1. GPCR/G Protein
  2. Endothelin Receptor
  3. IRL-1620 TFA

IRL-1620 TFA 

Cat. No.: HY-16465A
Handling Instructions

IRL-1620 (TFA) is a potent and selective endothelin receptor type B (ETB) agonist with a Ki of 16 pM.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

IRL-1620 TFA Chemical Structure

IRL-1620 TFA Chemical Structure

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 3014 In-stock
Estimated Time of Arrival: December 31
500 μg USD 120 In-stock
Estimated Time of Arrival: December 31
1 mg USD 204 In-stock
Estimated Time of Arrival: December 31
5 mg USD 708 In-stock
Estimated Time of Arrival: December 31
10 mg   Get quote  
50 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

IRL-1620 (TFA) is a potent and selective endothelin receptor type B (ETB) agonist with a Ki of 16 pM[1].

IC50 & Target

IC50: 16 pM (Endothelin receptor B); 19 μM (Endothelin receptor A)[1]

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[1].
IRL-1620 (TFA) is 60 times more selective for the ETB receptor than ET-3 (KiETA/ KiETB=1,900)[1].

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[1].
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,[1].
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[2].
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[3].

Molecular Weight

1934.97

Formula

C₈₈H₁₁₈F₃N₁₇O₂₉

Sequence

Suc-Asp-Glu-Glu-Ala-Val-Tyr-Phe-Ala-His-Leu-Asp-Ile-Ile-Trp

Sequence Shortening

Suc-DEEAVYFAHLDIIW

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

IRL-1620IRL1620IRL 1620Endothelin ReceptorInhibitorinhibitorinhibit

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IRL-1620 TFA
Cat. No.:
HY-16465A
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