PG01

PG01

中文名称PG01
中文同义词化合物 T16516;N-甲基-N-[2-[[4-(1-甲基乙基)苯
英文名称PHENYLGLYCINE-01
英文同义词PHENYLGLYCINE-01;N-Methyl-N-[2-[[4-(1-Methylethyl)phenyl]amino]-2-1H-indole-3-acetamide;PG 01;2-[(2-1H-indol-3-yl-acetyl)-methylamino]-N-(4-isopropylphenyl)-2-phenylacetamide;N-Methyl-N-[2-[[4-(1-methylethyl)phenyl]amino]-2-oxo-1-phenylethyl]-1H-indole-3-acetamide;1H-Indole-3-acetamide, N-methyl-N-[2-[[4-(1-methylethyl)phenyl]amino]-2-oxo-1-phenylethyl]-;PG-01 >=98% (HPLC);PG-01,PG01
CAS号853138-65-5
分子式C28H29N3O2
分子量439.55
EINECS号
相关类别
Mol文件853138-65-5.mol
结构式PG01 结构式

PG01 性质

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
溶解度二甲基亚砜:≥10mg/mL
形态粉末
酸度系数(pKa)13.31±0.70(Predicted)
颜色白色至类白色

PG01 用途与合成方法

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。

CFTR

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.

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.

安全信息

危险品标志Xn
危险类别码22
WGK Germany3

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/04/30HY-103369PG01
PG01
853138-65-51mg1550元
2024/04/30HY-103369PG01
PG01
853138-65-55mg4600元

PG01 上下游产品信息

"PG01"相关产品信息
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