J-104132
| Code | Size | Price |
|---|
| TAR-T27647-5mg | 5mg | £2,376.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T27647-50mg | 50mg | £4,713.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T27647-100mg | 100mg | £6,657.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃
Documents
Further Information
Bioactivity:
J-104132 is a potetn and selective endothelin A/B receptor antagonist (Ki: cloned human ETA = 0.034 nM; cloned human ETB = 0.104 nM) . In vitro, J-104132 is a potent antagonist of ET-1-induced accumulation of [3H]inositol phosphates in Chinese hamster ovary cells stably expressing cloned human ETA receptors (IC50 = 0.059 nM). Pretreatment with J-104132 prevents the lethal response to ET-1 when administered i.v. (ED50 = 0.045 mg/kg) or p.o. in fed animals (ED50 = 0.35 mg/kg).
CAS:
198279-45-7
Formula:
C31H33NO7
Molecular Weight:
531.605
Purity:
0.98
SMILES:
CCCCc1ccc2[C@@H]([C@H]([C@@H](c2n1)c1ccc(OC)cc1C[C@H](C)C(O)=O)C(O)=O)c1ccc2OCOc2c1
References
1. Kitada K, Yui N, Mori T, Ohkita M, Matsumura Y. Vasoprotective effects of an endothelin receptor antagonist in ovariectomized female rats. Life Sci. 2014 Nov 24;118(2):379-85. doi: 10.1016/j.lfs.2014.01.009. PubMed PMID: 24468711.
2. Kitada K, Yui N, Koyama M, Kimura K, Suzuki R, Tanaka R, Mori T, Ohkita M, Matsumura Y. Endothelin ETB receptor is involved in sex differences in the development of balloon injury-induced neointimal formation. J Pharmacol Exp Ther. 2011 Feb;336(2):533-9. doi: 10.1124/jpet.109.165308. PubMed PMID: 21075838.
3. Kitada K, Yui N, Matsumoto C, Mori T, Ohkita M, Matsumura Y. Inhibition of endothelin ETB receptor system aggravates neointimal hyperplasia after balloon injury of rat carotid artery. J Pharmacol Exp Ther. 2009 Dec;331(3):998-1004. doi: 10.1124/jpet.109.157065. PubMed PMID: 19737855.
4. Homma N, Nagaoka T, Morio Y, Ota H, Gebb SA, Karoor V, McMurtry IF, Oka M. Endothelin-1 and serotonin are involved in activation of RhoA/Rho kinase signaling in the chronically hypoxic hypertensive rat pulmonary circulation. J Cardiovasc Pharmacol. 2007 Dec;50(6):697-702. PubMed PMID: 18091588.