1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. GABA Receptor
  3. Tracazolate hydrochloride

Tracazolate hydrochloride  (Synonyms: ICI 136753 hydrochloride)

Cat. No.: HY-B1803A Purity: 99.03%
COA Handling Instructions

Tracazolate (ICI 136753) hydrochloride is a potent GABAA receptor modulator. Tracazolate hydrochloride has selectivity for β3 and potentiates α1β1γ2s (EC50=13.2 μM), α1β3γ2 (EC50=1.5 μM). Tracazolate hydrochloride has the potency (EC50) determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity.

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

Tracazolate hydrochloride Chemical Structure

Tracazolate hydrochloride Chemical Structure

CAS No. : 1135210-68-2

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5 mg USD 74 In-stock
10 mg USD 119 In-stock
25 mg USD 252 In-stock
50 mg USD 400 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Tracazolate (ICI 136753) hydrochloride is a potent GABAA receptor modulator. Tracazolate hydrochloride has selectivity for β3 and potentiates α1β1γ2s (EC50=13.2 μM), α1β3γ2 (EC50=1.5 μM). Tracazolate hydrochloride has the potency (EC50) 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].

IC50 & Target

GABAA[1]

In Vitro

Tracazolate (ICI 136753) hydrochloride inhibits α1β1ε (EC50=4.0 μM) and α1β3ε (EC50=1.2 μM), α1β3 (EC50=2.7 μM) and α6β3γ (EC50=1.1 μM). 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. Tracazolate hydrochloride interacts with γ-aminobutyric acid GABAA receptors, adenosinereceptors, and phosphodiesterases[1].
Tracazolate hydrochloride (10 μM) increases the maximum current amplitude and enhances the sensitivity of α1β2δ-containing GABAA receptors in oocytes[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

340.85

Formula

C16H25ClN4O2

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=C(C)N=C(N(CC)N=C2)C2=C1NCCCC)OCC.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°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: 

DMSO : 125 mg/mL (366.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9338 mL 14.6692 mL 29.3384 mL
5 mM 0.5868 mL 2.9338 mL 5.8677 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9338 mL 14.6692 mL 29.3384 mL 73.3460 mL
5 mM 0.5868 mL 2.9338 mL 5.8677 mL 14.6692 mL
10 mM 0.2934 mL 1.4669 mL 2.9338 mL 7.3346 mL
15 mM 0.1956 mL 0.9779 mL 1.9559 mL 4.8897 mL
20 mM 0.1467 mL 0.7335 mL 1.4669 mL 3.6673 mL
25 mM 0.1174 mL 0.5868 mL 1.1735 mL 2.9338 mL
30 mM 0.0978 mL 0.4890 mL 0.9779 mL 2.4449 mL
40 mM 0.0733 mL 0.3667 mL 0.7335 mL 1.8337 mL
50 mM 0.0587 mL 0.2934 mL 0.5868 mL 1.4669 mL
60 mM 0.0489 mL 0.2445 mL 0.4890 mL 1.2224 mL
80 mM 0.0367 mL 0.1834 mL 0.3667 mL 0.9168 mL
100 mM 0.0293 mL 0.1467 mL 0.2934 mL 0.7335 mL
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Tracazolate hydrochloride Related Classifications

Help & FAQs
  • 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.

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Tracazolate hydrochloride
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