| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Numerous guanixaben N-hydroxyguanidine analogues and a variety 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 guanixabenzene conjugates. Preincubating the membrane with guanoxabenz's LW03 N-hydroxyguanidine analog inhibits the establishment of high-affinity binding in a time- and concentration-dependent way [1]. The conversion of guanobendazole to guanobenzene is mediated by the splenic cytosolic fraction. Guanobenzene has a nearly 100-fold greater affinity for rat α2A-adrenergic receptors than does guanobenzene itself [2].
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|---|---|
| ln Vivo |
Both guanifaben and guanidine are known as centrally active antihypertensive medications. High-affinity guanizoxen binding is induced in rat meninges after administration of NADH or NADPH cofactors. The rat cerebral cortex has an enzyme activity that may activate guanidoxybenzenes leading to the production of metabolites with high affinity for α2-adrenergic receptors [3]. Guanixaben (0.1-3 mg/kg, intraperitoneally) generates a dose-related reduction in locomotor activity; the dose of 1 mg/kg was chosen since it causes a considerable and sustained reduction in behavioral activity [4].
|
| Animal Protocol |
Animal/Disease Models: Rat[4].
Doses: 0.5 mg/kg (RX 781094 or saline vehicle) intravenously (iv) (iv)(iv) (tail vein) at peak agonist effect (20 minutes for clonidine, 30 minutes for guazobenza). Mode of Route of Administration: IP. Experimental Results: RX 781094 (0.1- 1.0 mg/kg, i.v.) produces rapid (< 5 groups) and complete antagonism of clonidine- and guanoxaben-induced EEG and behavioral effects. |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Guanoxabenz is a known human metabolite of guanabenz. |
| References |
|
| Additional Infomation |
Guanoxabenz is a dichlorobenzene.
|
| Molecular Formula |
C8H8N4OCL2
|
|---|---|
| Molecular Weight |
247.08132
|
| Exact Mass |
246.008
|
| CAS # |
24047-25-4
|
| Related CAS # |
Guanoxabenz hydrochloride;23256-40-8
|
| PubChem CID |
9567831
|
| Appearance |
Typically exists as solid at room temperature
|
| Boiling Point |
435.6ºC at 760mmHg
|
| Flash Point |
217.2ºC
|
| LogP |
2.712
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
15
|
| Complexity |
249
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
ClC1=C(/C=N/NC(NO)=N)C(Cl)=CC=C1
|
| InChi Key |
QKIQJNNDIWGVEH-UUILKARUSA-N
|
| InChi Code |
InChI=1S/C8H8Cl2N4O/c9-6-2-1-3-7(10)5(6)4-12-13-8(11)14-15/h1-4,15H,(H3,11,13,14)/b12-4+
|
| Chemical Name |
2-[(E)-(2,6-dichlorophenyl)methylideneamino]-1-hydroxyguanidine
|
| 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 |
| 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 | 4.0473 mL | 20.2364 mL | 40.4727 mL | |
| 5 mM | 0.8095 mL | 4.0473 mL | 8.0945 mL | |
| 10 mM | 0.4047 mL | 2.0236 mL | 4.0473 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.
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