产品
编 号：F596645
分子式：C26H18BrN3O6
分子量：548.34
分子式：C26H18BrN3O6
分子量：548.34
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
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5mg
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10mg
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结构图
CAS No: 1415390-47-4
产品详情
生物活性：
(R)-BPO-27, the R enantiomer of BPO-27, is a potent, orally active and ATP-competitive CFTR?inhibitor with an?IC50 of 4 nM.
体内研究：
(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.(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 IC50 value is 0.1 mg/kg.(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.Animal Model:Female CD1 mice (age 8–10 wk)
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.
体外研究：
(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.(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.(R)-BPO-27 is applied directly to the cytoplasmic membrane surface and stabilizes the CFTR channel closed state with an IC50 of 600 pM in Single-channel electrophysiology assay.(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 IC50 of 4 nM for inhibition of forskolin-stimulated CFTR Cl-?current in FRT cells.
(R)-BPO-27, the R enantiomer of BPO-27, is a potent, orally active and ATP-competitive CFTR?inhibitor with an?IC50 of 4 nM.
体内研究：
(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.(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 IC50 value is 0.1 mg/kg.(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.Animal Model:Female CD1 mice (age 8–10 wk)
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.
体外研究：
(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.(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.(R)-BPO-27 is applied directly to the cytoplasmic membrane surface and stabilizes the CFTR channel closed state with an IC50 of 600 pM in Single-channel electrophysiology assay.(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 IC50 of 4 nM for inhibition of forskolin-stimulated CFTR Cl-?current in FRT cells.
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