PG01
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- CAS号:
- 853138-65-5
- 英文名:
- PHENYLGLYCINE-01
- 英文别名:
- PG 01;PG-01,PG01;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]-
- 中文名:
- PG01
- 中文别名:
- 化合物 T16516;N-甲基-N-[2-[[4-(1-甲基乙基)苯
- CBNumber:
- CB91474942
- 分子式:
- C28H29N3O2
- 分子量:
- 439.55
- MOL File:
- 853138-65-5.mol
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PG01化学性质
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沸点:
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704.6±60.0 °C(Predicted)
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密度:
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1.217±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: ≥10mg/mL
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形态:
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powder
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酸度系数(pKa):
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13.31±0.70(Predicted)
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颜色:
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white to off-white
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PG01性质、用途与生产工艺
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 itself does not activate ∆F508-CFTR, produces substantial ∆F508-CFTR Cl
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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
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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.
PG01
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下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-103369 | PG01
PG01 | 853138-65-5 | 1mg | 1550元 |
| 2024/04/30 | HY-103369 | PG01
PG01 | 853138-65-5 | 5mg | 4600元 |
853138-65-5, PG01 相关搜索:
- 合成有机化合物配体
- C28H29N3O2
- N-甲基-N-[2-[[4-(1-甲基乙基)苯
- 化合物 T16516
- 853138-65-5
- PG-01,PG01
- PG-01 >=98% (HPLC)
- 1H-Indole-3-acetamide, N-methyl-N-[2-[[4-(1-methylethyl)phenyl]amino]-2-oxo-1-phenylethyl]-
- N-Methyl-N-[2-[[4-(1-methylethyl)phenyl]amino]-2-oxo-1-phenylethyl]-1H-indole-3-acetamide
- 2-[(2-1H-indol-3-yl-acetyl)-methylamino]-N-(4-isopropylphenyl)-2-phenylacetamide
- PG 01
- N-Methyl-N-[2-[[4-(1-Methylethyl)phenyl]amino]-2-1H-indole-3-acetamide
- PHENYLGLYCINE-01