Golgicide A
Modify Date: 2024-08-16 21:33:26
Golgicide A structure
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Common Name | Golgicide A | ||
|---|---|---|---|---|
| CAS Number | 853138-65-5 | Molecular Weight | 439.54900 | |
| Density | 1.217g/cm3 | Boiling Point | 704.6ºC at 760 mmHg | |
| Molecular Formula | C28H29N3O2 | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | 379.9ºC | |
| Symbol |
GHS07 |
Signal Word | Warning | |
Use of Golgicide APG01 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[1][2]. |
| Name | 2-[[2-(1H-indol-3-yl)acetyl]-methylamino]-2-phenyl-N-(4-propan-2-ylphenyl)acetamide |
|---|---|
| Synonym | More Synonyms |
| Description | 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[1][2]. |
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| Related Catalog | |
| Target |
CFTR[1] |
| In Vitro | 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[1]. |
| In Vivo | 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[1]. |
| References |
| Density | 1.217g/cm3 |
|---|---|
| Boiling Point | 704.6ºC at 760 mmHg |
| Molecular Formula | C28H29N3O2 |
| Molecular Weight | 439.54900 |
| Flash Point | 379.9ºC |
| Exact Mass | 439.22600 |
| PSA | 65.20000 |
| LogP | 5.74520 |
| Index of Refraction | 1.662 |
| PG-01 |
| Phenylglycine-01 |