[CAS NO. 145821-59-6] Tiagabine hydrochloride

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PRODUCTS SPECIFICATIONS [145821-59-6]

Catalog

HY-B0696A

Brand

MCE

CAS

145821-59-6

DESCRIPTION [145821-59-6]

Overview

MDL	MFCD07369025
Molecular Weight	412.01
Molecular Formula	C20H26ClNO2S2
SMILES	O=C([C@H]1CN(CC/C=C(C2=C(C)C=CS2)/C3=C(C)C=CS3)CCC1)O.[H]Cl

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

Summary

Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC ₅₀ s of 67, 446 and 182 nM for [ ³ H]GABA uptake in Synaptosomes, Neurons and Glia, respectively ^[1] .

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00086255	National Institute on Drug Abuse (NIDA)\|University of Cincinnati	Cocaine-Related Disorders	October 2002	Phase 2
NCT00179465	Beth Israel Deaconess Medical Center\|Dartmouth-Hitchcock Medical Center	Schizophrenia	November 2003	Phase 3
NCT00129298	National Institute on Drug Abuse (NIDA)	Cocaine-Related Disorders\|Opiate Dependence	December 2004	Phase 2
NCT02387710	Brigham and Women´s Hospital	Sleep Apnea, Obstructive	March 2015	Phase 2
NCT03196466	Assistance Publique - Hôpitaux de Paris	Epilepsy	June 19, 2017
NCT01904487	Rajesh Narendran\|University of Pittsburgh	Alcoholism	April 19, 2011	Phase 1

Appearance

Solid

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:

H ₂ O : 100 mg/mL ( 242.71 mM ; Need ultrasonic)

DMSO : ≥ 53 mg/mL ( 128.64 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4271 mL	12.1356 mL	24.2713 mL
5 mM	0.4854 mL	2.4271 mL	4.8543 mL
10 mM	0.2427 mL	1.2136 mL	2.4271 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (5.05 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (5.05 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (5.05 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

3-Piperidinecarboxylic acid, 1-[4,4-bis(3-methyl-2-thienyl)-3-buten-1-yl]-, hydrochloride (1:1), (3R)-

3-Piperidinecarboxylic acid, 1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-, hydrochloride, (R)-

3-Piperidinecarboxylic acid, 1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-, hydrochloride, (3R)-

Tiagabine hydrochloride

Abbott 70569.1

Abbott 70569 hydrochloride

ABT 569

NO 05-0328

NNC 05-0328

Tiabex

Gabitril

(3R)-1-[4,4-Bis(3-methylthien-2-yl)-3-butenyl]piperidine-3-carboxylic acid hydrochloride

(3R)-1-[4,4-Bis(3-methylthiophen-2-yl)but-3-en-1-yl]piperidine-3-carboxylic acid hydrochloride