Guanabenz

SKU: orb1224901

Description

Guanabenz (WY 8678) is an α2 adrenergic receptor agonist that is used as an antihypertensive agent, also has been proposed to exert protective effects against misfolding by interfering with eIF2α-P dephosphorylation through selective disruption of a PP1-PPP1R15A holophosphatase complex; also has antiparasitic activity against replicative stages of Toxoplasma.Multiple Sclerosis Phase 1 Clinical(In Vitro):Guanabenz hydrochloride (0.5-50 μM, 24 h) is treated with increasing concentrations for 24 hours not affect cell viability.Guanabenz hydrochloride (0.5-50 μM, 24 h) alone not affects the UPR targets, neither on mRNA or protein level nor the phosphorylation status of eIF2a. Guanabenz also not induces GADD34 or the constitutively active form CReP.Guanabenz hydrochloride (0.5-50 μM, 24 h) alone not induces ER stress in neonatal rat cardiomyocytes.\n(In Vivo):Guanabenz hydrochloride (5 mg/kg/day; i.p.; for 3 weeks) can reproducibly reduce brain cyst burden.Guanabenz hydrochloride (5 mg /kg/d, i.p., oral; 10 mg/kg/d, gavage; for 3 weeks) reverses Toxoplasma-induced hyperactivity in latently infected mice.Guanabenz hydrochloride (100 and 320 μg/kg and 1 mg/kg, i.v., over a period of 5 min at intervals of 40 min) reduces sympathetic outflow, heart rate and blood pressure in debuffered cats.

Key Properties

• CAS Number: 5051-62-7
• MW: 231.08
• Purity: >98% (HPLC)
• Formula: C₈H₈Cl₂N₄
• SMILES: N/C(N)=N\N=C\C1=C(Cl)C=CC=C1Cl
• Target: Protein Phosphatase/PTP

Bioactivity

• In Vivo:
  Guanabenz (5 mg/kg/day; i.p.; for 3 weeks) can reproducibly reduce brain cyst burden. Guanabenz (5 mg /kg/d, i.p. , oral; 10 mg/kg/d, gavage; for 3 weeks) reverses Toxoplasma-induced hyperactivity in latently infected mice. Guanabenz (100 and 320 μg/kg and 1 mg/kg, i. v. , over a period of 5 min at intervals of 40 min) reduces sympathetic outflow, heart rate and blood pressure in debuffered cats. Animal model: BALB/cJ mice. Dosage: 5 mg/kg. Administration: 5 mg/kg/day; i.p.; for 3 weeks. Result: Reduced the latent brain cysts in both male and female BALB/cJ mice. Animal model: BALB/cJ mice. Dosage: 5 mg/kg; 10 mg/kg. Administration: 5 mg /kg/d, i.p. , oral; 10 mg/kg/d, gavage; for 3 weeks. Result: Reversed parasite-induced hyperactivity to near-baseline levels. Animal model: Cats. Dosage: 100 and 320 μg/kg and 1 mg/kg. Administration: 100 and 320 μg/kg and 1 mg/kg, i. v. , over a period of 5 min at intervals of 40 min. Result: Declined markedly blood pressure and nerve activity.
• In Vitro:
  Guanabenz (0.5-50 μM, 24 h) is treated with increasing concentrations for 24 hours not affect cell viability. Guanabenz (0.5-50 μM, 24 h) alone not affects the UPR targets, neither on mRNA or protein level nor the phosphorylation status of eIF2a. Guanabenz also not induces GADD34 or the constitutively active form CReP. Guanabenz (0.5-50 μM, 24 h) alone not induces ER stress in neonatal rat cardiomyocytes. Cell Viability Assay Cell line: Neonatal rat cardiac myocytes (NRCM). Concentration: 0.5-50 μM Incubation time: 24 h. Result: Did not affect cell survival. RT-PCR Cell line: Neonatal rat cardiac myocytes (NRCM). Concentration: 0.5-50 μM Incubation time: 24 h. Result: Did not affect levels of UPR targets. Western blot analysis. Cell line: Neonatal rat cardiac myocytes (NRCM). Concentration: 0.5-50 μM Incubation time: 24 h. Result: Increased the levels of low panel concentration-dependent UPR targets proteins.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

WY 8678

Quick Database Links

Gene Symbol

Protein Phosphatase/PTP