192703-06-3
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- CAS号:
- 192703-06-3
- 英文名:
- SR 144528
- 英文别名:
- SR 144528;SR-144528,SR144528;5-(4-Chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-1H-pyrazole-3-carboxamide;1H-Pyrazole-3-carboxamide, 5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-
- 中文名:
- 192703-06-3
- 中文别名:
- 化合物 T16928
- CBNumber:
- CB82592587
- 分子式:
- C29H34ClN3O
- 分子量:
- 476.05
- MOL File:
- 192703-06-3.mol
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192703-06-3化学性质
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沸点:
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627.7±55.0 °C(Predicted)
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密度:
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1.22±0.1 g/cm3(Predicted)
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储存条件:
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-20°C
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溶解度:
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Soluble in DMSO (up to 20 mg/ml, with warming).
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形态:
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powder
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酸度系数(pKa):
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11.52±0.60(Predicted)
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颜色:
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white to beige
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稳定性:
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Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
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192703-06-3性质、用途与生产工艺
SR144528 是一个有效且选择性的 CB2 受体拮抗剂，其 Ki 值为 0.6 nM。
Ki: 0.6 nM (CB2 receptor)
SR144528 is a potent and selective CB2 receptor antagonist with a K
i
of 0.6 nM. SR144528 alone is able to stimulate in a concentration-dependent manner (EC
50
=26±6 nM, two experiments) the forskolin-sensitive adenylyl cyclase activity in CHO-CB2 cells with a maximum effect at 1 μM (4-fold stimulation) whereas at this concentration it has no significant effect on CHO-CB1 cells (15% inhibition). Raw 264.7 macrophages supplemented with SR144528 display reduced caspase-3 activity. SR144528 inhibits microsomal acyl-coenzymeA:cholesterol acyltransferase (ACAT) activity in a concentration-dependent manner with an IC
50
value of 3.6±1.1 μM. At 10 μM, SR144528 inhibits ACAT activities ~68%.
No effect on the binding of [
3
H]-CP 55,940 to its specific sites in the brain is observed after either oral (up to 10 mg/kg) or i.c.v. (10 μg/animal) administration of SR144528 in mice. The occupancy by SR144528 of the spleen cannabinoid receptor is time-dependent and significant for at least 18 hours after oral administration at 3 mg/kg. SR144528 does not induce any significant effect on gastrointestinal (GI) motility when given alone. SR144528 does not block but enhances delayedgastric emptying.
192703-06-3
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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 |
|---|
| 2024/01/25 | HY-13439 | SR144528 | | 1 mg | 396元 |
| 2024/01/25 | HY-13439 | 192703-06-3
SR144528 | 192703-06-3 | 5mg | 990元 |
192703-06-3, 192703-06-3 相关搜索:
- 合成有机化合物配体
- C29H34ClN3O
- 化合物 T16928
- 192703-06-3
- SR-144528,SR144528
- 1H-Pyrazole-3-carboxamide, 5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-
- 5-(4-Chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-1H-pyrazole-3-carboxamide
- SR 144528