Alpidem |
カタログ番号GC49199
One-Click Copy Product Info
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Alpidem は、α1β2γ2 サブユニットを含む GABAA 受容体に 17 nM の IC50 で選択的に結合し、抗不安効果を発揮します 。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 82626-01-5
Sample solution is provided at 25 µL, 10mM.
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Alpidem is an anxiolytic agent.1 It selectively binds to α1β2γ2 subunit-containing GABAA receptors over α5β2γ2 subunit-containing GABAA receptors in HEK293 cells (IC50s = 0.017 and ≥10 µM, respectively, for the recombinant rat receptors).2 Alpidem also binds to the GABAA/benzodiazepine receptor complex and translocator protein 18 kDa (TSPO) with IC50 values of 0.028 and 0.0079 µM, respectively.3 It reduces marble burying in mice, indicating anxiolytic activity, with a minimum effective dose (MED) of 10 mg/kg.4 Unlike the benzodiazepine alprazolam, alpidem does not induce sedation in mice when administered at doses up to 2 mg/kg.5 Formulations containing alpidem have previously been used in the treatment of generalized anxiety disorder.
1.Skolnick, P.Anxioselective anxiolytics: On a quest for the holy grailTrends Pharamacol. Sci.33(11)611-620(2012) 2.Faure-Halley, C., Graham, D., Arbilla, S., et al.Expression and properties of recombinant α1β2γ2 and α5β2γ2 forms of the rat GABAA receptorEur. J. Pharmacol.246(3)283-287(1993) 3.Trapani, G., Franco, M.C., Ricciardi, L., et al.Synthesis and binding affinity of 2-phenylimidazo[1,2-alpha]pyridine derivatives for both central and peripheral benzodiazepine receptors. A new series of high-affinity and selective ligands for the peripheral typeJ. Med. Chem.40(19)3109-3118(1997) 4.Zivkovic, B., Morel, E., Joly, D., et al.Pharmacological and behavioral profile of alpidem as an anxiolyticPharmacopsychiatry23(Suppl. 3)108-113(1990) 5.HascoËt, M., and Bourin, M.Anticonflict effect of alpidem as compared with the benzodiazepine alprazolam in ratsPharmacol. Biochem. Behav.56(2)317-324(1997)
| Cas No. | 82626-01-5 | SDF | |
| Canonical SMILES | O=C(CC1=C(C2=CC=C(C=C2)Cl)N=C3C=CC(Cl)=CN31)N(CCC)CCC | ||
| Formula | C21H23Cl2N3O | M.Wt | 404.3 |
| 溶解度 | DMSO : 25 mg/mL (61.83 mM; Need ultrasonic) | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4734 mL | 12.3671 mL | 24.7341 mL |
| 5 mM | 494.7 μL | 2.4734 mL | 4.9468 mL |
| 10 mM | 247.3 μL | 1.2367 mL | 2.4734 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >95.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)