IPAG
Based on 1 Customer Validation
IPAG is a potent sigma-1 receptor antagonist with a pKi of 4.3. IPAG induces apoptosis.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.63%
- CAS No.: 193527-91-2
- Formule: C17H22IN3
- Masse moléculaire:395.28
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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Cell Line
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Type | Value | Description | References |
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| Caco-2 | CC50 |
11.48 μM
Compound: IPAG
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Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
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10.21203/rs.3.rs-23951/v1 |
| Caco-2 | IC50 |
5.96 μM
Compound: IPAG
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Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
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10.21203/rs.3.rs-23951/v1 |
Sigma1 inhibition by IPAG causes the autolysosomal degradation of PD-L1 in PC3 (hormone-insensitive prostate cancer) and MDA-MB-231 (triple-negative breast cancer) cell lines and reduces the levels of functional PD-L1 on the surface of the cells[2].
IPAG treatment produces a mean of 100±8 μg per 106 cells. IPAG can inhibit cell proliferation. Treatment with IPAG decreases cell mass[3].
IPAG treatment suppresses phosphorylation of translational regulator proteins p70S6K, S6, and 4E-BP1[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:T47D cells
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Concentration:10 μM
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Incubation Time:24 hours
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Result:The mean forward scatter height (FSC-H) of DMSO (control) measured 412±5, whereas the mean FSC-H of IPAG treated cells was 390±4.
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Cell Line:T47D cells
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Concentration:10 μM
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Incubation Time:
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Result:Decreased levels of phospho-threonine 389-p70S6Kinase (P-S6K), phospho-serine 235/236-ribosomal S6 (P-S6), and phospho-serine 65-4E-BP1 (P-4E-BP1).
Chemical Information
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CAS No. 193527-91-2
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Appearance Solid
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Masse moléculaire 395.28
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Formule C17H22IN3
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Color White to off-white
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SMILES
N=C(NC1=CC=C(I)C=C1)NC2[C@H]3C[C@H](C4)C[C@@H]2C[C@H]4C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
DMSO : 8.33 mg/mL (21.07 mM; ultrasonic and adjust pH to 3 with 1M HCl 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 (protect from light). 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 (protect from light). 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: ≥ 0.83 mg/mL (2.10 mM); Suspended solution
This protocol yields a suspended solution of ≥ 0.83 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 (8.3 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: ≥ 0.83 mg/mL (2.10 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Pureté et documentation
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Fiche technique (275 KB)
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SDS (398 KB)
- English - EN (398 KB)
- Français - FR (398 KB)
- Deutsch - DE (398 KB)
- Norwegian - NO (398 KB)
- Español - ES (398 KB)
- Swedish - SV (398 KB)
- Italian - IT (398 KB)
- Korean - KR (398 KB)
- Portuguese - PT (398 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. James M Brimson, et al. Simple ammonium salts acting on sigma-1 receptors yield potential treatments for cancer and depression. Sci Rep. 2020 Jun 8;10(1):9251. [Content Brief]
[2]. Halley M Oyer, et al.Small-Molecule Modulators of Sigma1 and Sigma2/TMEM97 in the Context of Cancer: Foundational Concepts and Emerging Themes. Front Pharmacol. 2019 Oct 21;10:1141. [Content Brief]
[3]. Felix J Kim, et al. Inhibition of tumor cell growth by Sigma1 ligand mediated translational repression. Biochem Biophys Res Commun. 2012 Sep 21;426(2):177-82. [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, 6 months; -20°C, 1 month (protect from light). 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 | 2.5299 mL | 12.6493 mL | 25.2985 mL | 63.2463 mL |
| 5 mM | 0.5060 mL | 2.5299 mL | 5.0597 mL | 12.6493 mL | |
| 10 mM | 0.2530 mL | 1.2649 mL | 2.5299 mL | 6.3246 mL | |
| 15 mM | 0.1687 mL | 0.8433 mL | 1.6866 mL | 4.2164 mL | |
| 20 mM | 0.1265 mL | 0.6325 mL | 1.2649 mL | 3.1623 mL |
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