BPTU - CAS:870544-59-5 - KKL Med Inc.

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BPTU (Synonyms:BMS-646786)

目录号 : KM8746 CAS No. : 870544-59-5 纯度 : 98%

Data Sheet 产品使用指南

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。

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生物活性

BPTU (BMS-646786) is a non-nucleotide P2Y₁ receptor allosteric antagonist with antithrombotic activity. BPTU is able to block the P2Y1 receptor located at the neuromuscular junction of the gastrointestinal tract.

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 0.3 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.

分子式

C₂₃H₂₂F₃N₃O₃

分子量

445.43

CAS号

870544-59-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 33.3 mg/mL (74.76 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2450 mL	11.2251 mL	22.4502 mL
5 mM	0.4490 mL	2.2450 mL	4.4900 mL
10 mM	0.2245 mL	1.1225 mL	2.2450 mL

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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.61 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.61 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。