| CAS NO: | 853138-65-5 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 生物活性 | PG01 is a potentCFTRCl-channel potentiator. PG01 can correct gating defects ofCFTRmutants, is effective on b>E193K,G970RandG551D(CFTR mutants) withKdvalues of 0.22 μM, 0.45 μM and 1.94 μM, respectively. PG01 is also effective onΔF508(Kaof 0.3 μM). PG01 increasesΔF508-CFTRCl-current after adding Forskolin[1][2]. | |||||||||
| IC50& Target | CFTR[1] | |||||||||
| 体外研究 (In Vitro) | PG01 itself does not activate ?F508-CFTR, produces substantial ?F508-CFTR Cl-current after the addition of 0.5 and 2 μM Forskolin. PG01 at 100 nM strongly stimulates channel activity with multiple channel openings observed. The apparent Kdfor PG01 for G551D-CFTR activation is 1 μM, approximately 100-fold better than that of genistein. The potency for activation G1349D-CFTR by PG01 is even better at 40 nM. PG01 produces large currents in both G551D- and G1349D-CFTR expressing cells. The currents are sensitive to CFTRinh-172 and are not seen in nontransfected cells[1]. | |||||||||
| 体内研究 (In Vivo) | Pharmacokinetic analysis of PG01 in rats is done by serial measurements of plasma concentrations after single bolus infusions (5 mg/kg). PG01 pharmacokinetics fitted a two-compartment model with half-times of ＜5 min and 130 min with volume of distribution 4 L. Microsome metabolism studies and rat pharmacokinetic analysis suggests significantly more rapid metabolism of PG01 than SF-03[1]. | |||||||||
| 分子量 | 439.55 | |||||||||
| 性状 | Solid | |||||||||
| Formula | C28H29N3O2 | |||||||||
| CAS 号 | 853138-65-5 | |||||||||
| 运输条件 | Room temperature in continental US; may vary elsewhere. | |||||||||
| 储存方式 |
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