Powder: -20°C for 3 years | In solvent: -80°C for 1 year
A-77636 is a potent, selective, and long-acting oral dopamine D1 receptor agonist with an effective concentration (EC50) of 1.1 nM and a corresponding pEC50 value of 8.13. It demonstrates the highest affinity for the dopamine D1 receptor with a dissociation constant (Ki) of 39.8 nM and a pKi of 7.40 ± 0.09. Notably, A-77636 exhibits antiparkinsonian activity [1].
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
25 mg | 約6-8 週間 | ¥ 349,000 |
50 mg | 約6-8 週間 | ¥ 454,500 |
100 mg | 約6-8 週間 | ¥ 574,000 |
説明 | A-77636 is a potent, selective, and long-acting oral dopamine D1 receptor agonist with an effective concentration (EC50) of 1.1 nM and a corresponding pEC50 value of 8.13. It demonstrates the highest affinity for the dopamine D1 receptor with a dissociation constant (Ki) of 39.8 nM and a pKi of 7.40 ± 0.09. Notably, A-77636 exhibits antiparkinsonian activity [1]. |
ターゲット&IC50 | D1 receptor:1.1 nM (EC50), D1 receptor:39.8 nM (Ki) |
In vivo | A-77636 (0-3.2 μmol/kg, subcutaneous injection) induced rotational behavior in rats with 6-OHDA lesions (ED50 = 0.32 μmol/kg sc) [1]. The compound A-77636 (1-10 mg/kg) attenuated drug-induced locomotor activity in a dose-dependent manner [2]. A-77636 elicited forelimb clonus in rats (ED50 = 12.3 μmol/kg s.c.) and mice (ED50 = 12.1 μmol/kg s.c.) [1]. In marmosets treated with MPTP to induce a Parkinsonian state, A-77636 (0.5, 1.0, or 2.0 μmol/kg, oral administration) increased motor activity and reduced the severity of Parkinsonian symptoms, with the compound demonstrating activity following both subcutaneous and oral administration [1]. |
分子量 | 329.43 |
分子式 | C20H27NO3 |
CAS No. | 778546-51-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. 詳細
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A-77636 778546-51-3 GPCR/G Protein Neuroscience Dopamine Receptor Inhibitor inhibitor inhibit