PF-03463275
Based on 1 Customer Validation
PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.79%
- CAS. Nr.: 1173239-39-8
- Formel: C19H22ClFN4O
- Molecular Weight:376.86
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Membrane Transporter/Ion Channel Compound Library
HY-L011
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Neuronal Signaling Compound Library
HY-L013
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Clinical Compound Library
HY-L026
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CNS-Penetrant Compound Library
HY-L028
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Drug Repurposing Compound Library
HY-L035
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Orally Active Compound Library
HY-L061
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
HY-L150
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Highly Selective Inhibitors Library
HY-L158
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Drug Repurposing Compound Library Plus
HY-L035P
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Clinical Compound Library Plus
HY-L026P
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Biologische Aktivität
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GlyT1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
8500 nM
Compound: 10
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Inhibition human ERG expressed in HEK293 cells assessed as blockade of membrane current by patch clamp method
Inhibition human ERG expressed in HEK293 cells assessed as blockade of membrane current by patch clamp method
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[PMID: 19410451] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats[2]
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Dosage:1, 3 and 10 mg/kg
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Administration:S.c.
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Result:A dose-dependent reduction in the amplitude of oscillatory potentials (OPs) elicited from the dark-adapted rats.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1173239-39-8
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Appearance Solid
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Molecular Weight 376.86
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Formel C19H22ClFN4O
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Color White to light yellow
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SMILES
O=C(C(N=C1)=CN1C)N(CC(C=C2)=CC(Cl)=C2F)C[C@@H]3[C@](C4)([H])[C@@]3([H])CN4C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
DMSO : 33.33 mg/mL (88.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.83 mg/mL (2.20 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.83 mg/mL (2.20 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Lowe JA 3rd, et al. The discovery of a structurally novel class of inhibitors of the type 1 glycine transporter [published correction appears in Bioorg Med Chem Lett. 2009 Aug 15;19(16):4885. Bronk, Brian S [added]; Schaeffer, Eric [added]]. Bioorg Med Chem Lett. 2009;19(11):2974-2976. [Content Brief]
[2]. Liu CN, Pettersen B, Seitis G, Osgood S, Somps C. GlyT1 inhibitor reduces oscillatory potentials of the electroretinogram in rats. Cutan Ocul Toxicol. 2014;33(3):206-211. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.6535 mL | 13.2675 mL | 26.5351 mL | 66.3376 mL |
| 5 mM | 0.5307 mL | 2.6535 mL | 5.3070 mL | 13.2675 mL | |
| 10 mM | 0.2654 mL | 1.3268 mL | 2.6535 mL | 6.6338 mL | |
| 15 mM | 0.1769 mL | 0.8845 mL | 1.7690 mL | 4.4225 mL | |
| 20 mM | 0.1327 mL | 0.6634 mL | 1.3268 mL | 3.3169 mL | |
| 25 mM | 0.1061 mL | 0.5307 mL | 1.0614 mL | 2.6535 mL | |
| 30 mM | 0.0885 mL | 0.4423 mL | 0.8845 mL | 2.2113 mL | |
| 40 mM | 0.0663 mL | 0.3317 mL | 0.6634 mL | 1.6584 mL | |
| 50 mM | 0.0531 mL | 0.2654 mL | 0.5307 mL | 1.3268 mL | |
| 60 mM | 0.0442 mL | 0.2211 mL | 0.4423 mL | 1.1056 mL | |
| 80 mM | 0.0332 mL | 0.1658 mL | 0.3317 mL | 0.8292 mL |
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