SB-649868
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- CAS号:
- 380899-24-1
- 英文名:
- SB-649868
- 英文别名:
- CS-2650;SB-649868;GSK649868;SB649868; 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;GSK 649868,Inhibitor,SB-649868,HCRT Receptor,GSK-649868,Orexin Receptor (OX Receptor),Hypocretin Receptor,SB 649868,inhibit,SB649868
- 中文名:
- SB-649868
- 中文别名:
- 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
- CBNumber:
- CB62628381
- 分子式:
- C26H24FN3O3S
- 分子量:
- 477.55
- MOL File:
- 380899-24-1.mol
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SB-649868化学性质
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沸点:
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725.1±55.0 °C(Predicted)
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密度:
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1.305±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMF: 15mg/mL; DMF:PBS (pH 7.2) (1:20): 0.04mg/mL; DMSO: 10mg/mL; Ethanol: 0.3mg/mL
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形态:
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A crystalline solid
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酸度系数(pKa):
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14.54±0.46(Predicted)
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SB-649868性质、用途与生产工艺
SB-649868 是一种口服有效的选择性食欲素 OX1 和 OX 2 受体拮抗剂 (作用于 OX1 和 OX2 受体,pKi 分别为 9.4 和 9.5)。
pKi: 9.4 (OX
1
), 9.5 (OX
2
)
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
.
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).
SB-649868
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下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
---|
2024/04/30 | HY-10806 | SB-649868 SB-649868 | 380899-24-1 | 10mg | 2400元 |
2024/04/30 | HY-10806 | SB-649868 SB-649868 | 380899-24-1 | 25mg | 5100元 |
380899-24-1, SB-649868 相关搜索:
3-苯基磺酰基-8-(哌嗪-1-基)喹啉 N/A INARIGIVIRSOPROXIL 化合物SB-265610 SBI-993;SBI993;SBI993 14-甲基-20-氧杂-5,7,14,27-四氮杂四环[19.3.1.1(2,6).1(8,12)]二十七碳-1(25),2,4,6(27),8,10,12(26),16,21,23-十烯 4-(4-氟苯基)-2-(4-甲基亚磺酰基苯基)-5-(4-吡啶基)-1H-咪唑 SB204741 N/A
- 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
- 380899-24-1
- GSK 649868,Inhibitor,SB-649868,HCRT Receptor,GSK-649868,Orexin Receptor (OX Receptor),Hypocretin Receptor,SB 649868,inhibit,SB649868
- GSK649868
- (S)-N-((1-(5-(4-Fluorophenyl)-2-methylthiazole-4-carbonyl)piperidin-2-yl)methyl)benzofuran-4-carboxamide
- 4-Benzofurancarboxamide, N-[[(2S)-1-[[5-(4-fluorophenyl)-2-methyl-4-thiazolyl]carbonyl]-2-piperidinyl]methyl]-
- CS-2650
- SB649868; SB 649868
- SB-649868, CID25195495
- N-[[(2S)-1-[5-(4-FLUOROPHENYL)-2-METHYL-1,3-THIAZOLE-4-CARBONYL]PIPERIDIN-2-YL]METHYL]-1-BENZOFURAN-4-CARBOXAMIDE
- N-[[(2S)-1-[[5-(4-Fluorophenyl)-2-methyl-4-thiazolyl]carbonyl]-2-piperidinyl]methyl]-4-benzofurancarboxamide
- SB-649868