DC Chemicals Limited
China
Product Name: Tracazolate hydrochloride
Price: $Inquiry/250mg $Inquiry/100mg $Inquiry/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

1135210-68-2

1135210-68-2 structure

Name: Tracazolate hydrochloride
Chemical Name: Tracazolate hydrochloride
CAS Number: 1135210-68-2
Molecular Formula: C₁₆H₂₅ClN₄O₂
Molecular Weight: 340.85
Catalog: Signaling Pathways Membrane Transporter/Ion Channel GABA Receptor
Create Date: 2021-01-09 18:53:41
Modify Date: 2024-01-14 17:21:38
Tracazolate hydrochloride (ICI 136753 hydrochloride) is a potent GABAA receptor modulator. Tracazolate hydrochloride potentiates α1β1γ2s (EC50=13.2 μM) and α1β3γ2 (EC50=1.5 μM) in a concentration-dependent manner. Tracazolate hydrochloride has the potency (EC50) is determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity[1][2].

Name	Tracazolate hydrochloride

Description	Tracazolate hydrochloride (ICI 136753 hydrochloride) is a potent GABAA receptor modulator. Tracazolate hydrochloride potentiates α1β1γ2s (EC50=13.2 μM) and α1β3γ2 (EC50=1.5 μM) in a concentration-dependent manner. Tracazolate hydrochloride has the potency (EC50) is determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity[1][2].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor Research Areas >> Neurological Disease Signaling Pathways >> Neuronal Signaling >> GABA Receptor
Target	GABAA[1]
In Vitro	Tracazolate hydrochloride (ICI 136753 hydrochloride) inhibits α1β1ε and α1β3ε GABAA receptors with IC50s of 4.0 μM, 1.2 μM, respectively. Replacement of Ser265 within the β1 subunit with Asn (the β3 counterpart) increases the sensitivity of tracazolate, whereas the opposite mutation (Asnβ3 to Ser) decreases the sensitivity to Tracazolate[1]. Tracazolate hydrochloride (10 μM) increases the maximum current amplitude and enhances the sensitivity of α1β2δ-containing GABAA receptors in oocytes[2].
References	[1]. Sally-Anne Thompson, et al. Tracazolate reveals a novel type of allosteric interaction with recombinant gamma-aminobutyric acid(A) receptors. Mol Pharmacol. 2002 Apr;61(4):861-9. [2]. N Zheleznova, et al. alpha1beta2delta, a silent GABA_A receptor: recruitment by tracazolate and neurosteroids. Br J Pharmacol. 2008 Mar;153(5):1062-71.

Molecular Formula	C₁₆H₂₅ClN₄O₂
Molecular Weight	340.85

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