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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。
(R)-BPO-27图片
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 t1/2≈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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM1.8237 mL9.1184 mL18.2369 mL
5 mM0.3647 mL1.8237 mL3.6474 mL
10 mM0.1824 mL0.9118 mL1.8237 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。