(+)-Razpipadon
Based on 1 Customer Validation
(+)-Razpipadon ((+)-PW0464) is a selective D1 dopamine receptor agonist belonging to non-catechol compounds. (+)-Razpipadon activates the G protein pathway, while restricting β-arrestin coupling through the proximity effect of fluoromethyl-TM5, thereby achieving specific regulation of downstream pathways. (+)-Razpipadon can be used in studies related to Parkinson's disease.
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。
- CAS 番号: 1643489-51-3
- 分子式: C19H17F2N3O4
- 分子量:389.35
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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
Dopamine Receptor アイソフォーム固有の製品をすべて表示
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生物活性
|
D1 Receptor |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
12 nM
Compound: 24; PW0464
|
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
|
[PMID: 31098001] |
(+)-Razpipadon is a G protein-biased agonist of human D1R that activates the G protein signaling pathway. Its potency is slightly lower than that of Tavapadon (HY-119486), but it cannot effectively activate the β-arrestin pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1643489-51-3
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性状 Solid
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分子量 389.35
-
分子式 C19H17F2N3O4
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SMILES
O=C1NC(N(C)C(C2=C(C)C=C(OC3=NC=CC=C3OC(F)F)C=C2)=C1C)=O
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別名
(+)-PW0464
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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
DMSO : 100 mg/mL (256.84 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
参考文献
[1]. Teng X, et al. Ligand recognition and biased agonism of the D1 dopamine receptor. Nat Commun. 2022;13(1):3186. Published 2022 Jun 8. [Content Brief]
[3]. Kumar S, et al. Discovery and structure - activity relationships of 2,4,5-trimethoxyphenyl pyrimidine derivatives as selective D5 receptor partial agonists. Bioorg Chem. 2024;153:107809. [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 | 2.5684 mL | 12.8419 mL | 25.6838 mL | 64.2096 mL |
| 5 mM | 0.5137 mL | 2.5684 mL | 5.1368 mL | 12.8419 mL | |
| 10 mM | 0.2568 mL | 1.2842 mL | 2.5684 mL | 6.4210 mL | |
| 15 mM | 0.1712 mL | 0.8561 mL | 1.7123 mL | 4.2806 mL | |
| 20 mM | 0.1284 mL | 0.6421 mL | 1.2842 mL | 3.2105 mL | |
| 25 mM | 0.1027 mL | 0.5137 mL | 1.0274 mL | 2.5684 mL | |
| 30 mM | 0.0856 mL | 0.4281 mL | 0.8561 mL | 2.1403 mL | |
| 40 mM | 0.0642 mL | 0.3210 mL | 0.6421 mL | 1.6052 mL | |
| 50 mM | 0.0514 mL | 0.2568 mL | 0.5137 mL | 1.2842 mL | |
| 60 mM | 0.0428 mL | 0.2140 mL | 0.4281 mL | 1.0702 mL | |
| 80 mM | 0.0321 mL | 0.1605 mL | 0.3210 mL | 0.8026 mL | |
| 100 mM | 0.0257 mL | 0.1284 mL | 0.2568 mL | 0.6421 mL |