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.


Chemical Structure

img
ZD1611
CAS# 186497-38-1

Theoretical Analysis

MedKoo Cat#: 525695
Name: ZD1611
CAS#: 186497-38-1
Chemical Formula: C22H24N4O5S
Exact Mass: 456.15
Molecular Weight: 456.517
Elemental Analysis: C, 57.88; H, 5.30; N, 12.27; O, 17.52; S, 7.02

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

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

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).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 456.52 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

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.