中文名称: BPTU 促销
英文名称: BPTU
CAS No: 870544-59-5
分子式: C23H22F3N3O3
分子量: 445.43
B10030 BPTU ≥98% (HPLC) (psaitong)
包装规格:
5mg 25mg 100mg in glass bottle
溶解性:
溶于DMSO(20mg/mL)
产品描述:

基本信息

产品编号:

B10030

产品名称:

BPTU

CAS:

870544-59-5

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C23H22F3N3O3

溶于液体

-80℃

6个月

分子量:

445.43

-20℃

1个月

化学名: 

N-[2-[2-(1,1-Dimethylethyl)phenoxy]-3-pyridinyl]-N′-[4-(trifluoromethoxy)phenyl]-urea BMS-646786

Solubility (25°C):

 

体外:

 

DMSO

 

Ethanol

'mg/mL

Water

 

体内(现配现用):

 

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

2.2450mL

11.2251mL

22.4502mL

5mM

0.4490mL

2.2450mL

4.4900mL

10mM

0.2245mL

1.1225mL

2.2450mL

 

生物活性

产品描述

一种抑制人血中ADP介导的血小板聚集的PY1嘌呤受体的强效特异性抑制剂。

靶点

P2Y1

 

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 EC50 of BPTU is approximately 0.3μM and 0.06μM for the rat and mouse colon,respectively. In the rat colon,addition of the P2Y agonist ADPβS at 10μM 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 3μM (93.3±5.1%).Similar results are obtained in the murine colon where ADPβS at 10μM 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 3μM (82.7±3.6%).Addition of MRS2365,a selective P2Y1 agonist,at a concentration of 5μM 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 3μM (93.1±3.8%).The blockage of the MRS2365-induced response by BPTU at 3μM 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 1h after administration.After only 1h,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 24h,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.

 

推荐实验方法(仅供参考)

细胞实验:

 

Electrophysiological experiments are performed with colonic rat and mouse strips.Inhibitory junction potentials (IJP) are elicited by electrical field stimulation (EFS) using two silver chloride plates placed 1.5 cm apart perpendicular to the longitudinal axis of the preparation.The protocol consists of single pulse trains of EFS (0.4 ms pulse duration) at increasing voltages (8,12,16,20,24,28,32,36,40 V).The voltage responsible for the supramaximal response is used to elicit single pulses during incubation with BPTU at increasing concentrations (1×10-8 M,1×10-7 M,3×10-7 M,1×10-6 M and 3×10-6 M).Another train of single pulses at increasing voltages is elicited after the highest dose of BPTU.The amplitude of the IJP (mV) is measured considering it as the difference between the maximal hyperpolarization and the resting membrane potential (RMP).

 

动物实验:

 

Mice are given BPTU intraperitoneally at doses of 3.15mg of boron per kg body weight.Injection volumes range from 0.25 to 0.5mL for both intravenous and intraperitoneal administrations.Six mice are not given any drug to allow measurement of boron background levels.Animals are killed with carbon dioxide 0.2,0.4,1,2,4,24 and 48h after drug administration and samples are taken from tumor,blood,skin,muscle,brain,kidneys and liver.Tumor tissue from mice bearing B16.013 tumor is checked by eye for the absence of pigmentation.BPTU is also given in a multiple dose scheme. Every 2h 0.4 to 0.5mL of the above-mentioned BPTU solution is given intraperitoneally (4×3.15mg/kg boron).Twenty-four hours after the last administration,the animals are sacrificed and samples are taken.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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