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Amifostine thiol

Cat. No. M13550
Amifostine thiol Structure
Synonym:

WR-1065

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Biological Activity

Amifostine thiol (WR-1065) is an active metabolite of the cytoprotector Amifostine . Amifostine thiol is a cytoprotective agent with radioprotective abilities. Amifostine thiol activates p53 through a JNK-dependent signaling pathway.

Chemical Information
Molecular Weight 134.24
CAS Number 31098-42-7
Solubility (25°C) DMSO 150 mg/mL
Water 90 mg/mL
Storage 2-8°C, protect from light, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ioannis Bougioukas, et al. Interact Cardiovasc Thorac Surg. The effect of amifostine on lung ischaemia-reperfusion injury in rats

[2] John R Kouvaris, et al. Oncologist. Amifostine: the first selective-target and broad-spectrum radioprotector

[3] Michael I Koukourakis. Semin Oncol. Amifostine: is there evidence of tumor protection?

[4] V Santini. Expert Opin Pharmacother. Amifostine: chemotherapeutic and radiotherapeutic protective effects

[5] L M Shaw, et al. Semin Oncol. Pharmacokinetic profile of amifostine

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Keywords: Amifostine thiol, WR-1065 supplier, p53, inhibitors, activators


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