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CAS No. :
MCE 国际站:IRL-1620 TFA
产品活性:IRL-1620 (TFA) 是高效,选择性的内啡肽受体 (endothelin receptor) B 型激动剂,Ki 值为 16 pM。
研究领域:GPCR/G Protein
作用靶点:Endothelin Receptor
In Vitro: IRL-1620 (TFA) is the most potent and specific ligand for the ETB receptor (KiETA/ KiETB=120,000) as judged by the Ki values for ETA (19 μM) and ETB (16 PM) receptors. IRL-1620 (TFA) is 60 times more selective for the ETB receptor than ET-3 (KiETA/ KiETB=1,900).
In Vivo: IRL-1620 (TFA) (1-100 nM) induces contractions of the guinea pig trachea. The effective concentration that produces 30 % of 60 mM KCI-induced contraction is estimated to be 28 nM for IRL-1620. IRL-1620 (TFA) (1-100 nM) increases cytosolic Ca2+ in the vascular endothelium ([Ca]E) with little effect on resting muscle tone, and relaxes the norepinephrine-stimulated tone with an increase in [Ca]E, in rat aorta,. IRL-1620 (TFA) improves both acquisition (learning) and retention (memory) on the water maze task and enhances angiogenic and neurogenic remodeling. Rats treated with IRL-1620 significantly reduces the cognitive impairment induced by Aβ. IRL-1620 treatment enhances the number of blood vessels labeled with VEGF compared to vehicle treatment.
相关产品:Bioactive Compound Library Plus | Peptide Library | BQ-788 | [Asn18] Endothelin-1, human | TBC3711 | BQ-3020 TFA | Sparsentan | [Lys4] Sarafotoxin S6c | Nebentan potassium | Bosentan | Endothelin 1 (swine, human) (TFA) | Ambrisentan | Ro 46-2005 | [Ala2] Endothelin-3, human | ZD-1611 | PD-159020 | Aminaftone | A-192621 | Macitentan | Sulfisoxazole | Endothelin-3, human, mouse, rabbit, rat TFA | IRL 2500 | Carperitide acetate | Atrial Natriuretic Peptide (ANP) (1-28), rat TFA | ACT-373898 | Kendomycin | Zibotentan | BQ-123 TFA
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