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IRL-1620 acetate is an effective and selective agonist of Endothelin B receptor (ETB) with a Ki of 16 pM which is more selective than ETA with a Ki of 19 μM.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $189 | In Stock | |
5 mg | $469 | In Stock | |
10 mg | $687 | In Stock | |
25 mg | $1,080 | In Stock | |
50 mg | $1,450 | In Stock | |
100 mg | $1,960 | In Stock |
Description | IRL-1620 acetate is an effective and selective agonist of Endothelin B receptor (ETB) with a Ki of 16 pM which is more selective than ETA with a Ki of 19 μM. |
Targets&IC50 | ETB receptor:16 pM(Ki), ETA receptor:19 μM(Ki) |
In vitro | IRL-1620 acetate is 60 times more selective for the ETB receptor than ET-3 (KiETA/ KiETB=1900)[3]. |
In vivo | IRL-1620 acetate improves both acquisition (learning) and retention (memory) on the water maze task and enhances angiogenic and neurogenic remodeling. Rats treated with IRL-1620 acetate significantly reduces the cognitive impairment induced by Aβ. IRL-1620 acetate treatment enhances the number of blood vessels labeled with VEGF compared to vehicle treatment[1]. IRL-1620 acetate, restores analgesic tolerance to morphine and oxycodone, but it does not affect morphine and oxycodone induced decrease in NGF/PI3K expression. IRL-1620 acetate attenuates opioid tolerance without the involvement of NGF/PI3K pathway[2]. IRL-1620 acetate (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[3]. IRL-1620 acetate (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[3]. |
Alias | IRL-1620 acetate(142569-99-1 free base) |
Molecular Weight | 1881 |
Formula | C88H121N17O29 |
Smiles | CC(O)=O.O=C(O)[C@H](CC1=CNC2=C1C=CC=C2)NC([C@H]([C@@H](C)CC)NC([C@H]([C@@H](C)CC)NC([C@H](CC(O)=O)NC([C@H](CC(C)C)NC([C@H](CC3=CNC=N3)NC([C@H](C)NC([C@H](CC4=CC=CC=C4)NC([C@H](CC5=CC=C(O)C=C5)NC([C@H](C(C)C)NC([C@H](C)NC([C@H](CCC(O)=O)NC([C@H](CCC(O)=O)NC([C@H](CC(O)=O)NC(CCC(O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O |
Relative Density. | no data available |
Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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