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PG01

CAS No. : 853138-65-5

MCE 站：PG01

产品活性：PG01 是一种有效的 CFTR Cl^- 通道增效剂。PG01 对 E193K，G970R 和 G551D (CFTR突变体) 有效，K_d 值分别为 0.22 μM，0.45 μM 和 1.94 μM。PG01对 ΔF508（K_a 为 0.3 μM）也有效。PG01 在添加 Forskolin 后增加 ΔF508-CFTR Cl^- 电流。

研究领域：Membrane Transporter/Ion Channel

作用靶点：CFTR

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 K_d for 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.

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.

相关产品：Bioactive Compound Library Plus  |  K41498 TFA  |  Kobusin

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