Emapunil
Based on 4 publication(s) in Google Scholar
Emapunil (AC-5216), an orally active and selective TSPO (a mitochondrial benzodiazepine receptor) ligand, produces anti-anxiety and antidepressant-like effects in various animal models.
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- Reinheit: 99.94%
- CAS. Nr.: 226954-04-7
- Formel: C23H23N5O2
- Molecular Weight:401.46
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Emapunil
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
>100 μM
Compound: XBD-173
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Antiproliferative activity against HEK293T cells expressing human TSPO A147T mutant after 48 hrs by BrdU incorporation assay
Antiproliferative activity against HEK293T cells expressing human TSPO A147T mutant after 48 hrs by BrdU incorporation assay
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[PMID: 30108706] |
| HEK-293T | IC50 |
>100 μM
Compound: XBD-173
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Antiproliferative activity against HEK293T cells expressing human wild type TSPO after 48 hrs by BrdU incorporation assay
Antiproliferative activity against HEK293T cells expressing human wild type TSPO after 48 hrs by BrdU incorporation assay
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[PMID: 30108706] |
| HEK-293T | IC50 |
26.2 μM
Compound: XBD-173
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Cytotoxicity against HEK293T cells expressing human TSPO A147T mutant assessed as decrease in cell viability after 48 hrs by CellTiter blue assay
Cytotoxicity against HEK293T cells expressing human TSPO A147T mutant assessed as decrease in cell viability after 48 hrs by CellTiter blue assay
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[PMID: 30108706] |
| HEK-293T | IC50 |
29.5 μM
Compound: XBD-173
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Cytotoxicity against HEK293T cells expressing human wild type TSPO assessed as decrease in cell viability after 48 hrs by CellTiter blue assay
Cytotoxicity against HEK293T cells expressing human wild type TSPO assessed as decrease in cell viability after 48 hrs by CellTiter blue assay
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[PMID: 30108706] |
Emapunil (AC-5216, 3-30 mg/kg, p.o.) reduces the immobility time, and this effect was blocked by PK11195[1].
Emapunil (AC-5216, 1-100 mg/kg, p.o.) produces no distinct change in the rat electroencephalogram[1].
Emapunil (AC-5216, 0.3 and 1 mg/kg, i.g.) causes significant suppression of the enhanced anxiety and contextual fear induced in post-TDS rats[3].
Emapunil (AC-5216, 0.3 and 1 mg/kg, i.g.) alleviates the enhanced anxiety and fear response in a time-dependent sensitization (TDS) procedure, a rat PTSD animal model[3].
Emapunil (AC-5216, 0.3 and 1 mg/kg, i.g.) reverses the increased plasma glucose (PG) and decreased insulin (INS) in HFD-STZ rats[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[1].
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Dosage:0.1-3 mg/kg.
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Administration:P.O..
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Result:Significantly increased the number of shocks that rats received.
Significantly increased the time spent in the light compartment but only slightly increased that time at 0.03 mg/kg, p.o. (P<0.1).
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 226954-04-7
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Appearance Solid
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Molecular Weight 401.46
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Formel C23H23N5O2
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Color White to off-white
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SMILES
O=C(N(CC)CC1=CC=CC=C1)CN2C(N(C)C3=CN=C(C4=CC=CC=C4)N=C23)=O
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Synonyms
AC-5216; XBD-173
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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J Transl Med
The soluble epoxide hydrolase inhibitor TPPU improves comorbidity of chronic pain and depression via the AHR and TSPO signaling. [Abstract]2023 Feb 2;21(1):71. PMID: 36732752 -
Sci Rep
The antidepressant-like activity of AC-5216, a ligand for 18KDa translocator protein (TSPO), in an animal model of diabetes mellitus. [Abstract]2016 Nov 25;6:37345. PMID: 27886206 -
Cancer Biomark
The effects of PK11195 on the MCF-7 and T47D were associated with the allopregnanolone biosynthesis, which was mediated by Translocator Protein 18 KDa. [Abstract]2016 Apr 1;17(1):11-6. PMID: 27062569 -
Lösungsmittel & Löslichkeit
DMSO : 33.33 mg/mL (83.02 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (6.23 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.
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.
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Atsuko Kita, et al. Antianxiety and antidepressant-like effects of AC-5216, a novel mitochondrial benzodiazepine receptor ligand. Br J Pharmacol. 2004 Aug;142(7):1059-72. [Content Brief]
[2]. Marcus Karlstetter, et al. Translocator protein (18 kDa) (TSPO) is expressed in reactive retinal microglia and modulates microglial inflammation and phagocytosis. J Neuroinflammation. 2014 Jan 8;11:3. [Content Brief]
[3]. Li-Ming Zhang, et al. Involvement of allopregnanolone in the anti-PTSD-like effects of AC-5216. J Psychopharmacol. 2016 May;30(5):474-81. [Content Brief]
[4]. Zhi-Kun Qiu, et al. The antidepressant-like activity of AC-5216, a ligand for 18KDa translocator protein (TSPO), in an animal model of diabetes mellitus. Sci Rep. 2016 Nov 25;6:37345. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4909 mL | 12.4545 mL | 24.9091 mL | 62.2727 mL |
| 5 mM | 0.4982 mL | 2.4909 mL | 4.9818 mL | 12.4545 mL | |
| 10 mM | 0.2491 mL | 1.2455 mL | 2.4909 mL | 6.2273 mL | |
| 15 mM | 0.1661 mL | 0.8303 mL | 1.6606 mL | 4.1515 mL | |
| 20 mM | 0.1245 mL | 0.6227 mL | 1.2455 mL | 3.1136 mL | |
| 25 mM | 0.0996 mL | 0.4982 mL | 0.9964 mL | 2.4909 mL | |
| 30 mM | 0.0830 mL | 0.4152 mL | 0.8303 mL | 2.0758 mL | |
| 40 mM | 0.0623 mL | 0.3114 mL | 0.6227 mL | 1.5568 mL | |
| 50 mM | 0.0498 mL | 0.2491 mL | 0.4982 mL | 1.2455 mL | |
| 60 mM | 0.0415 mL | 0.2076 mL | 0.4152 mL | 1.0379 mL | |
| 80 mM | 0.0311 mL | 0.1557 mL | 0.3114 mL | 0.7784 mL |
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