Vizenpistat
Based on 1 Customer Validation
Vizenpistat (SR-8541A) is an orally active ENPP1 inhibitor with an IC50 of 1.4 nM. Vizenpistat elevates cGAMP levels, blocks 2′3′-cGAMP hydrolysis, inhibits adenosine production, modulates STING pathway-mediated innate immune signaling, and regulates antitumor immune responses. Vizenpistat can be used in research related to breast cancer and metastatic microsatellite-stable colorectal cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.93%
- No. CAS: 2687222-58-6
- Fòrmula: C15H21N5O4S
- Peso molecular:367.42
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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
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[4]|
ENPP1 1.4 nM (IC50) |
In Vitro
Vizenpistat (0.5, 5 μM; 48 h) stimulates immune cell infiltration into HPAC pancreatic cancer spheroids in a dendritic cell-dependent manner, with no detectable infiltration from isolated T cells or dendritic cells alone[4].
Vizenpistat (SR-8541A) potently inhibits recombinant human ENPP1 enzymatic activity with an IC50 of 1.4 nM[4].
Vizenpistat shows no detectable inhibitory activity against recombinant human ENPP2[4].
Vizenpistat (0.03-3.0 μM) dose-dependently stimulates PBMC infiltration into parental MDA-MB-231 cancer spheroids, with no effect on ENPP1 knockout MDA-MB-231 spheroids, demonstrating ENPP1-dependent activity[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Vizenpistat (50 mg/kg; i.p.; twice daily; 14 days) synergizes with 10 Gy focal radiation to produce a 65% reduction in radiated tumor volume and a 38.5% abscopal reduction in non-radiated tumor volume in the murine MC38 colon cancer model, while increasing tumor infiltration of CD45+ immune cells and CD335+ NK cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2687222-58-6
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Appearance Solid
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Peso molecular 367.42
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Fòrmula C15H21N5O4S
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Color White to off-white
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SMILES
O=S(N)(N1CCN(CCC1)C2=C3C=C(OC)C(OC)=CC3=NC=N2)=O
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Synonyms
SR-8541A
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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 (272.17 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 (6.80 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.80 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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 (282 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 | 2.7217 mL | 13.6084 mL | 27.2168 mL | 68.0420 mL |
| 5 mM | 0.5443 mL | 2.7217 mL | 5.4434 mL | 13.6084 mL | |
| 10 mM | 0.2722 mL | 1.3608 mL | 2.7217 mL | 6.8042 mL | |
| 15 mM | 0.1814 mL | 0.9072 mL | 1.8145 mL | 4.5361 mL | |
| 20 mM | 0.1361 mL | 0.6804 mL | 1.3608 mL | 3.4021 mL | |
| 25 mM | 0.1089 mL | 0.5443 mL | 1.0887 mL | 2.7217 mL | |
| 30 mM | 0.0907 mL | 0.4536 mL | 0.9072 mL | 2.2681 mL | |
| 40 mM | 0.0680 mL | 0.3402 mL | 0.6804 mL | 1.7011 mL | |
| 50 mM | 0.0544 mL | 0.2722 mL | 0.5443 mL | 1.3608 mL | |
| 60 mM | 0.0454 mL | 0.2268 mL | 0.4536 mL | 1.1340 mL | |
| 80 mM | 0.0340 mL | 0.1701 mL | 0.3402 mL | 0.8505 mL | |
| 100 mM | 0.0272 mL | 0.1361 mL | 0.2722 mL | 0.6804 mL |
Vizenpistat Related Classifications
HY-176296 Related Classifications
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Keywords
- Vizenpistat
- 2687222-58-6
- SR-8541A
- Phosphodiesterase (PDE)
- STING
- Stimulator of Interferon Genes
- TMEM173
- MITA
- ERIS
- MPYS
- anti-tumor immune response
- refractory metastatic microsatellite stable colorectal cancer
- MDA-MB-231
- innate immune signaling
- ENPP1
- advanced metastatic solid tumors
- CT-26
- HEK293T
- STING pathway
- cGAMP
- Inhibitor
- inhibitor
- inhibit