AMifostine Thiol

AMifostine Thiol - Names and Identifiers

Name	Amifostine Thiol Dihydrochloride
Synonyms	WR-1065 2HCl AMifostine Thiol WR-1065 dihydrochloride Amifostine Thiol Dihydrochloride 2-[(3-AMinopropyl)aMino]ethanethiol Hydrochloride 2-[(3-Aminopropyl)amino]ethanethioldihydrochloride Amifostine Thiol (50 mg) (2-[(3-aminopropyl)amino]ethanethiol, dihydrochloride)
CAS	14653-77-1

AMifostine Thiol - Physico-chemical Properties

Molecular Formula	C5H16Cl2N2S
Molar Mass	207.16
Melting Point	184-186°C
Water Solubility	H2O: ≥20mg/mL
Appearance	Morphological powder color white to off-white
Storage Condition	-20°C
Use	WR-1065 dihydrochloride can protect normal tissues from the toxic effects of some cancer drugs and activate p53 through the JNK-dependent signaling pathway.

AMifostine Thiol - Risk and Safety

Hazard Symbols	Xn - Harmful
Risk Codes	R22 - Harmful if swallowed R41 - Risk of serious damage to eyes
Safety Description	S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S39 - Wear eye / face protection. S41 - In case of fire and / or explosion do not breathe fumes.
WGK Germany	3
HS Code	2930909165

AMifostine Thiol - Introduction

Target
p53

In vitro studies
The DNA-binding activity is increased in a WR-1065 dihydrochloride (WR-1065) concentration-dependent manner. Cells treated with 1 mM WR-1065 dihydrochloride for 24 h reveal that all of the p53-induced genes analyzed are transactivated following WR-1065 dihydrochloride treatment, in a p53-dependent manner. Significantly, treatment with WR-1065 dihydrochloride leads to a 3-fold increase in luciferase expression driven by AP-1, and a 5-fold increase when this reporter gene is driven by NF-κ B, when these values are normalized to the level of the cotransfected β-galactosidase gene.

In vivo studies
The results show that wR-1065 dihydrochloride (WR-1065) attenuates the severity of 6-OHDA-induced catalepsy (P<0.001) when compare with 6-OHDA-lesioned rats. Also it has been observed that WR-1065 dihydrochloride improves catalepsy in dose dependent manner (P<0.001). Pretreatment with three different doses of WR-1065 dihydrochloride (20, 40 and 80 μg/2 μL/rat) for 3 days before 6-OHDA administration, significantly (P<0.001) elevates SOD activity and restores it to normal range compare with 6-OHDA lesioned rats.

Last Update：2024-04-10 22:29:15