| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
While PG01 alone does not activate ΔF508-CFTR, the addition of 0.5 and 2 μM Forskolin causes significant ΔF508-CFTR Cl-currents. Channel activity was substantially increased by PG01 at 100 nM, and numerous channel openings were seen. PG01's apparent Kd for G551D-CFTR activation is 1 μM, which is around 100 times more effective than genistein's. At 40 nM, PG01's activation potency over G1349D-CFTR was considerably greater. When G551D and G1349D-CFTR are expressed in cells, PG01 produces significant currents. This current is not present in untransfected cells and is sensitive to CFTRinh-172 [1].
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| ln Vivo |
Rats receiving a single bolus injection of PG01 (5 mg/kg) had their plasma concentrations serially measured to conduct a pharmacokinetic analysis. PG01's pharmacokinetics, which have a distribution volume of 4L and half-lives of less than 5 minutes and 130 minutes, are in line with the two-compartment model. Research on microsomal metabolism and rat pharmacokinetics demonstrate that PG01's metabolism is substantially quicker than SF-03's[1].
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| References |
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| Molecular Formula |
C28H29N3O2
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|---|---|
| Molecular Weight |
439.54876
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| Exact Mass |
439.226
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| CAS # |
853138-65-5
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| PubChem CID |
4695397
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| Appearance |
White to off-white solid powder
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| Density |
1.217g/cm3
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| Boiling Point |
704.6ºC at 760 mmHg
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| Flash Point |
379.9ºC
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| Index of Refraction |
1.662
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| LogP |
5.745
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
33
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| Complexity |
652
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
PQAYCXMQTUEDRD-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
2-[[2-(1H-indol-3-yl)acetyl]-methylamino]-2-phenyl-N-(4-propan-2-ylphenyl)acetamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2751 mL | 11.3753 mL | 22.7505 mL | |
| 5 mM | 0.4550 mL | 2.2751 mL | 4.5501 mL | |
| 10 mM | 0.2275 mL | 1.1375 mL | 2.2751 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05539105 | RECRUITING | Procedure: Double tract reconstruction Procedure: Gastric conduit reconstruction Procedure: Other reconstructions |
Proximal Gastric Adenocarcinoma Reconstruction |
Shanghai Zhongshan Hospital | 2022-08-22 | |
| NCT01867073 | UNKNOWN STATUS | Other: Biomarker | Advanced Solid Tumors | National University Hospital, Singapore | 2011-05 | |
| NCT00941200 | UNKNOWN STATUS | Biological: Blood collection | Cancer | National University Hospital, Singapore | 2009-04 | |
| NCT06494956 | NOT YET RECRUITING | Procedure: Implant device | Parkinson Disease Dementia | Jiangsu CED Medtech Co., Ltd | 2024-07-01 | Not Applicable |
| NCT02205320 | UNKNOWN STATUS | Biological: DRL_PG Biological: Pegfilgrastim Form A Biological: Pegfilgrastim Form B |
Pharmacokinetics | Dr. Reddy's Laboratories Limited | 2014-02 | Phase 1 |
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