(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。

(R)-BPO-27, the R enantiomer of BPO-27, is a potent, orally active and ATP-competitive CFTR inhibitor with an IC 50 of 4 nM.

Solid

IC50: 4 nM

(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-express

(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.
(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 IC 50 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.
has not independently confirmed the accuracy

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : ≥ 14.28 mg/mL (26.04 mM)配制储备液