CS-2758 CAS#: 870544-59-5

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CS-2758

生物活性靶点体外研究体内研究 用途与合成方法 MSDS CS-2758价格(试剂级) 上下游产品信息

中文名称	CS-2758
中文同义词	化合物BPTU;BPTU游离态;BPTU,P2Y1别构拮抗剂;1-(2-(2-(叔丁基)苯氧基)吡啶-3-基)-3-(4-(三氟甲氧基)苯基)脲
英文名称	Urea, N-[2-[2-(1,1-diMethylethyl)phenoxy]-3-pyridinyl]-N'-[4-(trifluoroMethoxy)phenyl]-
英文同义词	Urea, N-[2-[2-(1,1-diMethylethyl)phenoxy]-3-pyridinyl]-N'-[4-(trifluoroMethoxy)phenyl]-;BPTU;1-(2-(2-(tert-butyl)phenoxy)pyridin-3-yl)-3-(4-(trifluoromethoxy)phenyl)urea;N-[2-[2-(1,1-Dimethylethyl)phenoxy]-3-pyridinyl]-N'-[4-(trifluoromethoxy)phenyl]urea;CS-2758;BMS-646786;BPTU,antithrombotic,thrombosis,BMS 646786,P2Y Receptor,inhibit,BMS646786,Inhibitor;Urea, N-[2-[2-(1,1-diMethylethyl)phenoxy]-3-pyridinyl]-N'-[4-(trifluoroMethoxy)phenyl]-
CAS号	870544-59-5
分子式	C23H22F3N3O3
分子量	445.43
EINECS号
相关类别	API
Mol文件	870544-59-5.mol
结构式

CS-2758 性质

CS-2758 用途与合成方法

生物活性

BPTU (BMS-646786) 是一种非核苷酸类 P2Y1 受体变构拮抗剂，具有抗血栓活性。BPTU 能够阻断位于胃肠道神经肌肉接头的 P2Y1 受体。

靶点

P2Y     ₁  

体外研究

BPTU blocks the supramaximal fast inhibitory junction potentials (fIJP) in a concentration-dependent manner both in the rat and mouse colon. The EC     ₅₀    of BPTU is approximately 0.3 μM and 0.06 μM for the rat and mouse colon, respectively. In the rat colon, addition of the P2Y agonist ADPβS at 10 μM significantly reduces spontaneous contractions to a 43.2±13.4% (N=5) (P=0.0002), and this reduction is blocked by 15 min incubation with BPTU at a concentration of 3 μM (93.3±5.1%). Similar results are obtained in the murine colon where ADPβS at 10 μM reduces the area under the curve (AUC) of contractions to a 15.8±5.1% (N=4) (P<0.0001) and its effect is reversed with BPTU at 3 μM (82.7±3.6%). Addition of MRS2365, a selective P2Y1 agonist, at a concentration of 5 μM significantly reduces spontaneous contractions to a 21.2±4.8% (N=5) (P=0.0002) in the murine colon, and this reduction is blocked by 15 min incubation with BPTU at a concentration of 3 μM (93.1±3.8%). The blockage of the MRS2365-induced response by BPTU at 3 μM also occurs in control conditions (N=5) (10.2±5.5% vs. 86.7±5.0%).

体内研究

Uptake of BPTU from the peritoneal cavity is relatively rapid. Blood boron levels are maximal within 1 h after administration. After only 1 h, a boron tumor-to-blood ratio above 1 is found for BPTU in pigmented tumors, which is indicative of drug retention. This is not seen in the non-pigmented tumor variant, in which tumor boron levels closely follow blood levels. Up to 24 h, Borocaptate sodium (BSH) exhibits no selective retention in either tumor, but achieves higher maximum tumor boron concentrations than BPTU as a result of the administration of higher amounts of boron. During the tissue distribution phase, liver-to-kidney boron concentration ratios range from 2 to 4 for BSH and from 0.5 to 1 for BPTU.

安全信息

MSDS信息

CS-2758 价格(试剂级)

CS-2758 上下游产品信息