Product Name :
PG01
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.
CAS:
853138-65-5
Molecular Weight:
439.55
Formula:
C28H29N3O2
Chemical Name:
2-[2-(1H-indol-3-yl)-N-methylacetamido]-2-phenyl-N-[4-(propan-2-yl)phenyl]acetamide
Smiles :
CC(C)C1C=CC(=CC=1)NC(=O)C(C1C=CC=CC=1)N(C)C(=O)CC1=CNC2C=CC=CC=21
InChiKey:
PQAYCXMQTUEDRD-UHFFFAOYSA-N
InChi :
InChI=1S/C28H29N3O2/c1-19(2)20-13-15-23(16-14-20)30-28(33)27(21-9-5-4-6-10-21)31(3)26(32)17-22-18-29-25-12-8-7-11-24(22)25/h4-16,18-19,27,29H,17H2,1-3H3,(H,30,33)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
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.|Product information|CAS Number: 853138-65-5|Molecular Weight: 439.55|Formula: C28H29N3O2|Chemical Name: 2-[2-(1H-indol-3-yl)-N-methylacetamido]-2-phenyl-N-[4-(propan-2-yl)phenyl]acetamide|Smiles: CC(C)C1C=CC(=CC=1)NC(=O)C(C1C=CC=CC=1)N(C)C(=O)CC1=CNC2C=CC=CC=21|InChiKey: PQAYCXMQTUEDRD-UHFFFAOYSA-N|InChi: InChI=1S/C28H29N3O2/c1-19(2)20-13-15-23(16-14-20)30-28(33)27(21-9-5-4-6-10-21)31(3)26(32)17-22-18-29-25-12-8-7-11-24(22)25/h4-16,18-19,27,29H,17H2,1-3H3,(H,30,33)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|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.{{Tenofovir alafenamide} web|{Tenofovir alafenamide} Reverse Transcriptase|{Tenofovir alafenamide} Biological Activity|{Tenofovir alafenamide} References|{Tenofovir alafenamide} manufacturer|{Tenofovir alafenamide} Epigenetic Reader Domain} The apparent Kd for PG01 for G551D-CFTR activation is 1 μM, approximately 100-fold better than that of genistein.{{MT1} web|{MT1} Epigenetics|{MT1} Purity & Documentation|{MT1} Data Sheet|{MT1} manufacturer|{MT1} Autophagy} The potency for activation G1349D-CFTR by PG01 is even better at 40 nM.PMID:24187611 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.|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.|Products are for research use only. Not for human use.|
