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Emapunil

Name: Emapunil
Brand: TargetMol
SKU: T2371
Price: 31 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T2371Cas No. 226954-04-7

Alias XBD-173, AC-5216

Emapunil (XBD-173) is an anxiolytic drug which acts as a selective agonist at the peripheral benzodiazepine receptor, also known as the mitochondrial 18 kDa translocator protein or TSPO.

Emapunil

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Purity: 99.9%

Catalog No. T2371Alias XBD-173, AC-5216Cas No. 226954-04-7

Emapunil (XBD-173) is an anxiolytic drug which acts as a selective agonist at the peripheral benzodiazepine receptor, also known as the mitochondrial 18 kDa translocator protein or TSPO.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$31	In Stock	In Stock
5 mg	$73	In Stock	In Stock
10 mg	$123	In Stock	In Stock
25 mg	$198	In Stock	In Stock
50 mg	$297	In Stock	In Stock
100 mg	$428	In Stock	In Stock
200 mg	$623	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$80	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.9%

Color:White

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COA HNMR LCMS

Product Introduction

Emapunil AI Summary

Emapunil exhibits high affinity for the PBR receptor with a Ki value of 0.2 nM, indicating strong binding at this site. It also shows high affinity for the TSPO (translocator protein) with a Ki value of 6.4 nM for the wild type and 31.3 nM for the A147T mutant, demonstrating selectivity with a ratio of 4.9. The compound displays moderate lipophilicity with a log D value ranging between 3.3 and 3.48, suggesting good solubility in both octanol and aqueous environments. In pharmacological evaluations, Emapunil exhibits antianxiety activity in mice, with increased time spent in the illuminated area in the light/dark box test at doses of 1 mg/kg, 3 mg/kg, and 10 mg/kg. Moreover, the compound was shown to displace [11C]-PK-11195 from TPSO in rat brain homogenate with a Ki value of 0.6 nM, reinforcing its high affinity for TSPO. Cytotoxicity assays indicate that Emapunil has moderate potency against cell lines expressing wild type TSPO and the A147T mutant with IC50 values of 29500.0 nM and 26200.0 nM, respectively, and presents a selectivity ratio of 0.9. In antiviral studies, Emapunil has shown some activity against SARS-CoV-2. It inhibits induced cytotoxicity in Caco-2 and VERO-6 cells with inhibition rates of -3.49% and 0.04% at a concentration of 10 µM after 48 hours of exposure, respectively. However, the IC50 value for this antiviral activity is greater than 20000.0 nM, indicating moderate to low potency. Additionally, Emapunil inhibits human HDAC6 enzyme activity, with an inhibition rate of 31.17% using a commercial peptide substrate, although this rate slightly decreases to -3.86% when a custom peptide substrate is used. The collective data indicates that Emapunil has multiple pharmacological effects, with significant binding and functional activity at specific receptor sites and variable efficacy in antiviral and enzyme inhibition assays..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Emapunil (XBD-173) is an anxiolytic drug which acts as a selective agonist at the peripheral benzodiazepine receptor, also known as the mitochondrial 18 kDa translocator protein or TSPO.
Synonyms	XBD-173, AC-5216

Chemical Properties

Molecular Weight	401.46
Formula	C₂₃H₂₃N₅O₂
Cas No.	226954-04-7
Smiles	CCN(Cc1ccccc1)C(=O)Cn1c2nc(ncc2n(C)c1=O)-c1ccccc1
Relative Density.	1.25g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 50 mg/mL (124.55 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.98 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4909 mL	12.4545 mL	24.9091 mL	124.5454 mL
5 mM	0.4982 mL	2.4909 mL	4.9818 mL	24.9091 mL
10 mM	0.2491 mL	1.2455 mL	2.4909 mL	12.4545 mL
20 mM	0.1245 mL	0.6227 mL	1.2455 mL	6.2273 mL
50 mM	0.0498 mL	0.2491 mL	0.4982 mL	2.4909 mL
100 mM	0.0249 mL	0.1245 mL	0.2491 mL	1.2455 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Emapunil

Emapunil

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