GDC-0334
Based on 1 Customer Validation
GDC-0334 is a selective TRPA1 antagonist. GDC-0334 inhibits TRPA1 function on airway smooth muscle and sensory neurons by decreasing cough and allergic airway inflammation in rats and guinea pigs. GDC-0334 can be used for TRPA1-mediated diseases research, such as pain or asthma.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.94%
- No. CAS: 1984824-54-5
- Fòrmula: C24H19F8N5O3S
- Peso molecular:609.49
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
Actividad biológica
Descripciòn
IC50 & Target
[2]|
TRPA1 |
In Vivo
GDC-0334 (0.5/1 mg/kg for i.v., 1/5 mg/kg mg/kg for p.o.) shows a T1/2 of 11.9 h in mice and 9.79 h in rats by i.v., and oral bioavailability (F%) of 45.0% in mice and 46.2% in rats [1].
Pharmacokinetic parameters for GDC-0334 in mouse/rat/dog/monkey [1]
| Species | IV Dose | CL (ml/min/kg) | VSS (liter/kg) | T1/2 (h) | PO Dose(mg/kg) | Oral F(%) |
| Mouse | 0.5 | 12.4 | 13.9 | 11.9 | 1 | 45.0 |
| Rat | 1 | 7.68 | 5.55 | 9.79 | 5 | 46.2 |
| Dog | 1 | 7.57 | 6.97 | 28.0 | 5 | 27.1 |
| Monkey | 1 | 14.9 | 5.41 | 7.75 | 5 | 13.4 |
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1984824-54-5
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Appearance Solid
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Peso molecular 609.49
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Fòrmula C24H19F8N5O3S
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Color White to off-white
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SMILES
O=C([C@H]1N(S(=O)(C2=CC=C(F)C=C2)=O)[C@@H](C)[C@H](F)C1)NCC3=CC(C4=CN=C(C(F)(F)F)N=C4)=NC=C3C(F)(F)F
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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 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (164.07 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: ≥ 2.5 mg/mL (4.10 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
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 (289 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6407 mL | 8.2036 mL | 16.4072 mL | 41.0179 mL |
| 5 mM | 0.3281 mL | 1.6407 mL | 3.2814 mL | 8.2036 mL | |
| 10 mM | 0.1641 mL | 0.8204 mL | 1.6407 mL | 4.1018 mL | |
| 15 mM | 0.1094 mL | 0.5469 mL | 1.0938 mL | 2.7345 mL | |
| 20 mM | 0.0820 mL | 0.4102 mL | 0.8204 mL | 2.0509 mL | |
| 25 mM | 0.0656 mL | 0.3281 mL | 0.6563 mL | 1.6407 mL | |
| 30 mM | 0.0547 mL | 0.2735 mL | 0.5469 mL | 1.3673 mL | |
| 40 mM | 0.0410 mL | 0.2051 mL | 0.4102 mL | 1.0254 mL | |
| 50 mM | 0.0328 mL | 0.1641 mL | 0.3281 mL | 0.8204 mL | |
| 60 mM | 0.0273 mL | 0.1367 mL | 0.2735 mL | 0.6836 mL | |
| 80 mM | 0.0205 mL | 0.1025 mL | 0.2051 mL | 0.5127 mL | |
| 100 mM | 0.0164 mL | 0.0820 mL | 0.1641 mL | 0.4102 mL |
GDC-0334 Related Classifications
HY-115877 Related Classifications
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