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BPO-27 racemate Sale

目录号 : GC30537

BPO-27racemate是有效的CFTR抑制剂,IC50值为8nM。

BPO-27 racemate Chemical Structure

Cas No.:1314873-02-3

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10mM (in 1mL DMSO)
¥2,153.00
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1mg
¥765.00
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5mg
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10mg
¥3,240.00
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50mg
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100mg
¥10,708.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment:

Whole-cell recordings are done on CFTR-expressing CHO-K1 cells. After establishing the whole-cell configuration, BPO-27 is added for 5 minutes, and then CFTR is activated by the addition of forskolin (10 μM) in the continued presence of BPO-27 (0.5 or 1 μM). Whole-cell currents are elicited by applying hyperpolarizing and depolarizing voltage pulses from a holding potential of 0 mV to potentials between +80 and −80 mV in steps of 20 mV. Recordings are made at room temperature using an Axopatch-200B. Currents are digitized with a Digidata 1440A converter and filtered at 5 kHz[2].

Animal experiment:

Mice: (R)-BPO-27 is formulated at 1 mg/mL in 5% DMSO, 2.5% Tween-80 and 2.5% PEG400 in water. Male mice in a CD1 genetic background are administered 300 μL of the (R)-BPO-27 formulation by intraperitoneal injection. At specified times, blood samples are collected by eye bleed. At 4 h, kidneys are removed following renal arterial perfusion with PBS. Kidneys are weighed, mixed with acetic acid and homogenized for analysis[1].

References:

[1]. Snyder DS, et al. Absolute Configuration And Biological Properties of Enantiomers of CFTR Inhibitor BPO-27. ACS Med Chem Lett. 2013 May 9;4(5):456-459.
[2]. Kim Y, et al. Benzopyrimido-pyrrolo-oxazine-dione (R)-BPO-27 Inhibits CFTR Chloride Channel Gating by Competition with ATP. Mol Pharmacol. 2015 Oct;88(4):689-96.

产品描述

BPO-27 racemate is a potent CFTR inhibitor with an IC50 of 8 nM.

The benzopyrimido-pyrrolo-oxazinedione BPO-27 is an analogue of PPQ-102, which inhibits CFTR with an IC50 of 8 nM. The R enantiomer of BPO-27 inhibits CFTR chloride conductance with an IC50 of 4 nM, while S enantiomer is inactive. In vitro metabolic stability in hepatic microsomes shows both enantiomers as stable, with less than 5% metabolism in 4 h[1]. (R)-BPO-27 binds near the canonical ATP binding site. Whole-cell patch-clamp studies shows linear CFTR currents with a voltage-independent (R)-BPO-27 block mechanism. At a concentration of (R)-BPO-27 that inhibits CFTR chloride current by 50%, the EC50 for ATP activation of CFTR increases from 0.27 to 1.77 mM[2].

Following bolus interperitoneal administration in mice, serum (R)-1 decays with t1/2 ≈ 1.6 h and gives sustained therapeutic concentrations in kidney[1].

[1]. Snyder DS, et al. Absolute Configuration And Biological Properties of Enantiomers of CFTR Inhibitor BPO-27. ACS Med Chem Lett. 2013 May 9;4(5):456-459. [2]. Kim Y, et al. Benzopyrimido-pyrrolo-oxazine-dione (R)-BPO-27 Inhibits CFTR Chloride Channel Gating by Competition with ATP. Mol Pharmacol. 2015 Oct;88(4):689-96.

Chemical Properties

Cas No. 1314873-02-3 SDF
Canonical SMILES O=C(C1=CC=C(OC(C2=CC=C(Br)O2)C3=C(N(C)C4=O)C(C(N4C)=O)=C(C5=CC=CC=C5)N36)C6=C1)O
分子式 C26H18BrN3O6 分子量 548.34
溶解度 DMSO : 6 mg/mL (10.94 mM) 储存条件 Store at -20°C
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储备液的保存方式和期限:-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。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.8237 mL 9.1184 mL 18.2369 mL
5 mM 0.3647 mL 1.8237 mL 3.6474 mL
10 mM 0.1824 mL 0.9118 mL 1.8237 mL
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