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ZD-1611 

Cat. No. M28967
ZD-1611  Structure
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Biological Activity

ZD-1611 is a potent, orally active, selective ETA receptor antagonist, used for the research of ischemic stroke.

Chemical Information
Molecular Weight 456.51
Formula C22H24N4O5S
CAS Number 186497-38-1
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Huw Bowen Jones, et al. Toxicol Pathol. Coronary and systemic arterial physiology and immunohistochemical markers related to early coronary arterial lesions in beagle dogs given the potassium channel opener, ZD6169, or the endothelin receptor antagonist, ZD1611

[2] Aida Maddahi, et al. J Neuroinflammation. Cerebral ischemia induces microvascular pro-inflammatory cytokine expression via the MEK/ERK pathway

[3] Emelie Stenman, et al. Eur J Pharmacol. Cooperative effect of angiotensin AT(1) and endothelin ET(A) receptor antagonism limits the brain damage after ischemic stroke in rat

[4] Huw B Jones, et al. Toxicol Pathol. Endothelin antagonist-induced coronary and systemic arteritis in the beagle dog

[5] C Wilson, et al. J Pharmacol Exp Ther. Pharmacological profile of ZD1611, a novel, orally active endothelin ETA receptor antagonist

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  Catalog
Abmole Inhibitor Catalog




Keywords: ZD-1611  supplier, Endothelin Receptor, inhibitors, activators


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