GDC-2394
Based on 1 Customer Validation
GDC-2394 is an orally active and selective NLRP3 inhibitor, and also inhibits IL-1β with IC50s of 0.4 μM (human IL-1β) and 0.1 μM (mouse IL-1β). GDC-2394 inhibits NLRP3-induced caspase-1 activity without inhibiting NLRC4-dependent inflammasome activation. GDC-2394 could be used to study gouty arthritis.
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- Purity: 99.87%
- CAS No.: 2238822-07-4
- 화학식: C20H25N5O4S
- 분자량:431.51
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보관:Powder -20°C, 3 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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Hepatocyte | IC50 |
>100 μM
Compound: 20; GDC-2394
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Cytotoxicity against human hepatocyte
Cytotoxicity against human hepatocyte
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[PMID: 36279149] |
GDC-2394 (Compound 20) (20 μM; 30 min) inhibits NLRP3-induced apoptosis associated speck-like protein containing CARD (ASC) speck formation in THP-1 cells[1].
GDC-2394 (1 nM-10 μM; 7 d) inhibits human macrophage IL-1β and IL-18 production after activation of the NLRP3 inflammasome[1].
GDC-2394 (0-20 μM; 30 min) inhibits NLRP3-dependent caspase-1 activation (IC50 = 51 nM) in THP-1 cells, also inhibits NLRP3-dependent IL-1β release (IC50=63 nM) and NLRC4-dependent IL-1β release (IC50 > 20 μM) in mouse bone marrow-derived macrophages (mBMDMs)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GDC-2394 (25 mg/kg; once daily for 7 d) reduces paw swelling and pain in a functional rat model of gouty arthritis[1].
Preclinical PK of GDC-2394[1].
| Species | Mouse | Rat | Dog | Cyno |
| CLp (mL/min/kg) | 10.1 | 1.3 | 11.7 | 4.1 |
| Vss (L/kg) | 0.72 | 0.29 | 0.67 | 0.18 |
| T1/2 (h) | 1.2 | 4.4 | 0.99 | 0.89 |
| %F (1 mg/kg) | 80 | 33 | 78 | 53 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Acute mouse peritonitis model[1]
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Dosage:1 mg/kg and 10 mg/kg
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Administration:Oral gavage; 2 h later treated with 1.25 μg LPS (i.p.) followed by 1 mg monosodium urate crystals (i.p.) a further 2 h later.
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Result:Resulted in a dose-dependent decrease in peritoneal IL-1β concentrations after MSU treatment, and decreased the level of IL-1β by 66.8 and 81.3% at 1 and 10 mg/kg compared with the control.
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Animal Model:Functional rat model of gouty arthritis[1]
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Dosage:25 mg/kg
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Administration:Interventional injection; once daily for 7 days
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Result:Significantly inhibited knee swelling after 48 h.
Chemical Information
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CAS No. 2238822-07-4
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Appearance Solid
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분자량 431.51
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화학식 C20H25N5O4S
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Color White to off-white
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SMILES
O=S(C1=C2OC[C@@H](NC)CN2N=C1)(NC(NC3=C4CCCC4=CC5=C3CCC5)=O)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 50 mg/mL (115.87 mM; ultrasonic and warming and heat to 60°C; 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)
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: ≥ 2.08 mg/mL (4.82 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.82 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
순도&문서
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Data Sheet (280 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)
References
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 | 2.3174 mL | 11.5872 mL | 23.1744 mL | 57.9361 mL |
| 5 mM | 0.4635 mL | 2.3174 mL | 4.6349 mL | 11.5872 mL | |
| 10 mM | 0.2317 mL | 1.1587 mL | 2.3174 mL | 5.7936 mL | |
| 15 mM | 0.1545 mL | 0.7725 mL | 1.5450 mL | 3.8624 mL | |
| 20 mM | 0.1159 mL | 0.5794 mL | 1.1587 mL | 2.8968 mL | |
| 25 mM | 0.0927 mL | 0.4635 mL | 0.9270 mL | 2.3174 mL | |
| 30 mM | 0.0772 mL | 0.3862 mL | 0.7725 mL | 1.9312 mL | |
| 40 mM | 0.0579 mL | 0.2897 mL | 0.5794 mL | 1.4484 mL | |
| 50 mM | 0.0463 mL | 0.2317 mL | 0.4635 mL | 1.1587 mL | |
| 60 mM | 0.0386 mL | 0.1931 mL | 0.3862 mL | 0.9656 mL | |
| 80 mM | 0.0290 mL | 0.1448 mL | 0.2897 mL | 0.7242 mL | |
| 100 mM | 0.0232 mL | 0.1159 mL | 0.2317 mL | 0.5794 mL |
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