MRS-1191

MRS-1191用途

MRS-1191 是一种有效的选择性的 A3 腺苷受体 (A3 adenosine receptor ) 拮抗剂,其 KB 值为 92 nM,对人 A3 受体的 Ki 值为 31.4 nM,对 CHO 细胞的 IC50 值为 120 nM。

MRS-1191名称

[ CAS 号 ]:
185222-90-6

[ 中文名 ]:
3-苄基 5-乙基 6-甲基-2-苯基-4-(苯基炔基)-1,4-二氢吡啶-3,5-二羧酸酯

[ 英文名 ]:
MRS 1191

[英文别名 ]:

mrs1191

MRS-1191生物活性

[ 描述 ]:

MRS-1191 是一种有效的选择性的 A3 腺苷受体 (A3 adenosine receptor ) 拮抗剂,其 KB 值为 92 nM,对人 A3 受体的 Ki 值为 31.4 nM,对 CHO 细胞的 IC50 值为 120 nM。

[ 靶点 ]

Ki: 31.4 nM (human A3 adenosine receptor)[1]

[体外研究]

推定的MRS-1191的A3腺苷受体拮抗剂的作用在受体结合和功能测定中表征。发现MRS-1191在使用激动剂放射性配体[125 I]AB-MECA(N6-(4-氨基-3-碘苯基)腺苷-5'-N-甲基脲酰胺)在克隆的人脑A3受体上的饱和结合研究中具有竞争性。在HEK-293细胞中表达。在由激动剂诱导的腺苷酸环化酶抑制和[35S]鸟苷5'-O-(3-硫代三磷酸)([35S]GTP-γ-S)与相关G蛋白结合的刺激组成的功能测定中证明了拮抗作用。。KB值为92 nM的MRS-1191被证明对人A3受体与人A1受体介导的对腺苷酸环化酶的作用具有高选择性[1]。

[参考文献]

[1]. Jacobson KA, et al. Pharmacological characterization of novel A3 adenosine receptor-selective antagonists. Neuropharmacology. 1997 Sep;36(9):1157-65.

MRS-1191物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
643.1±55.0 °C at 760 mmHg

[ 熔点 ]:
155 - 156 ℃

[ 分子式 ]:
C₃₁H₂₇NO₄

[ 分子量 ]:
477.550

[ 闪点 ]:
342.7±31.5 °C

[ 精确质量 ]:
477.194000

[ PSA ]:
64.63000

[ LogP ]:
7.16

[ 外观性状 ]:
白色固体

[ 蒸汽压 ]:
0.0±1.9 mmHg at 25°C

[ 折射率 ]:
1.639

[ 储存条件 ]:
-20 °C

MRS-1191MSDS

详细MSDS(安全技术说明书)

MRS-1191安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

MRS-1191文献

ATP releases ATP or other nucleotides from human peripheral blood leukocytes through purinergic P2 receptors.

Life Sci. 145 , 85-92, (2016)

Almost every eukaryotic cell releases ATP under certain conditions. The idea that ATP induces the release of ATP has been scantly investigated.We explored this possibility by assessing the rate of exo...

The infarct-sparing effect of IB-MECA against myocardial ischemia/reperfusion injury in mice is mediated by sequential activation of adenosine A3 and A 2A receptors.

Basic Res. Cardiol. 110(2) , 16, (2015)

Conflicting results exist regarding the role of A3 adenosine receptors (A3ARs) in mediating cardioprotection during reperfusion following myocardial infarction. We hypothesized that the effects of the...

Pharmacological characterization of novel A3 adenosine receptor-selective antagonists.

Neuropharmacology 36 , 1157-1165, (1997)

The effects of putative A3 adenosine receptor antagonists of three diverse chemical classes (the flavonoid MRS 1067, the 6-phenyl-1,4-dihydropyridines MRS 1097 and MRS 1191, and the triazoloquinazolin...

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