标签归档：irl

IRL-1620 TFA

发表于由

IRL-1620 TFA; 纯度: 95.46%

IRL-1620 (TFA) 是高效，选择性的内啡肽受体 (endothelin receptor) B 型激动剂，Ki 值为 16 pM。

IRL-1620 TFAamp;;

IRL-1620 TFA Chemical Structure

规格 价格 是否有货 数量
10;mM;*;1 mL in DMSO ￥25116 In-stock
500 μg ￥1000 In-stock
1 mg ￥1700 In-stock
5 mg ￥5900 In-stock
10 mg ; 询价 ;
50 mg ; 询价 ;

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IRL-1620 TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

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]
体外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

1934.97

Formula

C88H118F3N17O29
Sequence

{Suc}-Asp-Glu-Glu-Ala-Val-Tyr-Phe-Ala-His-Leu-Asp-Ile-Ile-Trp
Sequence Shortening

{Suc}-DEEAVYFAHLDIIW
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Sealed storage, away from moisture and light

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro:;

DMSO : 100 mg/mL (51.68 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (ultrasonic) (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.5168 mL 2.5840 mL 5.1680 mL
5 mM 0.1034 mL 0.5168 mL 1.0336 mL
10 mM 0.0517 mL 0.2584 mL 0.5168 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Takai M, 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]. Briyal S, et al. Stimulation of endothelin B receptors by IRL-1620 decreases the progression of Alzheimer’s disease. Neuroscience. 2015 Aug 20;301:1-11.

    [3]. Gulati S, et al. Attenuation of opioid tolerance by ETB receptor agonist, IRL-1620, is independent of an accompanied decrease in nerve growth factor in mice. Heliyon. 2017 Jun 7;3(6):e00317.