(R)-BPO-27,99.86%
产品编号:Bellancom-19778| CAS NO:1415390-47-4| 分子式:C26H18BrN3O6| 分子量:548.34
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(R)-BPO-27
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。 | ||||||||||||||||
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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. 西域 has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||||||
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. 西域 has not independently confirmed the accuracy of these methods. They are for reference only.
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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. 西域 has not independently confirmed the accuracy of these methods. They are for reference only.
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性状 | Solid | ||||||||||||||||
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
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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。 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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参考文献 |
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