2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. Ro15-4513

Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR). Ro15-4513 is a potent ethanol antagonist. Ro15-4513 has anti-anxiety effect. Ro15-4513 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

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Ro15-4513 Chemical Structure

Ro15-4513 Chemical Structure

CAS No. : 91917-65-6

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 138 In-stock
Solution
10 mM * 1 mL in DMSO USD 138 In-stock
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5 mg USD 125 In-stock
10 mg USD 185 In-stock
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Based on 1 publication(s) in Google Scholar

Ro15-4513 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR)[1]. Ro15-4513 is a potent ethanol antagonist[2]. Ro15-4513 has anti-anxiety effect[3]. Ro15-4513 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

IC50 & Target

BZR[1]; ethanol[2];
In Vitro

Ro15-4513 usually acts as a partial inverse agonist at GABAA receptors, except an agonist for α4 and α6 subunit-containing ones[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Ro15-4513 Related Antibodies
In Vivo

Ro 15-4513 (i.p.; 3 mg/kg; 10 min before being tested) completely inhibits the ethanol-induced (1.8 g/kg) reduction in total locomotor activity and partly the reduction in rearing[2].
Ro 15-4513 (i.p.; 3 mg/kg; 15 min before administration of 1.5 g/kg ethanol) reverses ethanol-induced sedation in GABAA receptor δ subunit-deficient mice[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6J mice[2]
Dosage: 3 mg/kg
Administration: I.p.; 10 min before being tested
Result: Completely inhibited the ethanol-induced reduction in total locomotor activity and partly the reduction in rearing.
Molecular Weight

326.31

Formula

C15H14N6O3
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(C1=C(CN2C)N(C=N1)C3=CC=C(N=[N+]=[N-])C=C3C2=O)OCC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (30.65 mM; ultrasonic and warming and heat to 60°C; 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 3.0646 mL 15.3229 mL 30.6457 mL
5 mM 0.6129 mL 3.0646 mL 6.1291 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1 mg/mL (3.06 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Purity & Documentation

Purity: 99.17%

COA (250 KB) HNMR (118 KB) RP-HPLC (168 KB) LCMS (203 KB) Elemental Analysis Report (108 KB)

Handling Instructions (2659 KB)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0646 mL 15.3229 mL 30.6457 mL 76.6143 mL
5 mM 0.6129 mL 3.0646 mL 6.1291 mL 15.3229 mL
10 mM 0.3065 mL 1.5323 mL 3.0646 mL 7.6614 mL
15 mM 0.2043 mL 1.0215 mL 2.0430 mL 5.1076 mL
20 mM 0.1532 mL 0.7661 mL 1.5323 mL 3.8307 mL
25 mM 0.1226 mL 0.6129 mL 1.2258 mL 3.0646 mL
30 mM 0.1022 mL 0.5108 mL 1.0215 mL 2.5538 mL
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Ro15-4513 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:

Ro15-451391917-65-6GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorimidazobenzodiazepinonederivativepartialinverseagonistbenzodiazepinereceptorBZRethanol,GABAA,anti-anxietyInhibitorinhibitorinhibit

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