ZD-1611
- Product Name
- ZD-1611
- CAS No.
- 186497-38-1
- Chemical Name
- ZD-1611
- Synonyms
- ZD-1611;ZD 1611,ZD1611;Benzenepropanoic acid, 4-[3-[[(3-methoxy-5-methyl-2-pyrazinyl)amino]sulfonyl]-2-pyridinyl]-α,α-dimethyl-
- CBNumber
- CB03175606
- Molecular Formula
- C22H24N4O5S
- Formula Weight
- 456.52
- MOL File
- 186497-38-1.mol
ZD-1611 Property
- Boiling point:
- 653.9±65.0 °C(Predicted)
- Density
- 1.339±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- pka
- 4.62±0.13(Predicted)
ZD-1611 Chemical Properties,Usage,Production
Uses
ZD-1611 is a potent, orally active, selective ETA receptor antagonist, used for the research of ischemic stroke.
in vivo
ZD1611 (0.3 mg/kg, p.o.) has a duration of action of more than 7 h in rats. In the dog, ZD1611 is active for at least 6 h at dose of 0.6 mg/kg p.o[1]. ZD1611 (0.15 mg/kg/day) in combination with candesartan decreases the brain damage and improves the neurological scores in rats. However, ZD1611 or candesartan alone does not significantly decrease the brain damage or improve neurological scores[2].
IC 50
ETA
References
[1] Wilson C, et al. Pharmacological profile of ZD1611, a novel, orally active endothelin ETA receptor antagonist. J Pharmacol Exp Ther. 1999 Sep;290(3):1085-91. PMID:10454481
[2] Stenman E, et al. Cooperative effect of angiotensin AT(1) and endothelin ET(A) receptor antagonism limits the brain damage after ischemic stroke in rat. Eur J Pharmacol. 2007 Sep 10;570(1-3):142-8. Epub 2007 Jun 9. DOI:10.1016/j.ejphar.2007.05.049
ZD-1611 Preparation Products And Raw materials
Raw materials
Preparation Products
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