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规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5mg | ¥1654.00 | 现货 | |
10mg | ¥2647.00 | 现货 |
特色产品
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- 可将信号灵敏度提高100倍
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- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
产品描述
FAUC-365 is a D3 dopamine receptor agonist.
The dopamine D3 receptor, first identified in 1990, is preferentially expressed in the nucleus accumbens, where dopamine is released by neurons originating from the ventral tegmental area. Convincing pharmacological studies implicate D3-mediated neurotransmission in the reinforcing effects of cocaine. It is therefore a target for drugs which treat drug addiction, schizophrenia, as well as Parkinson's disease.
In vitro: FAUC-365 was discovered by a rational and interactive SAR sequence. As a dichloro derivative, FAUC-365 revealed D3 affinities that were comparable to its methoxy-substituted analogues, however, the selectivities of FAUC-365 against 5HT-1A, 5-HT2, and R1 were substantially higher, which was demonstrated by that extraordinary selectivity ratios of 17600, 7200, 5200, and 680 over D1, D2long, D2short, and D4, respectively, were determined for FAUC-365 with Ki of 0.50 nM. In addition, the benzothiophene analog FAUC 346 and its oxa analogue showed partial agonist character with EC50 values at 0.36 and 1.5 nM, respectively [1].
In vivo: Up to now, there is no animal in vivo data reported for FAUC-365.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Bettinetti L, Schlotter K, Hübner H, Gmeiner P. Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists. J Med Chem. 2002 Oct 10;45(21):4594-7.
产品性质
CAS号 | 474432-66-1 |
分子式 | C23H25CI2N3OS |
分子量 | 462.4 |
化学名称 | N-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butyl]-benzo[b]thiophene-2-carboxamide |
溶解度 | insoluble in EtOH; insoluble in H2O; ≥5.79 mg/mL in DMSO |
SMILES | ClC1=C(Cl)C(N2CCN(CCCCNC(C3=CC4=C(C=CC=C4)S3)=O)CC2)=CC=C1 |
存储条件 | -20°C |
运输条件 | 蓝冰 |
SDF文件 | Download SDF |