(S)-N-((1-(5-(4-氟苯基)-2-甲基噻唑-4-羰基)哌啶-2-基)甲基)苯并呋喃-4-甲酰胺
SB-649868(SB-649868)
CAS: 380899-24-1
化学式: C26H24FN3O3S
| 中文名 | SB-649868 |
| 英文名 | SB-649868 |
| 别名 | 化合物SB-649868 (S)-N-((1-(5-(4-氟苯基)-2-甲基噻唑-4-羰基)哌啶-2-基)甲基)苯并呋喃-4-甲酰胺 |
| 英文别名 | CS-2650 SB649868 SB-649868 SB 649868 SB-649868, CID25195495 (S)-N-((1-(5-(4-Fluorophenyl)-2-methylthiazole-4-carbonyl)piperidin-2-yl)methyl)benzofuran-4-carboxamide N-[[(2S)-1-[[5-(4-Fluorophenyl)-2-methyl-4-thiazolyl]carbonyl]-2-piperidinyl]methyl]-4-benzofurancarboxamide 4-Benzofurancarboxamide, N-[[(2S)-1-[[5-(4-fluorophenyl)-2-methyl-4-thiazolyl]carbonyl]-2-piperidinyl]methyl]- N-[[(2S)-1-[5-(4-FLUOROPHENYL)-2-METHYL-1,3-THIAZOLE-4-CARBONYL]PIPERIDIN-2-YL]METHYL]-1-BENZOFURAN-4-CARBOXAMIDE |
| CAS | 380899-24-1 |
| 化学式 | C26H24FN3O3S |
| 分子量 | 477.55 |
| 密度 | 1.305±0.06 g/cm3(Predicted) |
| 沸点 | 725.1±55.0 °C(Predicted) |
| 溶解度 | DMSO |
| 酸度系数 | 14.54±0.46(Predicted) |
| 存储条件 | -20℃ |
| 体外研究 | SB-649868 is identified as one the most in vitro potent dual OX 1 and OX 2 receptor antagonist known at that time (pK i =9.4 and 9.5 at the OX 1 and OX 2 receptor, respectively) . SB-649868 antagonizes orexin-A-induced inositol 1 phosphate (IP1) accumulation with the following pK B value (OX 1 =9.67; OX 2 =9.64). SB-649868 displaces the [ 3 H]ACT-078573 receptor binding with the following pKi values: OX 1 =9.27; OX 2 =8.91. Increasing concentrations of SB-649868 (0.3 nM-30 nM) induces a rightward shift of the orexin-A CRCs with a depression of the agonist efficacy suggesting a clear non-surmountable behavior. The calculated apparent pK b values are 9.67±0.03 and 9.64±0.07 for OX 1 and OX 2 . |
| 体内研究 | Pharmacokinetic studies in the male CD rat, performed at 1 mg/kg, iv and 3 mg/kg, po, demonstrate an excellent pharmacokinetic profile for a hypnotic agent featuring moderate clearance in plasma (Cl p =24 mL/min/kg), short half-life of (<0.6 h) and a low volume of distribution (V ss =1.1 l/kg), coupled with excellent oral bioavailability (F=85%) and good exposure in plasma (C max =333 ng/mL). A brain to blood ratio (B/B) of 0.1:1 is observed 1 h after iv administration, a value in line with the expected partition between the two compartments based on the lower tissue binding observed in vitro in brain tissues (fraction unbound/brain=5.28%) with respect to plasma proteins (fraction unbound/plasma=1.34%). SB-649868, administered orally 3 h before OX-A injection at doses of 1, 3 and 10 mg/kg, causes a dose-dependent reduction of OX-A induced grooming as measured by total time spent grooming and number of grooming bouts (p <0.01 at 3 and 10 mg/kg po) . From dissociation kinetic studies using [ 3 H]ACT-078573, the calculated long half-life, (t 1/2 ) supports the non-surmountability profile of SB-649868 (t 1/2 =35.91 min) at OX 1 orexin receptor. The long or moderately long t 1/2 values for SB-649868 at OX 2 orexin receptor (t 1/2 =8.09 min). |
(S)-N-((1-(5-(4-氟苯基)-2-甲基噻唑-4-羰基)哌啶-2-基)甲基)苯并呋喃-4-甲酰胺 - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.094 ml | 10.47 ml | 20.94 ml |
| 5 mM | 0.419 ml | 2.094 ml | 4.188 ml |
| 10 mM | 0.209 ml | 1.047 ml | 2.094 ml |
| 5 mM | 0.042 ml | 0.209 ml | 0.419 ml |
最后更新：2024-01-02 23:10:35
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产品名: (S)-N-((1-(5-(4-氟苯基)-2-甲基噻唑-4-羰基)哌啶-2-基)甲基)苯并呋喃-4-甲酰胺 去供应商网站查看 询盘CAS: 380899-24-1
产地: 北京
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规格: YS107686-250mg,YS107686-25mg,YS107686-100mg,YS107686-50mg
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库存: 一周左右
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产品描述: 产品覆盖：小分子化合物、分析对照品、染色试剂、生化试剂盒、细胞生物学、分子生物学、抗体、蛋白、多肽、ELISA试剂盒、微生物培养、化学合成、仪器耗材、CRO技术 更多
现货供应
产品名: (S)-N-((1-(5-(4-氟苯基)-2-甲基噻唑-4-羰基)哌啶-2-基)甲基)苯并呋喃-4-甲酰胺 去供应商网站查看 询盘CAS: 380899-24-1
产地: 北京
包装: 瓶
规格: YS107686-250mg,YS107686-25mg,YS107686-100mg,YS107686-50mg
价格: 电话、微信、QQ、邮件
库存: 一周左右
电话: 010-50973130
手机: 17801761073(微信同号)
电子邮件: 3193328036@qq.com
QQ: 3193328036
微信: 17801761073
产品描述: 产品覆盖：小分子化合物、分析对照品、染色试剂、生化试剂盒、细胞生物学、分子生物学、抗体、蛋白、多肽、ELISA试剂盒、微生物培养、化学合成、仪器耗材、CRO技术 更多
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