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853138-65-5

中文名称 PG01
CAS 853138-65-5
分子式 C28H29N3O2
分子量 439.55
MOL 文件 853138-65-5.mol
更新日期 2024/05/11 14:52:47
853138-65-5 结构式 853138-65-5 结构式

基本信息

英文别名
PG 01
PHENYLGLYCINE-01
PG-01 >=98% (HPLC)
N-Methyl-N-[2-[[4-(1-Methylethyl)phenyl]amino]-2-1H-indole-3-acetamide
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]-

物理化学性质

储存条件-20°C储存
溶解度二甲基亚砜:≥10mg/mL
形态粉末
颜色白色至灰白色

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H302-H413
危险品标志Xn
危险类别码22
WGK Germany3
PG01价格(试剂级)
报价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
2024/04/30HY-103369PG01
PG01
853138-65-510mg7800元

常见问题列表

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。
靶点

CFTR

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.

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.

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