(R)-BPO-27

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

(R)-BPO-27，BPO-27 的 R 对映体，CFTR 氯化物电导，IC50 为 4 nM； BPO-27 S 对映体无活性。

(R)-BPO-27, the R enantiomer of BPO-27, CFTR chloride conductance with IC50 of 4 nM; BPO-27 S enantiomer is inactive.

(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 (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.

R)-BPO 27 | (R)-BPO27

Apoptosis

CFTR

CFTR

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1415390-47-4

548.3416

C26H18BrN3O6

>98% (HPLC)

DMSO

O=C(C1=CC=C(O[C@@H](C2=CC=C(Br)O2)C3=C(N(C)C4=O)C(C(N4C)=O)=C(C5=CC=CC=C5)N36)C6=C1)O

6H-Pyrimido[4',5':3,4]pyrrolo[2,1-c][1,4]benzoxazine-2-carboxylic acid, 6-(5-bromo-2-furanyl)-7,8,9,10-tetrahydro-7,9-dimethyl-8,10-dioxo-11-phenyl-, (6R)-

(-20℃)

With Ice Pack

≥ 2 years