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Ro 15-4513

Alias: Ro-15-4513; Ro 154513; Ro 15-4513
Cat No.:V13862 Purity: ≥98%
Ro15-4513 is an imidazobenzodiazepine analogue and a partial inverse agonist of the benzodiazepine receptor (BZR).
Ro 15-4513
Ro 15-4513 Chemical Structure CAS No.: 91917-65-6
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
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1mg
5mg
10mg
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Product Description
Ro15-4513 is an imidazobenzodiazepine analogue and a partial inverse agonist of the benzodiazepine receptor (BZR). Ro15-4513 is a potent ethanol antagonist. Ro15-4513 has anxiolytic (anti-anxiety) effects. Ro15-4513 is a reagent for click chemistry. It has an Azide (N3) moiety and could undergo CuAAc (copper-catalyzed azide-alkyne cycloaddition reaction) with compounds bearing an Alkyne group. SPAAC (Strain-promoted alkyne-azide cycloaddition) may also happen with compounds bearing a BCN or DBCO group.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
For GABAA receptors, Ro15-4513 typically functions as a partial inverse agonist, with the exception of agonists that contain α4 and α6 subunits [3].
ln Vivo
Complete inhibition of the ethanol (1.8 g/kg)-induced decrease in overall locomotor activity and partial inhibition of the ethanol-induced drop in backup force were observed with Ro 15-4513 (ip; 3 mg/kg; 10 min before testing) [2]. In mice lacking the GABAA receptor delta subunit, Ro 15-4513 (ip injection; 3 mg/kg; 15 minutes prior to 1.5 g/kg ethanol administration) reverses ethanol-induced drowsiness [2].
Animal Protocol
Animal/Disease Models: Male C57BL/6J mice [2]
Doses: 3 mg/kg
Route of Administration: intraperitoneal (ip) injection; 10 minutes before test
Experimental Results: Complete inhibition of ethanol-induced decrease in total locomotor activity and partial decrease in standing.
References

[1]. Ro 15-4513: partial inverse agonism at the BZR and interaction with ethanol. Pharmacol Biochem Behav. 1988 Nov;31(3):733-49.

[2]. Effects of Ro15-4513 and other benzodiazepine receptor inverse agonists on alcohol-inducedintoxication in the rat. J Pharmacol Exp Ther. 1988 Jun;245(3):880-6.

[3]. Ro 15-4513 Antagonizes Alcohol-Induced Sedation in Mice Through αβγ2-type GABA(A) Receptors. Front Neurosci. 2011 Jan 20;5:3.

Additional Infomation
8-azido-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid ethyl ester is an organonitrogen heterocyclic compound and an organic heterotricyclic compound.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C16H17N7O3
Molecular Weight
355.36
Exact Mass
326.113
CAS #
91917-65-6
PubChem CID
5081
Appearance
Off-white to yellow solid powder
LogP
1.967
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
6
Rotatable Bond Count
4
Heavy Atom Count
24
Complexity
563
Defined Atom Stereocenter Count
0
InChi Key
CFSOJZTUTOQNIA-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H14N6O3/c1-3-24-15(23)13-12-7-20(2)14(22)10-6-9(18-19-16)4-5-11(10)21(12)8-17-13/h4-6,8H,3,7H2,1-2H3
Chemical Name
ethyl 8-azido-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate
Synonyms
Ro-15-4513; Ro 154513; Ro 15-4513
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~10 mg/mL (~30.65 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 1 mg/mL (3.06 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.8140 mL 14.0702 mL 28.1405 mL
5 mM 0.5628 mL 2.8140 mL 5.6281 mL
10 mM 0.2814 mL 1.4070 mL 2.8140 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.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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.

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