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Chemical Structure| 23256-50-0 Chemical Structure| 23256-50-0

Structure of Guanabenz Acetate
CAS No.: 23256-50-0

Chemical Structure| 23256-50-0

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Guanabenz acetate is a centrally-acting α-2 adrenergic receptor agonist that is used as an antihypertensive drug to treat hypertension.

Synonyms: Wy8678 acetate; BR-750; Guanabenz(Acetate)

4.5 *For Research Use Only !

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Product Details of Guanabenz Acetate

CAS No. :23256-50-0
Formula : C10H12Cl2N4O2
M.W : 291.13
SMILES Code : ClC1=C(/C=N/NC(N)=N)C(Cl)=CC=C1.CC(O)=O
Synonyms :
Wy8678 acetate; BR-750; Guanabenz(Acetate)
MDL No. :MFCD00153801
InChI Key :MCSPBPXATWBACD-GAYQJXMFSA-N
Pubchem ID :5702062

Safety of Guanabenz Acetate

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H301
Precautionary Statements:P301+P310
Class:6.1
UN#:2811
Packing Group:

Related Pathways of Guanabenz Acetate

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Jurkat T lymphocytes 5 or 10 µM Suppressed PMA-induced upregulation of IL2 and IFNγ mRNA expression PMC4881500
HeLa cells 0-200 µM 24 hours To assess the impact of Guanabenz on HeLa cell viability, showing toxicity at concentrations of 125 µM and above. PMC4605330
HCM-BROD-0106-C71 cells 50 μM 24 hours To evaluate the cytotoxicity of Guanabenz on patient-derived glioblastoma cells and its combined effect with Sunitinib. Results showed that Guanabenz enhanced the cytotoxicity of Sunitinib on patient-derived glioblastoma cells. PMC8423979
T98G-R cells 50 μM 24 hours To evaluate the cytotoxicity of Guanabenz on TMZ-resistant glioblastoma cells and its combined effect with Sunitinib. Results showed that Guanabenz enhanced the cytotoxicity of Sunitinib on TMZ-resistant glioblastoma cells. PMC8423979
A172 cells 50 μM 24 hours To evaluate the cytotoxicity of Guanabenz on glioblastoma cells and its combined effect with Sunitinib. Results showed that Guanabenz enhanced the cytotoxicity of Sunitinib on glioblastoma cells and reduced Sunitinib-induced autophagy. PMC8423979
U-87MG cells 50 μM 24 hours To evaluate the cytotoxicity of Guanabenz on glioblastoma cells and its combined effect with Sunitinib. Results showed that Guanabenz enhanced the cytotoxicity of Sunitinib on glioblastoma cells and reduced Sunitinib-induced autophagy. PMC8423979
DLD1 cells 50 µM 48 hours GBZ treatment reduced the expression of β-catenin target genes PMC8814139
U2OS cells 50 µM overnight GBZ treatment induced condensation of transiently expressed conductin PMC8814139
HMC-1.1 mast cells 10 µM Suppressed PMA-induced upregulation of TNFα and IL13 mRNA expression PMC4881500
Human placental BeWo cell line 5 μM 24 hours To assess the effect of GADD34 inhibition on ER stress-induced reduction in mTORC1 activity, results showed that guanabenz attenuated the tunicamycin-mediated increase in CHOP protein levels and reduction in mTORC1 activity PMC10644500
SW480 cells 50 µM 48 hours GBZ treatment decreased β-catenin levels, which was markedly attenuated by conductin knockout PMC8814139
Differentiated oligodendrocyte progenitor cells (dOPCs) 5.0 μM 48 hours Guanabenz protected dOPCs from IFN-γ-mediated apoptotic death, restoring cell survival to control levels. PMC4360920
J774.1 cells 50 μM 6 hours Measure mRNA expression levels of inflammatory cytokines, results showed that Guanabenz blocked LPS-induced increases in IFN-γ, TNF-α, IL-6, IL-1β, and COX-2 mRNA expression PMC6495372
Primary macrophages 10 µM 6 hours Suppressed LPS-induced upregulation of IL1β, IL6, TNFα, and Cox2 mRNA expression PMC4881500
RAW264.7 macrophages 10 µM 6 hours Suppressed LPS-induced upregulation of IL1β, IL6, TNFα, and Cox2 mRNA expression PMC4881500
Bone marrow-derived dendritic cells 50 µM 8 hours To evaluate the effect of GBZ on IL-10 production in LPS-stimulated dendritic cells. Results showed that GBZ increased IL-10 production. PMC5468566

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice MPZmutant mice and SOD1mutant mice Oral 1 mg/kg or 5 mg/kg Twice a day or once a day for several weeks to months Sephin1 prevented the motor, morphological, and molecular defects of MPZmutant and SOD1mutant mice without adverse effects. PMC4490275
BALB/c nude mice SW480 xenograft model Oral 50 µM Daily for 20 days GBZ treatment reduced tumor growth by about 60% PMC8814139
Mice Tsc1 conditional knockout mice Intraperitoneal injection 8 mg/kg Once daily from P7 to P14 To evaluate the effect of Guanabenz on oligodendrocyte survival and myelination in Tsc1 mutant mice, results showed that Guanabenz treatment partially rescued myelination defects PMC4947172
Mice GFAP/tTA; TRE/IFN-γ transgenic mice Intraperitoneal injection 4 mg/kg Daily from P7 to P18 Guanabenz protected oligodendrocytes and myelin from the detrimental effects of IFN-γ, restoring myelination to levels observed in wild type littermates. PMC4360920
Mice (C57BL/6J) Experimental autoimmune encephalomyelitis (EAE) model Intraperitoneal injection 8 mg/kg Once daily, starting from PID 7 until the end of the study To evaluate the effect of Sephin1 on the disease progression in EAE model mice. Results showed that Sephin1 significantly delayed disease onset, reduced oligodendrocyte and axon loss, and decreased T cell presence in the CNS. PMC6351782
NOD-SCID mice U-87MG glioblastoma xenograft model Peritumoral injection 10 mg/kg 3 injections on days 14, 21, and 28 To evaluate the therapeutic effect of combined treatment with Guanabenz and Sunitinib on glioblastoma xenograft model. Results showed that combined treatment significantly inhibited tumor growth, reduced Ki67 expression, and decreased autophagy-related markers. PMC8423979
Drosophila OPMD model Oral 3 mM Daily administration until adulthood Alleviate OPMD phenotypes, including muscle degeneration and nuclear inclusion formation PMC3044817
C57BL/6 mice OVX-induced osteoporosis model Intraperitoneal injection 4, 8 mg/kg Every two days for 6 weeks Inhibition of OVX-induced osteoporosis PMC10943029
C57BL/6 mice Tunicamycin-induced ER stress model Intraperitoneal injection 4 mg/kg For 3 consecutive days Sephin1 significantly suppressed tunicamycin-induced renal tubular cell death, improved survival, and markedly suppressed nuclear translocation of CHOP. PMC11840111
BALB/cJ and C57BL/6J mice Chronic Toxoplasma infection model Intraperitoneal injection 5 mg/kg Once daily for 3 to 6 weeks Evaluate the effects of Guanabenz on brain cyst burden and neuroinflammation in chronically Toxoplasma-infected mice. Results showed that Guanabenz significantly reduced brain cyst burden (~75%) in BALB/cJ mice via i.p. injection and reversed Toxoplasma-induced hyperactivity, which correlated with reduced neuroinflammation. However, in C57BL/6J mice, Guanabenz increased cyst burden but still reversed hyperactivity. PMC6495372
BALB/cJ and C57BL/6J mice Chronic Toxoplasma infection model Oral gavage 10 mg/kg Once daily for 3 to 6 weeks Evaluate the effects of Guanabenz on brain cyst burden and neuroinflammation in chronically Toxoplasma-infected mice. Results showed that Guanabenz significantly reduced brain cyst burden (~75%) in BALB/cJ mice via i.p. injection and reversed Toxoplasma-induced hyperactivity, which correlated with reduced neuroinflammation. However, in C57BL/6J mice, Guanabenz increased cyst burden but still reversed hyperactivity. PMC6495372
C57BL/6 mice D-galactosamine/LPS-induced liver damage model Intraperitoneal injection 2 mg/kg Single injection, observed for 48 hours To evaluate the effect of GBZ on d-galN/LPS-induced liver damage and mortality. Results showed that GBZ significantly improved Mice survival, reduced liver damage, increased IL-10 levels, and inhibited TNF-α production. PMC5468566
C57BL/6 mice G93A mtSOD1 transgenic mice Intraperitoneal injection 8 mg/kg Three times a week starting at 60 days of age Guanabenz significantly delayed disease onset, prolonged the duration of the early phase of disease, and extended survival of G93A mice. PMC4179984

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02423083 Multiple Sclerosis, Relapsing-... More >>Remitting Multiple Sclerosis Less << Phase 1 Terminated - United States, Maryland ... More >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 Less <<
NCT02443103 Bone Cancer M... More >>etastasis Less << Not Applicable Terminated(Slow accrual) - United States, Indiana ... More >> Indiana University Health Hospital Indianapolis, Indiana, United States, 46202 Indiana University Melvin and Bren Simon Cancer Center Indianapolis, Indiana, United States, 46202 Sidney & Lois Eskenazi Hospital Indianapolis, Indiana, United States, 46202 Spring Mill Medical Center Indianapolis, Indiana, United States, 46290 Less <<
NCT02443103 - Terminated(Slow accrual) - -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.43mL

0.69mL

0.34mL

17.17mL

3.43mL

1.72mL

34.35mL

6.87mL

3.43mL

References

 

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