LU-32-176B

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LU-32-176B, a GABA transporter 1(GAT1) selective inhibitor, is found to exert a synergistic anticonvulsant action with GAT2 transport inhibitor EF1502. LU-32-176B inhibits neurons, astrocytes and mGAT1 with the IC₅₀ values of 2μM, 1μM, 4μM, respectively.

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LU-32-176B Chemical Structure

CAS No. : 770688-66-9

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Description	LU-32-176B, a GABA transporter 1(GAT1) selective inhibitor, is found to exert a synergistic anticonvulsant action with GAT2 transport inhibitor EF1502. LU-32-176B inhibits neurons, astrocytes and mGAT1 with the IC₅₀ values of 2μM, 1μM, 4μM, respectively^[1]^[2].
IC₅₀ & Target	LU-32-176B inhibits neurons, astrocytes and mGAT1 with the IC₅₀ values of 2μM, 1μM, 4μM, respectively^[1]^[2].
In Vivo	LU-32-176B (i.p.) and EF1502 can prevent sound-induced seizures in the Frings AGS-susceptible mouse model^[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight	398.45
Formula	C₂₃H₂₄F₂N₂O₂
CAS No.	770688-66-9
SMILES	OC1=NOC2=C1C(CCC2)NCCCC(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (270 KB) Handling Instructions (2659 KB)
References	[1]. Schousboe A, et al. GABA transporters as drug targets for modulation of GABAergic activity. Biochem Pharmacol. 2004;68(8):1557-1563. [Content Brief] [2]. White HS, et al. First demonstration of a functional role for central nervous system betaine/{gamma}-aminobutyric acid transporter (mGAT2) based on synergistic anticonvulsant action among inhibitors of mGAT1 and mGAT2. J Pharmacol Exp Ther. 2005;312(2):86 [Content Brief]

LU-32-176B Related Classifications

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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:

LU-32-176B770688-66-9GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorsynergistic anticonvulsant actionGAT2EF1502neuronsastrocytesmGAT1Inhibitorinhibitorinhibit

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LU-32-176B

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