Guanabenz

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

guanabenz (WY 8678) 是一种 α2 肾上腺素能受体激动剂，用作抗高血压药。

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. (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.

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 hResult:Did not affect cell survival.RT-PCRCell 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.

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.

WY 8678

Metabolic Enzyme/Protease

Protein Phosphatase/PTP

Protein Phosphatase/PTP

Inflammation/Immunology

Multiple Sclerosis

5051-62-7

231.08

C8H8Cl2N4

>98% (HPLC)

——

N/C(N)=N\N=C\C1=C(Cl)C=CC=C1Cl

2-[(E)-(2,6-dichlorophenyl)methylideneamino]guanidine

(-20℃)

With Ice Pack

≥ 2 years