他拉罗唑
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- CAS号:
- 201410-53-9
- 英文名:
- R 115866
- 英文别名:
- R 115866;RaMbazole;RAMBAZOLE;R115866;R-115866;R 115866;N-[4-[2-Ethyl-1-(1H-1,2,4-triazol-1-yl)butyl]phenyl]-2-benzothiazolamine;N-[4-[2-ethyl-1-(1,2,4-triazol-1-yl)butyl]phenyl]-1,3-benzothiazol-2-amine;N-(4-(2-Ethyl-1-(1H-1,2,4-triazol-1-yl)butyl)phenyl)benzo[d]thiazol-2-amine);Retinoid X receptors,R 115866,Retinoic acid receptors,RAR/RXR,inhibit,Talarozole,Cytochrome P450,CYPs,Inhibitor,Autophagy,R-115866
- 中文名:
- 他拉罗唑
- 中文别名:
- N-(4-(2-乙基-1-(1H-1,2,4-三唑-1-基)丁基)苯基)苯并[D]噻唑-2-胺
- CBNumber:
- CB52628344
- 分子式:
- C21H23N5S
- 分子量:
- 377.51
- MOL File:
- 201410-53-9.mol
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他拉罗唑化学性质
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沸点:
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561.0±60.0 °C(Predicted)
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密度:
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1.26±0.1 g/cm3(Predicted)
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储存条件:
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Keep in dark place,Sealed in dry,Store in freezer, under -20°C
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溶解度:
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Soluble in DMSO
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形态:
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Powder
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酸度系数(pKa):
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2.70±0.10(Predicted)
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他拉罗唑性质、用途与生产工艺
Talarozole (R115866) 是一种口服性全反式维甲酸代谢阻断剂 (RAMBA)，可提高内源性全反式维甲酸 (RA) 的细胞内水平。Talarozole 抑制 CYP26A1 和 CYP26B1，IC50 值分别为 5.4 和 0.46 nM。
IC50: 0.46/5.1 nM (CYP26B1/A1)
When HepG2 cells are cotreated with atRA and Talarozole (1 μM), 4-OH-RA and 4-oxo-RA formation is significantly decreased.
A maximum 84% inhibition of CYP26 activity at 0.5 hours post-dose is predicted based on Talarozole (TLZ) C
max
of 80 nM and a K
i
of 1 nM following a single dose of Talarozole. Due to the short Talarozole half-life (2.2 hrs) CYP26 activity is predicted to return to 100% by 12 hours. In agreement with the predictions,
at
RA concentrations are increased by 82, 63 and 60% at 4 hours post-dose in the serum, liver and testes, respectively, and concentrations returned to baseline by 24 hours. Following multiple doses of Talarozole, liver CYP26 mRNA and activity are increased suggesting autoinduction of CYP26 due to increased
at
RA concentrations. In agreement,
at
RA concentrations are elevated in serum and liver at all timepoints measured. This increase in
at
RA concentrations is associated with increased mRNA of the mitochondrial biogenesis markers PGC-1β and NRF-1 in comparison to control mice.
他拉罗唑
上下游产品信息
上游原料
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201410-53-9, 他拉罗唑 相关搜索:
- 对照品
- N-(4-(2-乙基-1-(1H-1,2,4-三唑-1-基)丁基)苯基)苯并[D]噻唑-2-胺
- 201410-53-9
- Retinoid X receptors,R 115866,Retinoic acid receptors,RAR/RXR,inhibit,Talarozole,Cytochrome P450,CYPs,Inhibitor,Autophagy,R-115866
- N-[4-[2-ethyl-1-(1,2,4-triazol-1-yl)butyl]phenyl]-1,3-benzothiazol-2-amine
- RAMBAZOLE;R115866;R-115866;R 115866
- N-(4-(2-Ethyl-1-(1H-1,2,4-triazol-1-yl)butyl)phenyl)benzo[d]thiazol-2-amine)
- N-[4-[2-Ethyl-1-(1H-1,2,4-triazol-1-yl)butyl]phenyl]-2-benzothiazolamine
- RaMbazole
- R 115866