264622-58-4|MRS 1754|CsnPharm

CAS No.: 264622-58-4

MRS 1754 Catalog No. CSN22988

Synonyms: MRS 1754

MRS 1754 is a selective adenosine A2B receptor antagonist with Ki of 1.97 nM for hA2B.

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400-920-2911

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实验方案

技术信息

生物活性

描述The A_2B adenosine receptor (AR) is a member of the P₁ family of seven-transmembrane ARs, and it couples to G_s to increase cAMP and G_q11 to increase (1,4,5)inositol triphosphate (IP₃)/diacylglycerol (DAG). MRS 1754 is a selective antagonist ligand of A_2BAR with K_i value of 1.97 nM^[1]. ³H-MRS 1754 was shown to bind with high affinity to a single class of binding sites in membranes of HEK-293 cells expressing the human A_2B receptor^[2]. Finally, MRS 1754 inhibited the NECA-induced Ca²⁺ responses and cAMP production in a concentration-dependent manner. Treatment of the T24 cell line for 4h with NECA resulted in an increase in interleukin-8 production which was sensitive to the adenosine A_2B antagonist MRS 1754^[3].
参考文献

[1] Kalla RV, Zablocki J, Tabrizi MA, Baraldi PG. Recent developments in A2B adenosine receptor ligands. Handb Exp Pharmacol. 2009;(193):99-122
[2] Ji X, Kim YC, Ahern DG, Linden J, Jacobson KA. ³HMRS 1754, a selective antagonist radioligand for A(2B) adenosine receptors. Biochem Pharmacol. 2001;61(6):657-663
[3] Phelps PT, Anthes JC, Correll CC. Characterization of adenosine receptors in the human bladder carcinoma T24 cell line. Eur J Pharmacol. 2006;536(1-2):28-37

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0554 mL
- 10.2770 mL
- 20.5540 mL
- 5 mM
- 0.4111 mL
- 2.0554 mL
- 4.1108 mL
- 10 mM
- 0.2055 mL
- 1.0277 mL
- 2.0554 mL

技术信息

CAS号

264622-58-4

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H26N6O4

运输

蓝冰

分子量

486.52

别名

MRS 1754

溶解度

DMSO	15.0 mg/mL (30.8 mM) warming
Water	Insoluble

动物实验配方

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