GRPR antagonist-1
Based on 1 Customer Validation
GRPR antagonist-1 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 4.97, 4.36 and 3.40 μM in PC3, Pan02 and HGC-27 cells, respectively). GRPR antagonist-1 inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis, with anticancer activity.
For research use only. We do not sell to patients.
- Purity: 99.80%
- CAS No.: 3052544-28-9
- Formula: C29H33F3N4O4
- Molecular Weight:558.59
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
IC50: 4.97 μM (GRPR) in PC3, 4.36 μM (GRPR) in Pan02, 3.40 μM (GRPR) in HGC-27[1]
GRPR antagonist-1 (compound 5a) (0.032-100?μM; 48 hours) has the cytotoxicity against certain cancer cells, also reduces PC3, Pan02, HGC-27, and HepG2 cell viability combined with HDAC inhibitor (1 μM)[1].
GRPR antagonist-1 (1, 2, 8 μM; 24 hours) increases the rate of late apoptosis/necrosis, inducing apoptosis of HGC-27 cells[1].
GRPR antagonist-1 (0.8, 4 μM; 24 hours) inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC3, HepG2, HGC-27, Pan02, and HK2 cells[1]
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Concentration:0.032-100 μM
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Incubation Time:48 hours
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Result:Showed the cytotoxicity against these cancer cells, also reduced PC3, Pan02, HGC-27, and HepG2 cell viability combined with HDAC inhibitor (1 μM).
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Cell Line:HGC-27[1]
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Concentration:1, 2, 8 μM
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Incubation Time:24 hours
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Result:Increased the rate of late apoptosis/necrosis, inducing apoptosis of HGC-27 cells.
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Cell Line:HGC-27[1]
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Concentration:0.8, 4 μM
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Incubation Time:24 hours
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Result:Inhibited HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis.
Chemical Information
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CAS No. 3052544-28-9
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Appearance Solid
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Molecular Weight 558.59
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Formula C29H33F3N4O4
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Color White to off-white
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SMILES
CC(C)(OC(N1CCN(CC1)C([C@H](CC2=CNC3=C2C=CC=C3)NC(CC4=CC=C(C=C4)C(F)(F)F)=O)=O)=O)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : ≥ 100 mg/mL (179.02 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Purity & Documentation
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Data Sheet (276 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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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 (sealed storage, away from moisture). 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 | 1.7902 mL | 8.9511 mL | 17.9022 mL | 44.7555 mL |
| 5 mM | 0.3580 mL | 1.7902 mL | 3.5804 mL | 8.9511 mL | |
| 10 mM | 0.1790 mL | 0.8951 mL | 1.7902 mL | 4.4756 mL | |
| 15 mM | 0.1193 mL | 0.5967 mL | 1.1935 mL | 2.9837 mL | |
| 20 mM | 0.0895 mL | 0.4476 mL | 0.8951 mL | 2.2378 mL | |
| 25 mM | 0.0716 mL | 0.3580 mL | 0.7161 mL | 1.7902 mL | |
| 30 mM | 0.0597 mL | 0.2984 mL | 0.5967 mL | 1.4919 mL | |
| 40 mM | 0.0448 mL | 0.2238 mL | 0.4476 mL | 1.1189 mL | |
| 50 mM | 0.0358 mL | 0.1790 mL | 0.3580 mL | 0.8951 mL | |
| 60 mM | 0.0298 mL | 0.1492 mL | 0.2984 mL | 0.7459 mL | |
| 80 mM | 0.0224 mL | 0.1119 mL | 0.2238 mL | 0.5594 mL | |
| 100 mM | 0.0179 mL | 0.0895 mL | 0.1790 mL | 0.4476 mL |
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