IRL-1620 TFA |
Catalog No.GC38641
One-Click Copy Product Info
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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.
Sample solution is provided at 25 µL, 10mM.
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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.
| 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: | |
| Cas No. | SDF | ||
| Formula | C88H118F3N17O29 | M.Wt | 1934.97 |
| Solubility | DMSO : 50 mg/mL (25.84 mM; Need ultrasonic) | Storage | -20°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 516.8 μL | 2.584 mL | 5.168 mL |
| 5 mM | 103.4 μL | 516.8 μL | 1.0336 mL |
| 10 mM | 51.7 μL | 258.4 μL | 516.8 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >95.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)