PG01

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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，Kd 值分别为 0.22 μM，0.45 μM 和 1.94 μM。PG01对 ΔF508（Ka 为 0.3 μM）也有效。PG01 在添加 Forskolin 后增加 ΔF508-CFTR Cl- 电流。

PG01 is a potent CFTR Cl- channel potentiator. PG01 can correct gating defects of CFTR mutants, is effective on b>E193K, G970R and G551D (CFTR mutants) with Kd values of 0.22 μM, 0.45 μM and 1.94 μM, respectively. PG01 is also effective on ΔF508 (Ka of 0.3 μM). PG01 increases ΔF508-CFTR Cl- current after adding Forskolin.

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 Kd 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.

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.

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Apoptosis

CFTR

CFTR

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853138-65-5

439.55

C28H29N3O2

>98% (HPLC)

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CC(C)c1ccc(NC(=O)C(N(C)C(=O)Cc2c[nH]c3ccccc23)c2ccccc2)cc1

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(-20℃)

With Ice Pack

≥ 2 years