IRL-1620 TFA

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IRL-1620 TFA

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
500 μg	电议
1mg	电议
5mg	电议
10mg	电议
50mg	电议

产品介绍

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

生物活性

IRL-1620 (TFA) is a potent and selectiveendothelin receptortype B (ETB)agonist with aK_iof 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 (K_iETA/ K_iETB=120,000) as judged by the K_ivalues 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 (K_iETA/ K_iETB=1,900)^[1].

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].

分子量

1934.97

性状

Solid

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	-80°C	2 years
	-20°C	1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据

In Vitro:

DMSO : 50 mg/mL(25.84 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。