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Cat. No.: HY-120146

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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 K_i value of 1.4 μM. NNC 05-2090 has anticonvulsant activity and can be used in the study of epilepsy and neurological diseases.

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CAS No.: 184845-43-0
Formule: C₂₇H₃₀N₂O₂
Masse moléculaire:414.54

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Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (277 KB)

NNC 05-2090 Chemical Structure

CAS No.: 184845-43-0

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Cellular Effect

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]

In Vitro

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. .

In Vivo

NNC 05-2090 (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 (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.

Chemical Information

CAS No. 184845-43-0
Masse moléculaire 414.54
Formule C₂₇H₃₀N₂O₂
SMILES

OC1(CCN(CC1)CCCN2C3=C(C=CC=C3)C4=C2C=CC=C4)C5=CC=CC=C5OC
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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

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Calculateur de dilution

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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