2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. NNC 05-2090 hydrochloride

NNC 05-2090 hydrochloride is a GABA uptake inhibitor and inhibitor of the β-GABA transporter (BGT-1) (IC50< /sub>: 10.6 μM). NNC 05-2090 hydrochloride also inhibits mGAT2 with a Ki value of 1.4 μM. NNC 05-2090 has anticonvulsant activity and can be used in the study of epilepsy and neurological diseases.

For research use only. We do not sell to patients.

NNC 05-2090 hydrochloride Chemical Structure

NNC 05-2090 hydrochloride Chemical Structure

CAS No. : 184845-18-9

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Based on 1 publication(s) in Google Scholar

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NNC 05-2090 hydrochloride Related Antibodies

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Description

NNC 05-2090 hydrochloride is a GABA uptake inhibitor and inhibitor of the β-GABA transporter (BGT-1) (IC50< /sub>: 10.6 μM). NNC 05-2090 hydrochloride also inhibits mGAT2 with a Ki value of 1.4 μM. NNC 05-2090 has anticonvulsant activity and can be used in the study of epilepsy and neurological diseases[1][2][3].

In Vitro

NNC 05-2090 hydrochloride shows IC50 values for binding with prazosin and spiperone of 266 and 1632 nM, respectively[1].
NNC 05-2090 hydrochloride (0.1-100 μM) inhibits [3H]GABA uptake in synaptosomes from rat cortex with an IC50 value of 4.4 μM[1].
NNC 05-2090 hydrochloride (0.1-100 μM) inhibits [3H]GABA uptake in synaptosomes prepared from inferior colliculus with an IC50 value of 2.5 μM[1].
NNC 05-2090 hydrochloride inhibits serotonin, noradrenaline, dopamine transporters and BGT-1 with IC50 values of 5.29, 7.91, 4.08 and 10.6 μM, respectively[1].
NNC 05-2090 hydrochloride inhibits GAT-1, GAT-2 and GAT-3 with IC50 values of 29.62, 45.29 and 22.51 μM, respectively[1].
NNC 05-2090 dose-dependently inhibited sound-induced tonic and clonic convulsions in DBA/2 mice with an ED50 value 19 μmol/kg[2].
NNC 05-2090 dose-dependently antagonized tonic hindlimb extension in the maximal electroshock (MES) test with an ED50 values of 73 mmol/kg[2].
NNC 05-2090 significantly (PB0.05) reduces generalized seizure severity (seizure grade 3-5) at highest doses (72-242 mmol/kg) and NNC 05-2090 also significantly reduced afterdischarge duration at these doses (P<0.05)[2].

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

NNC 05-2090 hydrochloride Related Antibodies
In Vivo

NNC 05-2090 hydrochloride (intraperitoneal injection) dose-dependently protects against maximal electroshock (MES) in mice with an ED50 values of 73 μmol/kg, and shows ED50 values against tonic and clonic convulsions in DBA/2 mice of 19 and 26 μmol /kg, respectively[1].
NNC 05-2090 hydrochloride (0.01, 0.1 and 0.3 mg/kg; i.p. or i.,t., once) reverses mechanical allodynia in (partial sciatic nerve ligation) PSL model mice[3].

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

Animal Model: Partial sciatic nerve ligation (PSL) mice with mechanical allodynia[2]
Dosage: 0.01, 0.1 and 0.3 mg/kg
Administration: Intraperitoneal injection or intrathecal injection; 0.1 mg/kg, once
Result: Dose-dependently reversed mechanical allodynia in PSL model mice by both intraperitoneal injection and intrathecal injection.
Molecular Weight

451.00

Formula

C27H31ClN2O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

OC1(CCN(CC1)CCCN2C3=C(C4=C2C=CC=C4)C=CC=C3)C5=C(OC)C=CC=C5.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (221.73 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 2.2173 mL 11.0865 mL 22.1729 mL
5 mM 0.4435 mL 2.2173 mL 4.4346 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 (sealed storage, away from moisture). 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 (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.5 mg/mL (5.54 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 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (5.54 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:

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(per animal)

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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
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 (sealed storage, away from moisture). 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 2.2173 mL 11.0865 mL 22.1729 mL 55.4324 mL
5 mM 0.4435 mL 2.2173 mL 4.4346 mL 11.0865 mL
10 mM 0.2217 mL 1.1086 mL 2.2173 mL 5.5432 mL
15 mM 0.1478 mL 0.7391 mL 1.4782 mL 3.6955 mL
20 mM 0.1109 mL 0.5543 mL 1.1086 mL 2.7716 mL
25 mM 0.0887 mL 0.4435 mL 0.8869 mL 2.2173 mL
30 mM 0.0739 mL 0.3695 mL 0.7391 mL 1.8477 mL
40 mM 0.0554 mL 0.2772 mL 0.5543 mL 1.3858 mL
50 mM 0.0443 mL 0.2217 mL 0.4435 mL 1.1086 mL
60 mM 0.0370 mL 0.1848 mL 0.3695 mL 0.9239 mL
80 mM 0.0277 mL 0.1386 mL 0.2772 mL 0.6929 mL
100 mM 0.0222 mL 0.1109 mL 0.2217 mL 0.5543 mL
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NNC 05-2090 hydrochloride 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:

NNC 05-2090184845-18-9GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorrat cortexpartial sciatic nerve ligationPSLsynaptosomescortexInhibitorinhibitorinhibit

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