TACA
Based on 1 Customer Validation
TACA (trans-4-Aminocrotonic acid) is a potent agonist of GABAA and GABAC receptors (KD= 0.6 μM). TACA also is GABA uptake inhibitor and substrate for GABA-T. TACA produces late biphasic responses in the MPG neurons.
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- 純度: 99.33%
- CAS 番号: 38090-53-8
- 分子式: C4H7NO2
- 分子量:101.10
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
KD: 0.6 μM (GABAC)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Oocyte | EC50 |
0.4 μM
Compound: 44
|
Partial agonist activity against homomeric rho-2 subunit GABA-C receptor expressed in Xenopus oocytes
Partial agonist activity against homomeric rho-2 subunit GABA-C receptor expressed in Xenopus oocytes
|
[PMID: 10780899] |
| Oocyte | EC50 |
0.4 μM
Compound: TACA
|
Agonist activity at human GABAc Rho1 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
Agonist activity at human GABAc Rho1 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
|
[PMID: 18528996] |
| Oocyte | EC50 |
0.44 μM
Compound: 44
|
Partial agonist activity against human rho-1 subunit GABA-C receptor expressed in Xenopus oocytes
Partial agonist activity against human rho-1 subunit GABA-C receptor expressed in Xenopus oocytes
|
[PMID: 10780899] |
| Oocyte | EC50 |
0.6 μM
Compound: 44
|
Partial agonist activity against homomeric rho-1 subunit GABA-C receptor expressed in Xenopus oocytes
Partial agonist activity against homomeric rho-1 subunit GABA-C receptor expressed in Xenopus oocytes
|
[PMID: 10780899] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 38090-53-8
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性状 Solid
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分子量 101.10
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分子式 C4H7NO2
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Color Off-white to yellow
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SMILES
O=C(O)/C=C/CN
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別名
trans-4-Aminocrotonic acid
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
H2O : 20 mg/mL (197.82 mM; ultrasonic and warming and heat to 60°C)
DMSO : < 1 mg/mL (insoluble or slightly soluble)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 4 mg/mL (39.56 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
純度とドキュメンテーション
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データシート (268 KB)
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SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Chebib M, et al. Analogues of gamma-aminobutyric acid (GABA) and trans-4-aminocrotonic acid (TACA) substituted in the 2 position as GABAC receptor antagonists. Br J Pharmacol. 1997;122(8):1551-1560. [Content Brief]
[2]. Akasu T, et al. Role of GABAA and GABAC receptors in the biphasic GABA responses in neurons of the rat major pelvic ganglia. J Neurophysiol. 1999;82(3):1489-1496. [Content Brief]
[3]. Johnston GA, et al. Cis- and trans-4-aminocrotonic acid as GABA analogues of restricted conformation. J Neurochem. 1975;24(1):157-160. [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. 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 |
|---|---|---|---|---|---|
| H2O | 1 mM | 9.8912 mL | 49.4560 mL | 98.9120 mL | 247.2799 mL |
| 5 mM | 1.9782 mL | 9.8912 mL | 19.7824 mL | 49.4560 mL | |
| 10 mM | 0.9891 mL | 4.9456 mL | 9.8912 mL | 24.7280 mL | |
| 15 mM | 0.6594 mL | 3.2971 mL | 6.5941 mL | 16.4853 mL | |
| 20 mM | 0.4946 mL | 2.4728 mL | 4.9456 mL | 12.3640 mL | |
| 25 mM | 0.3956 mL | 1.9782 mL | 3.9565 mL | 9.8912 mL | |
| 30 mM | 0.3297 mL | 1.6485 mL | 3.2971 mL | 8.2427 mL | |
| 40 mM | 0.2473 mL | 1.2364 mL | 2.4728 mL | 6.1820 mL | |
| 50 mM | 0.1978 mL | 0.9891 mL | 1.9782 mL | 4.9456 mL | |
| 60 mM | 0.1649 mL | 0.8243 mL | 1.6485 mL | 4.1213 mL | |
| 80 mM | 0.1236 mL | 0.6182 mL | 1.2364 mL | 3.0910 mL | |
| 100 mM | 0.0989 mL | 0.4946 mL | 0.9891 mL | 2.4728 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.