2. Neuronal Signaling
  3. TSPO
  4. Emapunil

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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Emapunil

Emapunil 화학구조

CAS No. : 226954-04-7

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
1 mg 해외재고보유
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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고객리뷰

Based on 4 publication(s) in Google Scholar

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Emapunil Related Antibodies

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제품 설명

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[1][2].

Cellular Effect
Cell Line Type Value Description References
HEK-293T IC50
>100 μM
Compound: XBD-173
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
[PMID: 30108706]
HEK-293T IC50
>100 μM
Compound: XBD-173
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
[PMID: 30108706]
HEK-293T IC50
26.2 μM
Compound: XBD-173
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
[PMID: 30108706]
HEK-293T IC50
29.5 μM
Compound: XBD-173
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
[PMID: 30108706]
In Vivo

Emapunil (AC-5216, 0.1-3, 0.003-0.01 and 0.01-0.3 mg/kg, p.o.) produces anti-anxiety effects in the Vogel-type conflict test in rats, and in the light/dark box and social interaction tests in mice[1].
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.

Animal Model: Rats[1].
Dosage: 0.1-3 mg/kg.
Administration: P.O..
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).
Clinical Trial
분자량

401.46

화학식

C23H23N5O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N(CC)CC1=CC=CC=C1)CN2C(N(C)C3=CN=C(C4=CC=CC=C4)N=C23)=O
선적

Room temperature in continental US; may vary elsewhere.
보관
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
용액&용해도
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4909 mL 12.4545 mL 24.9091 mL
5 mM 0.4982 mL 2.4909 mL 4.9818 mL
View the 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.

  • 몰농도 계산기

  • 농도 희석 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
순도&문서
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, 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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Emapunil Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Emapunil226954-04-7AC-5216 XBD-173AC5216AC 5216XBD173XBD 173XBD-173TSPOTranslocator ProteinAntidepressantMBRantianxietydepressionanti-inflammatoryneuroprotectiveposttraumaticstressdisorderPTSDT2DMInhibitorinhibitorinhibit

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상품명:
Emapunil
Cat. No.:
HY-15527
수량:
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