CAS NO: | 1415390-47-4 |
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 |
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].
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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 |
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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
* 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。 |