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A-71623

CCK1激动剂,A-71623是CCKA受体的选择性激动剂，对豚鼠胰腺的IC50值为3.7 nM[1,2]。CCKA受体属于大脑中胆囊收缩素（CCK）受体的亚型。CCK是一种神经肽，在整个中枢神经系统中广泛分布。CCK可以作为正常和异常脑中的神经递质。CCK受体在大脑以两种形式存在，CCK受体的另一亚型是CCKB亚型[1]

目录号: PC11236 纯度: ≥98%

CAS No. :130408-77-4

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中文名称

A-71623

英文名称

A-71623

英文别名

L-Phenylalaninamide,N-[(1,1-dimethylethoxy)carbonyl]-L-tryptophyl-N6-[[(2-methylphenyl)amino]carbonyl]-L-lysyl-L-a-aspartyl-Na-methyl-;A 71623;A-71623;Boc-Trp-Lys(Tac)-Asp-N(Me)Phe-NH2;L-Phenylalaninamide,N-[(1,1-dimethylethoxy)carbonyl]-L-tryptophyl-N6-[[(2-methylphenyl)amino]c...;L-Phenylalaninamide,N-[(1,1-dimethylethoxy)carbonyl]-L-tryptophyl-N6-[[(2-methylphenyl)amino]carbonyl]-L-lysyl-L-a-aspartyl-N;Boc-Trp-His-OMe;N-[(1,1-DiMethylethoxy)carbonyl]-L-tryptophyl-N6-[[(2-Methylphenyl)aMino]carbonyl]-L-lysyl-L-α-aspartyl-Nα-Methyl-L-phenylalaninaMide;N-Boc-L-Trp-[(2S)-2-Amino*-6-[3-(2-methylphenyl)ureido]hexanoyl]-L-Asp-N-methyl-L-Phe-NH2;N-[(1,1-DIMETHYLETHOXY)CARBONYL]-L-TRYPTOPHYL-N6-[[(2-METHYLPHENYL)AMINO]CARBONYL]-L-LYSYL-L-ALPHA-ASPARTYL-NA-METHYL-L-PHENYLALANINAMIDE

Cas No.

130408-77-4

分子式

C₄₄H₅₆N₈O₉

分子量

840.96

包装储存

Sealed storage, away from moisture and light, under nitrogen

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, under nitrogen)

生物活性

A71623, a CCK-4-based peptide, is a potent and highly selective CCK-A full agonist. The IC₅₀s for A-71623 are 3.7 nM in guinea pig pancreas (CCK-A) and 4500 nM in cerebral cortex (CCK-B) in radioligand binding assays, respectively.

性状

Solid

IC50 & Target[1][2]

CCKAR

体外研究(In Vitro)

In guinea pig gastric glands, the affinities of A-71623 for the cholecystokinin (CCK)-B/gastrin receptor were 11 μM.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

A71623 (A-63387; i.c.v., but not i.p., injections) reduces food intakes and suppresses intakes of a liquid diet in both deprived and sated rats.
A71623 dampens Purkinje neuron pathology and associates deficits in motor performance in Pcp2-ATXN1[30Q]D776;Cck and Pcp2-AXTN1[82Q] mice.
A71623 improves motor performance of Pcp2-ATXN2[127Q] SCA2 mice.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Adult male, Sprague-Dawley rats
Dosage:	5 μL
Administration:	Intracerebroventricular (i.c.v) administration, A-71623 was infused using a 28 gauge injection cannula in a volume of 5uL over 60 s
Result:	Reduced food intakes and suppressed intakes of a liquid diet.

Animal Model:	ATXN1[30Q]-D776, ATXN1[82Q]-D776, ATXN2[127Q], and WT/FVB/NJ mice
Dosage:	0.02 mg/kg/day
Administration:	Osmotic minipumps containing either A71623 (0.02mg/kg/day) were implanted intraperitoneally (i.p.)
Result:	Treatment dampened Purkinje neuron pathology in ATXN1[30Q]D776;Cck mice and ATXN1[82Q] mice. Improved motor performance in ATXN2[127Q] mice.

运输条件

Room temperature or refrigerated transportation.

储存方式

Sealed storage, away from moisture and light, under nitrogen

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, under nitrogen)

参考文献

[1]. C W Lin, et al. Characterization of two novel cholecystokinin tetrapeptide (30-33) analogues, A-71623 and A-70874, that exhibit high potency and selectivity for cholecystokinin-A receptors. Mol Pharmacol. 1991 Mar;39(3):346-51. [Information]

[2]. K E Asin, et al. Effects of selective CCK receptor agonists on food intake after central or peripheral administration in rats. Brain Res. 1992 Jan 31;571(1):169-74. [Information]

[3]. Emily A.L. Wozniak, et al. Cholecystokinin 1 Receptor (Cck1R) Activates mTORC1 signaling and is Protective to Purkinje cells in SCA Mice. ?bioRxiv. February 17, 2021.

溶解度数据

体外研究:

DMSO : 50 mg/mL (59.46 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.1891 mL	5.9456 mL	11.8912 mL
5 mM	0.2378 mL	1.1891 mL	2.3782 mL
10 mM	0.1189 mL	0.5946 mL	1.1891 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, under nitrogen)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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