Tracazolate hydrochloride
Based on 1 Customer Validation
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.
- Purity: 99.24%
- CAS No.: 1135210-68-2
- Formula: C16H25ClN4O2
- Molecular Weight:340.85
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
GABAA[1]
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.
Chemical Information
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CAS No. 1135210-68-2
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Appearance Solid
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Molecular Weight 340.85
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Formula C16H25ClN4O2
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Color Off-white to light yellow
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SMILES
O=C(C1=C(C)N=C(N(CC)N=C2)C2=C1NCCCC)OCC.[H]Cl
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Synonyms
ICI 136753 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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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
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[2]. N Zheleznova, et al. alpha1beta2delta, a silent GABAA receptor: recruitment by tracazolate and neurosteroids. Br J Pharmacol. 2008 Mar;153(5):1062-71. [Content Brief]
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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