IRL-1620 TFA高效且选择性的内皮素B受体（ETB；Ki=16pM）激动剂。
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.
IRL-1620 TFA高效且选择性的内皮素B受体（ETB；Ki=16pM）激动剂。IRL-1620 TFA通过激活血管内皮上的ETB受体，刺激血管生成和神经再生[1-2]。IRL-1620 TFA可用于急性缺血性脑卒中和阿尔茨海默病等相关研究[3-4]。
在体外，IRL-1620 TFA（100-1000nM）刺激ND7/104和HEK 293T细胞。在实时监测条件下，IRL-1620 TFA未引起细胞内钙浓度（[Ca2+]in）的升高[5]。IRL-1620 TFA（0.1-10nM）孵育人脐静脉内皮细胞（HUVEC）。在实时监测条件下，IRL-1620 TFA促进了NO的剂量依赖性产生[6]。
在体内，IRL-1620 TFA（3nmol/kg）与聚乙二醇化脂质体共同静脉注射于接种了CT-26结肠癌的BALB/c小鼠，在注射后48小时检测。IRL-1620 TFA显著增强了脂质体在肿瘤中的积累[7]。IRL-1620 TFA（5μg/kg）于大鼠接受大脑中动脉闭塞（MCAO）后4、6和8小时静脉注射，提高了大鼠的存活率，并显著改善了神经功能缺损及运动功能[8]。
| 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 | ||
| 分子式 | C88H118F3N17O29 | 分子量 | 1934.97 |
| 溶解度 | DMSO : 50 mg/mL (25.84 mM; Need ultrasonic) | 储存条件 | -20°C, protect from light |
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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 |
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