Description
ZD-1611 is a potent, orally active, selective ETA receptor antagonist, used for the research of ischemic stroke.
Product information
CAS Number: 186497-38-1
Molecular Weight: 456.51
Formula: C22H24N4O5S
Chemical Name: 3-(4-{3-[(3-methoxy-5-methylpyrazin-2-yl)sulfamoyl]pyridin-2-yl}phenyl)-2,2-dimethylpropanoic acid
Smiles: CC1=CN=C(NS(=O)(=O)C2=CC=CN=C2C2C=CC(CC(C)(C)C(O)=O)=CC=2)C(=N1)OC
InChiKey: CDBNTQYPMBJKQZ-UHFFFAOYSA-N
InChi: InChI=1S/C22H24N4O5S/c1-14-13-24-19(20(25-14)31-4)26-32(29,30)17-6-5-11-23-18(17)16-9-7-15(8-10-16)12-22(2,3)21(27)28/h5-11,13H,12H2,1-4H3,(H,24,26)(H,27,28)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
ZD1611 competitively inhibits 125I-labeled ET-1 binding at human cloned ETA and ETB receptors with pIC50 values of 8.6 and 5.6, respectively, showing 1000-fold selectivity for the ETA receptor.
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. 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.
Products are for research use only. Not for human use.
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