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

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

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IRL-1620 Chemical Structure

IRL-1620 Chemical Structure

CAS No. : 142569-99-1

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Other Forms of IRL-1620:

IRL-1620 Related Antibodies

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Description

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

IC50 & Target

ETB

 

In Vitro

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

IRL-1620 Related Antibodies
In Vivo

IRL-1620 (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 (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 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

1820.95

Formula

C86H117N17O27
CAS No.
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.
Purity & Documentation
References
Kinase Assay
[1]

The plasma membrane of porcine lung (2 ug of protein) is incubated at 37°C for 1 hr with 30 pM [125I]ET-1 or 10 pM [125I]ET-3 in the absence or presence of various amounts of nonlabeled ligands (IRL-1620) in a total volume of 1 mL of assay buffer. After the incubation, unbound [125I]ETs are separated and radioactivity in the membrane pellet is measured in an autogamma counter[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2][3]

Rats: Specific ETB receptor agonist, IRL-1620 (5 μg/kg) and specific ETB receptor antagonist, BQ788 (1 mg/kg) are administered intravenously (i.v.) on day 8. IRL-1620 is administered on day 8 three times at a dose of 5 μg/kg, i.v. at 2-h intervals between each injection[2].

Mice: Tolerance to morphine is induced using a 3-day cumulative dosing regimen. Morphine treatment schedule consisted of twice-daily s.c. injections of morphine for three days given at (i) 30 mg/kg (a.m.) and 45 mg/kg (p.m.) on day 1; (ii) 60 mg/kg (a.m.) and 90 mg/kg (p.m.) on day 2; and (iii) 120 mg/kg twice (a.m. and p.m.) on day 3. The IRL-1620 treatment schedule consists of three times-daily injections of IRL-1620 for two days given at 5 μg/kg, i.v. spaced apart every 2 h on days 1 and 3. At the end of the treatment schedule, a challenge dose of morphine (5 mg/kg, s.c.) is administered on day 4 to assess tolerance[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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IRL-1620 Related Classifications

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IRL-1620142569-99-1IRL1620IRL 1620Endothelin ReceptorInhibitorinhibitorinhibit

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HY-16465
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