GLPBio

IRL-1620 TFA

Catalog No.: GC38641Purity:>95.00%
COASDSData Sheet
IRL-1620 TFA is a potent and selective endothelin B receptor (ETB) agonist (Ki=16pM).

Products are for research use only. Not for human use. We do not sell to patients.

IRL-1620 TFA
500μgIn Stock
$70.00
1
1mgIn Stock
$119.00
1
5mgIn Stock
$252.00
1
10mgIn Stock
$391.00
1
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Description

IRL-1620 TFA is a potent and selective endothelin B receptor (ETB) agonist (Ki=16pM). IRL-1620 TFA stimulates angiogenesis and neuroregeneration by activating ETB receptors on the vascular endothelium[1-2]. IRL-1620 TFA can be used in research related to acute ischemic stroke and Alzheimer's disease[3-4].

In vitro, IRL-1620 TFA (100-1000nM) stimulated ND7/104 and HEK 293T cells. Under real-time monitoring conditions, IRL-1620 TFA did not cause an increase in intracellular calcium concentration ([Ca2+]in)[5]. IRL-1620 TFA (0.1-10nM) was incubated with human umbilical vein endothelial cells (HUVEC). Under real-time monitoring conditions, IRL-1620 TFA promoted a dose-dependent production of NO[6].

In vivo, IRL-1620 TFA (3nmol/kg) was co-administered intravenously with PEGylated liposomes to BALB/c mice inoculated with CT-26 colon carcinoma, and detection was performed 48 hours after injection. IRL-1620 TFA significantly enhanced the accumulation of liposomes in the tumor[7]. IRL-1620 TFA (5µg/kg) was administered intravenously to rats at 4, 6, and 8 hours after middle cerebral artery occlusion (MCAO). IRL-1620 TFA improved the survival rate of the rats and significantly ameliorated neurological deficits and motor function[8].

References:
[1] Takai M, Umemura I, Yamasaki K, et al. A potent and specific agonist, Suc-[Glu9,Ala11,15]-endothelin-1(8-21), IRL 1620, for the ETB receptor. Biochem Biophys Res Commun. 1992 Apr 30;184(2):953-9.
[2] Gulati A, Hornick MG, Briyal S, et al. A novel neuroregenerative approach using ET(B) receptor agonist, IRL-1620 TFA, to treat CNS disorders. Physiol Res. 2018 Jun 27;67(Suppl 1):S95-S113.
[3] Ramos MD, Briyal S, Prazad P, et al. Neuroprotective Effect of Sovateltide (IRL 1620, PMZ 1620) in a Neonatal Rat Model of Hypoxic-Ischemic Encephalopathy. Neuroscience. 2022 Jan 1;480:194-202.
[4] Keam SJ. Sovateltide: First Approval. Drugs. 2023 Sep;83(13):1239-1244.
[5] Montmayeur JP, Barr TP, Kam SA, et al. ET-1 induced Elevation of intracellular calcium in clonal neuronal and embryonic kidney cells involves endogenous endothelin-A receptors linked to phospholipase C through Gα(q/11). Pharmacol Res. 2011 Sep;64(3):258-67.
[6] Tsukahara H, Ende H, Magazine HI, et al. Molecular and functional characterization of the non-isopeptide-selective ETB receptor in endothelial cells. Receptor coupling to nitric oxide synthase. J Biol Chem. 1994 Aug 26;269(34):21778-85.
[7] Feng H, Nam LT, Yoshikawa T, et al. Effect of an Endothelin B Receptor Agonist on the Tumor Accumulation of Nanocarriers. Biol Pharm Bull. 2020;43(9):1301-1305.
[8] Ranjan AK, Briyal S, Gulati A. Sovateltide (IRL-1620 TFA) activates neuronal differentiation and prevents mitochondrial dysfunction in adult mammalian brains following stroke. Sci Rep. 2020 Jul 29;10(1):12737.

Protocol

Cell experiment [1]:

Cell lines

Human umbilical vein endothelial cells (HUVEC)

Preparation Method

HUVEC were cultured in M199 medium supplemented with heparin, endothelial cell growth factor, and 10% fetal bovine serum. For nitric oxide (NO) release assays, cells were preincubated in Krebs-Ringer buffer, and a precalibrated amperometric NO-selective electrode was introduced to continuously monitor baseline NO release. After reaching steady state, IRL-1620 TFA (0.1-10nM) were added to the incubation medium, and NO release was recorded.

Reaction Conditions

0.1–10nM; NO release was measured immediately.

Applications

IRL-1620 TFA (0.1–10nM) induced an immediate, dose‑dependent, and long‑lasting NO generation in HUVEC.

Animal experiment [2]:

Animal models

Adult male Sprague-Dawley rats (weight range 350-390g)

Preparation Method

Rats were subjected to permanent middle cerebral artery occlusion (MCAO) to induce focal cerebral ischemia. IRL-1620 TFA (5µg/kg) was administered intravenously into the tail vein at 4, 6, and 8 hours post MCAO.

Dosage form

5µg/kg; i.p.; administered at 4, 6, and 8 hours post MCAO.

Applications

IRL-1620 TFA treatment improved survival rate, significantly reduced neurological deficit scores, and improved motor functions at 24h and day 7 post MCAO.

References:
[1] Tsukahara H, Ende H, Magazine HI, et al. Molecular and functional characterization of the non-isopeptide-selective ETB receptor in endothelial cells. Receptor coupling to nitric oxide synthase. J Biol Chem. 1994 Aug 26;269(34):21778-85.
[2] Ranjan AK, Briyal S, Gulati A. Sovateltide (IRL-1620 TFA) activates neuronal differentiation and prevents mitochondrial dysfunction in adult mammalian brains following stroke. Sci Rep. 2020 Jul 29;10(1):12737.

Product Documents

Purity:>95.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

Molecular Formula
C88H118F3N17O29
Molecular Weight
1934.97
Solubility
DMSO : 50 mg/mL (25.84 mM; Need ultrasonic)
Storage
-20°C, protect from light
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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