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MRS 1754

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Chemical Structure| 264622-58-4 同义名 : -
CAS号 : 264622-58-4
货号 : A540042
分子式 : C26H26N6O4
纯度 : 98%+
分子量 : 486.522
MDL号 : MFCD09971130
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 14 mg/mL(28.78 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The A2B adenosine receptor (AR) is a member of the P1 family of seven-transmembrane ARs, and it couples to Gs to increase cAMP and Gq11 to increase (1,4,5)inositol triphosphate (IP3)/diacylglycerol (DAG). MRS 1754 is a selective antagonist ligand of A2BAR with Ki 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 A2B 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 A2B antagonist MRS 1754[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.06mL

0.41mL

0.21mL

10.28mL

2.06mL

1.03mL

20.55mL

4.11mL

2.06mL
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