al. Characterization of the enzymatic activity for biphasic competition by guanoxabenz (1-(2,6-dichlorobenzylidene-amino)-3-hydroxyguanidine) at alpha2-adrenoceptors. I. Description of an enzymatic activity in spleen membranes. Biochem Pharmac
[2]. Dambrova M, et al. Characterization of the enzymatic activity for biphasic competition by guanoxabenz (1-(2,6-dichlorobenzylidene-amino)-3-hydroxyguanidine) at alpha2-adrenoceptors. II. Description of a xanthine-dependent enzymatic activity in spleen cyto [3]. Dambrova M, et al. Characterization of Guanoxabenz reducing activity in rat brain. Pharmacol Toxicol. 1998 Oct;83(4):158-63. [4]. P W Dettmar, et al. Neuropharmacological studies in rodents on the action of RX 781094, a new selective alpha 2-adrenoceptor antagonist. Neuropharmacology. 1983 Jun;22(6):729-37. |
| Molecular Formula |
C8H9CL3N4O
|
|---|---|
| Molecular Weight |
283.54
|
| Exact Mass |
281.984
|
| CAS # |
23256-40-8
|
| Related CAS # |
Guanoxabenz;24047-25-4
|
| PubChem CID |
9567830
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
16
|
| Complexity |
249
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
Cl.ON/C(=N/N=C/C1C(Cl)=CC=CC=1Cl)/N
|
| InChi Key |
PQPZROSFRCBPIM-AQCBZIOHSA-N
|
| InChi Code |
InChI=1S/C8H8Cl2N4O.ClH/c9-6-2-1-3-7(10)5(6)4-12-13-8(11)14-15;/h1-4,15H,(H3,11,13,14);1H/b12-4+;
|
| Chemical Name |
2-[(E)-(2,6-dichlorophenyl)methylideneamino]-1-hydroxyguanidine;hydrochloride
|
| 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) |
DMSO: 83.33 mg/mL (293.89 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.34 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 (7.34 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5268 mL | 17.6342 mL | 35.2684 mL | |
| 5 mM | 0.7054 mL | 3.5268 mL | 7.0537 mL | |
| 10 mM | 0.3527 mL | 1.7634 mL | 3.5268 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
