MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

IRL-1620 TFA

CAS No. :

MCE 站：IRL-1620 TFA

产品活性：IRL-1620 (TFA) 是选择性的内啡肽受体 (endothelin receptor) B 型激动剂，K_i 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 (K_iETA/ K_iETB=120,000) as judged by the K_i 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 (K_iETA/ K_iETB=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.
IRL-1620 (TFA), restores analgesic tolerance to morphine ａnd oxycodone, but it does not affect morphine ａnd oxycodone induced decrease in NGF/PI3K expression. IRL-1620 attenuates opioid tolerance without the involvement of NGF/PI3K pathway.

相关产品：Bioactive Compound Library Plus  |  Endothelin 1 (swine, human)  |  BQ-788 sodium salt  |  Bosentan  |  BQ-123  |  Atrasentan hydrochloride  |  Ambrisentan  |  Sparsentan  |  Atrial Natriuretic Peptide (ANP) (1-28), human, porcine Acetate  |  Sulfisoxazole  |  Atrial Natriuretic Peptide (ANP) (1-28), rat  |  Avosentan  |  Sitaxsentan sodium  |  Zibotentan  |  Darusentan  |  A-192621  |  BQ-3020 TFA  |  IRL 2500  |  IRL-1620  |  Nebentan  |  Tezosentan  |  ABT-546  |  Aminaftone  |  Aprocitentan D4  |  BMS-248360