| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Cell viability is not affected by treating ganabenzene at increasing concentrations for 24 hours (0.5-50 μM) [1]. Guanidine alone (0.5–50 μM, 24 h) had no effect on UPR targets' mRNA, protein, or eIF2a phosphorylation levels. Furthermore, neither GADD34 nor the constitutively active version of CReP are induced by guanabenz[1]. In newborn rat cardiomyocytes, guanidine (0.5-50 μM) does not cause endoplasmic reticulum stress over a 24-hour period [1].
|
|---|---|
| ln Vivo |
For three weeks, guanabenz (5 mg/kg/day; intraperitoneally) lowers the burden of brain cysts in a reproducible manner [2]. In mice that are latently infected, guanabenz (5 mg/kg/d, intraperitoneal injection, orally; 10 mg/kg/d, gavage, for 3 weeks) can correct the hyperactivity caused by Toxoplasma [2]. In debuffered cats, guanabenz (100 and 320 μg/kg and 1 mg/kg intravenously for 5 minutes at 40-minute intervals) lowers blood pressure, heart rate, and sympathetic outflow [3].
|
| Cell Assay |
Cell viability assay [1]
Cell Types: Neonatal rat cardiomyocytes (NRCM) Tested Concentrations: 0.5–50 μM Incubation Duration: 24 hrs (hours) Experimental Results: No effect on cell survival. RT-PCR[1] Cell Types: Neonatal rat cardiomyocytes (NRCM) Tested Concentrations: 0.5–50 μM Incubation Duration: 24 hrs (hours) Experimental Results: Does not affect levels of UPR targets. Western Blot Analysis[1] Cell Types: Neonatal rat cardiomyocytes (NRCM) Tested Concentrations: 0.5–50 μM Incubation Duration: 24 hrs (hours) Experimental Results: The levels of UPR target proteins increased in a concentration-dependent manner in the low group. |
| Animal Protocol |
Animal/Disease Models: BALB/cJ mice [2]
Doses: 5 mg/kg Doses: 5 mg/kg/day; ip; for 3 weeks Experimental Results: Latent brain cysts were diminished in both male and female BALB/cJ mice . Animal/Disease Models: BALB/cJ mice[2] Doses: 5 mg/kg; 10 mg/kg Route of Administration: 5 mg/kg/d, intraperitoneal (ip) injection, oral administration; 10 mg/kg/d, gavage; last for 3 weeks Experimental Results: Reversal of parasite-induced hyperactivity to near baseline levels. Animal/Disease Models: Cat [3] Doses: 100 and 320 μg/kg and 1 mg/kg Route of Administration: 100 and 320 μg/kg and 1 mg/kg, intravenously (iv) (iv)(iv) for 5 minutes at 40 minute intervals Experimental Results: Rejection of blood pressure and Neural activity is evident. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Approximately 75% absorbed from gastrointestinal tract Metabolism / Metabolites Hepatic Guanabenz has known human metabolites that include Guanoxabenz. Biological Half-Life 6 hours. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Because no information is available on the use of guanabenz during breastfeeding, other agents may be preferred, especially while nursing a newborn or preterm infant. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. Protein Binding 90% |
| References |
|
| Additional Infomation |
Guanabenz is a dichlorobenzene.
Guanabenz is a Central alpha-2 Adrenergic Agonist. The mechanism of action of guanabenz is as an Adrenergic alpha2-Agonist. An alpha-2 selective adrenergic agonist used as an antihypertensive agent. See also: Guanabenz Acetate (has salt form). Drug Indication For management of High blood pressure FDA Label Mechanism of Action Guanabenz's antihypertensive effect is thought to be due to central alpha-adrenergic stimulation, which results in a decreased sympathetic outflow to the heart, kidneys, and peripheral vasculature in addition to a decreased systolic and diastolic blood pressure and a slight slowing of pulse rate. Chronic administration of guanabenz also causes a decrease in peripheral vascular resistance. Pharmacodynamics Guanabenz, a centrally acting α-2 adrenergic agonist, is indicated for treatment of hypertension. |
| Molecular Formula |
C8H8CL2N4
|
|---|---|
| Molecular Weight |
231.08
|
| Exact Mass |
230.013
|
| CAS # |
5051-62-7
|
| Related CAS # |
Guanabenz hydrochloride;23113-43-1;(E)-Guanabenz;60329-03-5
|
| PubChem CID |
5702063
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.49g/cm3
|
| Boiling Point |
405.7ºC at 760mmHg
|
| Melting Point |
227-229ºC (decomposition)
|
| Flash Point |
199.1ºC
|
| Index of Refraction |
1.645
|
| LogP |
3.001
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
14
|
| Complexity |
228
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=CC(=C(C(=C1)Cl)C=NN=C(N)N)Cl
|
| InChi Key |
WDZVGELJXXEGPV-YIXHJXPBSA-N
|
| InChi Code |
InChI=1S/C8H8Cl2N4/c9-6-2-1-3-7(10)5(6)4-13-14-8(11)12/h1-4H,(H4,11,12,14)/b13-4+
|
| Chemical Name |
2-[(E)-(2,6-dichlorophenyl)methylideneamino]guanidine
|
| Synonyms |
WY-8678; Guanabenz
|
| 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 | 4.3275 mL | 21.6375 mL | 43.2751 mL | |
| 5 mM | 0.8655 mL | 4.3275 mL | 8.6550 mL | |
| 10 mM | 0.4328 mL | 2.1638 mL | 4.3275 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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