PG01
- CAS号:853138-65-5
- 英文名:PHENYLGLYCINE-01
- 中文名:PG01
- CBNumber:CB91474942
- 分子式:C28H29N3O2
- 分子量:439.55
- MOL File:853138-65-5.mol
- 沸点 :704.6±60.0 °C(Predicted)
- 密度 :1.217±0.06 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :DMSO: ≥10mg/mL
- 形态 :powder
- 酸度系数(pKa) :13.31±0.70(Predicted)
- 颜色 :white to off-white
PG01性质、用途与生产工艺
- 生物活性 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，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。
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靶点
CFTR
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体外研究
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.
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体内研究
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.
- 更新日期：2024/11/08
- 产品编号：HY-103369
- 产品名称：PG01 PG01
- CAS编号：853138-65-5
- 包装：1mg
- 价格：1550元
- 更新日期：2024/11/08
- 产品编号：HY-103369
- 产品名称：PG01 PG01
- CAS编号：
- 包装：10 mM * 1 mLin DMSO
- 价格：4448元
- 公司名称：TOCRIS-US
- 联系电话：--
- 电子邮件：customerservice@tocris.co.uk
- 国家：英国
- 产品数：5726
- 优势度：77
