ZD1611

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 525695

CAS#: 186497-38-1

Description: ZD1611 is an endothelin receptor antagonist.


Price and Availability

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ZD1611 is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 525695
Name: ZD1611
CAS#: 186497-38-1
Chemical Formula: C22H24N4O5S
Exact Mass: 456.1467
Molecular Weight: 456.517
Elemental Analysis: C, 57.88; H, 5.30; N, 12.27; O, 17.52; S, 7.02


Synonym: ZD1611

IUPAC/Chemical Name: 3-[4-[3-[(3-Methoxy-5-methylpyrazin-2-yl)sulfamoyl]pyridin-2-yl]phenyl]-2,2-dimethylpropanoic acid

InChi Key: CDBNTQYPMBJKQZ-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: O=C(O)C(C)(C)CC1=CC=C(C2=NC=CC=C2S(=O)(NC3=NC=C(C)N=C3OC)=O)C=C1


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: Jones HB, Björkman JA, Schofield J. 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. Toxicol Pathol. 2013 Jul;41(5):722-35. doi: 10.1177/0192623312464123. Epub 2012 Nov 2. PubMed PMID: 23125115.

2: Maddahi A, Edvinsson L. Cerebral ischemia induces microvascular pro-inflammatory cytokine expression via the MEK/ERK pathway. J Neuroinflammation. 2010 Feb 26;7:14. doi: 10.1186/1742-2094-7-14. Erratum in: J Neuroinflammation. 2011;8:18. PubMed PMID: 20187933; PubMed Central PMCID: PMC2837637.

3: Stenman E, Jamali R, Henriksson M, Maddahi A, Edvinsson L. 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. PubMed PMID: 17597600.

4: Jones HB, Macpherson A, Betton GR, Davis AS, Siddall R, Greaves P. Endothelin antagonist-induced coronary and systemic arteritis in the beagle dog. Toxicol Pathol. 2003 May-Jun;31(3):263-72. PubMed PMID: 12746113.

5: Berg T. The vascular response to the K+ channel inhibitor 4-aminopyridine in hypertensive rats. Eur J Pharmacol. 2003 Apr 18;466(3):301-10. PubMed PMID: 12694813.

6: Bialecki RA, Fisher CS, Abbott BM, Barthlow HG, Caccese RG, Stow RB, Rumsey J, Rumsey W. ZD1611, an orally active endothelin-A receptor antagonist, prevents chronic hypoxia-induced pulmonary hypertension in the rat. Pulm Pharmacol Ther. 1999;12(5):303-12. PubMed PMID: 10545286.

7: Wilson C, Hunt SJ, Tang E, Wright N, Kelly E, Palmer S, Heys C, Mellor S, James R, Bialecki R. Pharmacological profile of ZD1611, a novel, orally active endothelin ETA receptor antagonist. J Pharmacol Exp Ther. 1999 Sep;290(3):1085-91. PubMed PMID: 10454481.

8: Bialecki RA, Stinson-Fisher C, Murdoch W, Bertelsen D, Desiato M, Rumsey W. A novel orally active endothelin-A receptor antagonist, ZD1611, prevents chronic hypoxia-induced pulmonary hypertension in the rat. Chest. 1998 Jul;114(1 Suppl):91S. PubMed PMID: 9676649.