GDC-0276
Based on 1 Customer Validation
GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.69%
- No. CAS: 1494581-70-2
- Fòrmula: C24H31FN2O4S
- Peso molecular:462.58
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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Nav1.7 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.011 μM
Compound: 4; GDC-0276
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Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
0.02 μM
Compound: 4; GDC-0276
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Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
0.049 μM
Compound: 4; GDC-0276
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Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
0.48 μM
Compound: 4; GDC-0276
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Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
0.0004 μM
Compound: 4; GDC-0276
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Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
0.4 nM
Compound: 4; GDC-0276
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Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six drug-naïve beagle dogs Group 1 four dogs (n=2 per sex) and Group 2 2 BDC dogs (n=2 male)[3]
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Dosage:0.5, 1, 2, 3, 4, 5 mg/kg
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Administration:Oral adminstration
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Result:Showed mean specific activities of 12.2 µCi/mg (a 24% enrichment) (n=4 animals) and 23.5 µCi/mg (a 139% enrichment) (n=2 animals) for Groups 1 and 2, respectively.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1494581-70-2
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Appearance Solid
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Peso molecular 462.58
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Fòrmula C24H31FN2O4S
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Color White to off-white
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SMILES
O=C(NS(=O)(N1CCC1)=O)C2=CC(C3CC3)=C(OCC4(C5)CC6CC5CC(C6)C4)C=C2F
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
DMSO : 125 mg/mL (270.22 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Pureza y Documentación
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Ficha de datos (275 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Rothenberg ME, et al. Safety, Tolerability, and Pharmacokinetics of GDC-0276, a Novel NaV1.7 Inhibitor, in a First-in-Human, Single- and Multiple-Dose Study i [Content Brief]
[3]. Takahashi RH,et al.Unequal Absorption of Radiolabeled and Nonradiolabeled Drug from the Oral Dose Leads to Incorrect Estimates of Drug Absorption and Circulating Metabolites in a Mass Balance Study.Drug Metab Lett. 2019;13(1):37-44. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1618 mL | 10.8089 mL | 21.6179 mL | 54.0447 mL |
| 5 mM | 0.4324 mL | 2.1618 mL | 4.3236 mL | 10.8089 mL | |
| 10 mM | 0.2162 mL | 1.0809 mL | 2.1618 mL | 5.4045 mL | |
| 15 mM | 0.1441 mL | 0.7206 mL | 1.4412 mL | 3.6030 mL | |
| 20 mM | 0.1081 mL | 0.5404 mL | 1.0809 mL | 2.7022 mL | |
| 25 mM | 0.0865 mL | 0.4324 mL | 0.8647 mL | 2.1618 mL | |
| 30 mM | 0.0721 mL | 0.3603 mL | 0.7206 mL | 1.8015 mL | |
| 40 mM | 0.0540 mL | 0.2702 mL | 0.5404 mL | 1.3511 mL | |
| 50 mM | 0.0432 mL | 0.2162 mL | 0.4324 mL | 1.0809 mL | |
| 60 mM | 0.0360 mL | 0.1801 mL | 0.3603 mL | 0.9007 mL | |
| 80 mM | 0.0270 mL | 0.1351 mL | 0.2702 mL | 0.6756 mL | |
| 100 mM | 0.0216 mL | 0.1081 mL | 0.2162 mL | 0.5404 mL |
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