(R)-BPO-27

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(R)-BPO-27

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1415390-47-4

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
1mg	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品介绍

(R)-BPO-27 是 BPO-27 的 R 型对映体，是一种有效的、具有口服活性的、ATP 竞争性的CFTR抑制剂，具有IC₅₀的 4 nM。

生物活性

(R)-BPO-27, the R enantiomer of BPO-27, is a potent, orally active and ATP-competitiveCFTR inhibitor with an IC₅₀of 4 nM.

IC₅₀& Target

IC50: 4 nM^[1]

体外研究
(In Vitro)

(R)-BPO-27 exhibits a dose-response inhibition and inhibits the CFTR current by 50% at 0.53 nM in HEK-293T cells. (R)-BPO-27 acts from the cytoplasmic side and has low membrane permeability^[1].
(R)-BPO-27 reduces the channel open probability (NPo) from 0.29 to 0.08, modestly reduces in mean channel open time, and strongly increases mean channel closed time in HEK-293T cells expressing human wild-type CFT in a single-channel patch-clamp experiment. Meanwhile, (S)-BPO-27 does not affect any of these parameters^[1].
(R)-BPO-27 is applied directly to the cytoplasmic membrane surface and stabilizes the CFTR channel closed state with an IC₅₀of 600 pM in Single-channel electrophysiology assay^[2].
(R)-BPO-27 (10 μM, 10 min pretreatment) inhibits Cl^- current with apparent IC₅₀ values of 5 and 10 nM for CPT-cAMP and 8-Br-cGMP, respectively, in CFTR-expressing FRT cells after CFTR stimulation by cAMP agonist. the IC₅₀of 4 nM for inhibition of forskolin-stimulated CFTR Cl^- current in FRT cells^[3].

体内研究
(In Vivo)

(R)-BPO-27 (interperitoneal administration; 10 mg/kg) decays with t_1/2≈1.6 h and gives sustained therapeutic concentrations in kidney in a PK study^[1].
(R)-BPO-27 (intraperitoneal injection; 5 mg/kg; 30 min before abdominal surgery) prevents fluid accumulation in closed midjejunal loops produced by cholera toxin, giving an intestinal loop weight/length ratio similar to that in PBS-injected loops. This effect is dose-dependently and the IC₅₀value is 0.1 mg/kg^[3].
(R)-BPO-27 (intraperitoneal injection or oral administration; 5 mg/kg) shows a slow (R)-BPO-27 metabolism and produces sustained serum (R)-BPO-27 levels for at least 4 h. The AUC analysis gave an oral bioavailability of ~94% for (R)-BPO-27 in mouse pharmacokinetics and toxicity study^[3].

Animal Model:	Female CD1 mice (age 8–10 wk)^[3]
Dosage:	0.05, 0.15, 0.5, 1.5, and 5 mg/kg
Administration:	Intraperitoneal injection; 5 mg/kg; 30 min before abdominal surgery
Result:	Exhibited apparent efficacy in mice models of cholera and traveler’s diarrhea.

分子量

548.34

性状

Solid

Formula

C₂₆H₁₈BrN₃O₆

CAS 号

1415390-47-4

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 : ≥ 14.28 mg/mL(26.04 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	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

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。