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Purity: ≥98%
Emapunil (formerly known as AC-5216 or XBD-173) is an antianxiolytic drug that also has neuroprotective activities. It acts as a potent and selective agonist at the peripheral benzodiazepine receptor, also known as the mitochondrial 18 kDa translocator protein or TSPO. TSPO is a five transmembrane domain protein (18 kDa) that is expressed predominantly in steroid-synthesizing tissues. This protein has multiple functions including the regulation of steroidogenesis, in particular the production of neuroactive steroids such as allopregnanolone in the brain. Emapunil exerts anxiolytic effects not only in animal models, but also in human volunteers. As a ligand for TSPO, AC-5216 produces anxiolytic- and antidepressant-like effects in animal models. The antidepressant-like effects of AC-5216 on HFD-STZ rats, suggests that TSPO may represent a novel therapeutic target for depression in T2DM.
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| ln Vivo |
Anxiolytic effects are produced by emapunil (AC-5216, 0.1-3, 0.003-0.01 and 0.01-0.3 mg/kg, po) in the Vogel-type conflict test, as well as in the light/dark box and social interaction tests in rats and mice[1]. Emapunil (AC-5216, 3–30 mg/kg, po) shortens the duration of immobility; PK11195 inhibits this effect [1]. An electroencephalogram of rats treated with emapunil (AC-5216, 1-100 mg/kg, po) did not show any appreciable changes [1]. Emapunil (AC-5216, 0.3 and 1 mg/kg, ig) has been shown to dramatically reduce rats' increased anxiety and contextual fear following TDS [3]. In rats used as an animal model for post-traumatic stress disorder, emapunil (AC-5216, 0.3 and 1 mg/kg, ig) reduces increased anxiety and fear responses during a time-dependent sensitization (TDS) procedure [3]. In HFD-STZ rats, the increase in plasma glucose (PG) and decrease in insulin (INS) are reversed by emapunil (AC-5216, 0.3 and 1 mg/kg, ig) [4].
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| Animal Protocol |
Animal/Disease Models: Rats[1].
Doses: 0.1-3 mg/kg. Route of Administration: PO. Experimental Results: Dramatically increased the number of shocks that rats received. Dramatically increased the time spent in the light compartment but only slightly increased that time at 0.03 mg/kg, po (P<0.1). |
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| References |
[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.
[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. [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. [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. |
| Molecular Formula |
C23H23N5O2
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| Molecular Weight |
401.46
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| CAS # |
226954-04-7
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| SMILES |
O=C(CN1C2N=C(N=CC=2N(C)C1=O)C1C=CC=CC=1)N(CC)CC1C=CC=CC=1
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2491 mL | 1.2455 mL | 2.4909 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
J Med Chem.2011 Oct 27;54(20):7165-75. |
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SJL/J mice weight kinetics for vehicle- and XBD173-treatment.Biochim Biophys Acta.2017 Dec;1863(12):3016-3027. |
Clinical score for vehicle- and XBD173-treatment.Biochim Biophys Acta.2017 Dec;1863(12):3016-3027. |
Effect of XBD173 on motor activity.Biochim Biophys Acta.2017 Dec;1863(12):3016-3027. |
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Cerebral distribution of MBP-immunoreactivity at D14.Biochim Biophys Acta.2017 Dec;1863(12):3016-3027. |
MBP-immunofluorescent material in the spinal cord at the disease peak (D14).Biochim Biophys Acta.2017 Dec;1863(12):3016-3027. |
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