Talsaclidine
Based on 1 Customer Validation
Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes. Talsaclidine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.75%
- CAS 番号: 147025-53-4
- 分子式: C10H15NO
- 分子量:165.24
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保管条件:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
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mAChR2 |
mAChR3 |
|
Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
2696 nM
Compound: Talsaclidine
|
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
|
[PMID: 26299349] |
| CHO | EC50 |
422 nM
Compound: Talsaclidine
|
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
|
[PMID: 26299349] |
| CHO | EC50 |
820 nM
Compound: Talsaclidine
|
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
|
[PMID: 26299349] |
| CHO | EC50 |
844 nM
Compound: Talsaclidine
|
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
|
[PMID: 26299349] |
| CHO | EC50 |
849 nM
Compound: Talsaclidine
|
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
|
[PMID: 26299349] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 147025-53-4
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性状 Liquid (Density: 1.06±0.1 g/cm3)
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分子量 165.24
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分子式 C10H15NO
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Color Light yellow to brown
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SMILES
C#CCO[C@@H]1[C@@H]2CCN(CC2)C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 5 mg/mL (30.26 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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (269 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
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- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Ensinger HA, et al. WAL 2014--a muscarinic agonist with preferential neuron-stimulating properties. Life Sci. 1993;52(5-6):473-80. [Content Brief]
[2]. Wienrich M, et al. Pharmacodynamic profile of the M1 agonist talsaclidine in animals and man. Life Sci. 2001 Apr 27;68(22-23):2593-600. [Content Brief]
[3]. Walland A, et al. In vivo consequences of M1-receptor activation by talsaclidine. Life Sci. 1997;60(13-14):977-84. [Content Brief]
[4]. Walland A, et al. Compensation of muscarinic bronchial effects of talsaclidine by concomitant sympathetic activation in guinea pigs. Eur J Pharmacol. 1997 Jul 9;330(2-3):213-9. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 6.0518 mL | 30.2590 mL | 60.5180 mL | 151.2951 mL |
| 5 mM | 1.2104 mL | 6.0518 mL | 12.1036 mL | 30.2590 mL | |
| 10 mM | 0.6052 mL | 3.0259 mL | 6.0518 mL | 15.1295 mL | |
| 15 mM | 0.4035 mL | 2.0173 mL | 4.0345 mL | 10.0863 mL | |
| 20 mM | 0.3026 mL | 1.5130 mL | 3.0259 mL | 7.5648 mL | |
| 25 mM | 0.2421 mL | 1.2104 mL | 2.4207 mL | 6.0518 mL | |
| 30 mM | 0.2017 mL | 1.0086 mL | 2.0173 mL | 5.0432 mL |