Synonym
L-749329; L749329; L 749329
IUPAC/Chemical Name
4-[1-(1,3-Benzodioxol-5-yl)-2-oxo-2-[(4-propan-2-ylphenyl)sulfonylamino]ethoxy]-3-propylbenzoic acid
InChi Key
JPPYWKVKLSBQJM-UHFFFAOYSA-N
InChi Code
InChI=1S/C28H29NO8S/c1-4-5-19-14-21(28(31)32)9-12-23(19)37-26(20-8-13-24-25(15-20)36-16-35-24)27(30)29-38(33,34)22-10-6-18(7-11-22)17(2)3/h6-15,17,26H,4-5,16H2,1-3H3,(H,29,30)(H,31,32)
SMILES Code
O=C(O)C1=CC=C(OC(C2=CC=C(OCO3)C3=C2)C(NS(=O)(C4=CC=C(C(C)C)C=C4)=O)=O)C(CCC)=C1
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
Preparing Stock Solutions
The following data is based on the
product
molecular weight
539.60
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.
| 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 |
1: Maguire JJ, Kuc RE, Davenport AP. Defining the affinity and receptor sub-type selectivity of four classes of endothelin antagonists in clinically relevant human cardiovascular tissues. Life Sci. 2012 Oct 15;91(13-14):681-6. doi: 10.1016/j.lfs.2012.05.008. Epub 2012 May 23. PubMed PMID: 22634326.
2: Huckle WR, Drag MD, Acker WR, Powers M, McFall RC, Holder DJ, Walsh TF, Schwartz RS, Greenlee WJ, Johnson RG Jr. Effects of L-749,329, an ET(A)/ET(B) endothelin receptor antagonist, in a porcine coronary artery injury model of vascular restenosis. Circulation. 2001 Apr 10;103(14):1899-905. PubMed PMID: 11294810.
3: Hara M, Tozawa F, Itazaki K, Mihara S, Fujimoto M. Endothelin ET(B) receptors show different binding profiles in intact cells and cell membrane preparations. Eur J Pharmacol. 1998 Mar 26;345(3):339-42. PubMed PMID: 9592035.
4: Wu-Wong JR, Chiou WJ, Hoffman DJ, Winn M, von Geldern TW, Opgenorth TJ. Endothelins and endothelin receptor antagonists: binding to plasma proteins. Life Sci. 1996;58(21):1839-47. PubMed PMID: 8637410.
5: Iwasaki T, Mihara S, Shimamura T, Kawakami M, Masui M, Hayasaki-Kajiwara Y, Naya N, Ninomiya M, Fujimoto M, Nakajima M. Pharmacologic characterization of S-1255, a highly potent and orally active endothelin A receptor antagonist. J Cardiovasc Pharmacol. 2001 Apr;37(4):471-82. PubMed PMID: 11300660.
6: Wu-Wong JR, Dixon DB, Chiou WJ, Opgenorth TJ. Endothelin receptor antagonists: effect of serum albumin on potency and comparison of pharmacological characteristics. J Pharmacol Exp Ther. 1997 May;281(2):791-8. PubMed PMID: 9152387.
