NNC 05-2090
NNC 05-2090 is aGABA uptake inhibitor and inhibitor of the β-GABA transporter (BGT-1) (IC50 sub>: 10.6 μM). NNC 05-2090 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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 184845-43-0
- Fòrmula: C27H30N2O2
- Peso molecular:414.54
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
11.4 μM
Compound: NNC05-2090
|
Inhibition of human GAT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
Inhibition of human GAT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
|
[PMID: 25147609] |
| CHO | IC50 |
5.1 μM
Compound: 9, NNC 05-2090
|
Inhibition of human BGT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
Inhibition of human BGT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
|
[PMID: 23886812] |
| CHO | IC50 |
5.1 μM
Compound: NNC05-2090
|
Inhibition of human BGT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
Inhibition of human BGT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
|
[PMID: 25147609] |
| CHO | IC50 |
6.2 μM
Compound: NNC05-2090
|
Inhibition of human GAT2 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
Inhibition of human GAT2 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
|
[PMID: 25147609] |
| CHO | IC50 |
8.92 μM
Compound: NNC05-2090
|
Inhibition of human GAT3 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
Inhibition of human GAT3 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
|
[PMID: 25147609] |
| HEK293 | IC50 |
1.4 μM
Compound: 3, NNC 05-2090
|
Inhibition of mouse mGAT2 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
Inhibition of mouse mGAT2 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
|
[PMID: 25882526] |
| HEK293 | IC50 |
15 μM
Compound: 3, NNC 05-2090
|
Inhibition of mouse mGAT4 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
Inhibition of mouse mGAT4 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
|
[PMID: 25882526] |
| HEK293 | IC50 |
19 μM
Compound: 3, NNC 05-2090
|
Inhibition of mouse mGAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
Inhibition of mouse mGAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
|
[PMID: 25882526] |
| HEK293 | IC50 |
41 μM
Compound: 3, NNC 05-2090
|
Inhibition of mouse mGAT3 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
Inhibition of mouse mGAT3 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
|
[PMID: 25882526] |
NNC 05-2090 shows IC50 values for binding with prazosin and spiperone of 266 and 1632 nM, respectively[1].
NNC 05-2090 (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 (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 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 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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
No. CAS 184845-43-0
-
Peso molecular 414.54
-
Fòrmula C27H30N2O2
-
SMILES
OC1(CCN(CC1)CCCN2C3=C(C=CC=C3)C4=C2C=CC=C4)C5=CC=CC=C5OC
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. C Thomsen, et al. 1-(3-(9H-carbazol-9-yl)-1-propyl)-4-(2-methoxyphenyl)-4-piperidinol, a novel subtype selective inhibitor of the mouse type II GABA-transporter. Br J Pharmacol. 1997 Mar;120(6):983-5. [Content Brief]
[2]. N O Dalby, et al. Anticonvulsant properties of two GABA uptake inhibitors NNC 05-2045 and NNC 05-2090, not acting preferentially on GAT-1. Epilepsy Res. 1997 Jul;28(1):51-61. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NNC 05-2090 Related Classifications
HY-120146 Related Classifications
Powered by Bioz