RTI-13951-33
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- CAS号:
- 2244884-08-8
- 英文名:
- RTI-13951-33
- 英文别名:
- RTI-13951-33;RTI1395133,RTI 13951 33;Cyclopropanecarboxamide, N-[(2R,3R)-2-amino-3-methoxybutyl]-N-[4'-(methoxymethyl)[1,1'-biphenyl]-4-yl]-2-(2-pyridinyl)-, (1R,2R)-
- 中文名:
- RTI-13951-33
- 中文别名:
- 化合物 T12778L;化合物 RTI-13951-33
- CBNumber:
- CB94668465
- 分子式:
- C28H33N3O3
- 分子量:
- 459.58
- MOL File:
- 2244884-08-8.mol
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RTI-13951-33化学性质
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沸点:
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637.3±55.0 °C(Predicted)
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密度:
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1.181±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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Soluble in DMSO
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酸度系数(pKa):
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6.99±0.13(Predicted)
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RTI-13951-33性质、用途与生产工艺
RTI-13951-33 是一种有效、选择性、可透过血脑屏障的 GPR88 激动剂，在 GPR88 cAMP 功能性实验中，EC50 值为 25 nM。RTI-13951-33 可以减少大鼠酒精强化和摄取行为。
RTI-13951-33 is a potent, selective, and brain-penetrant GPR88 agonist, with an EC
50
of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 elevates [
35
S]-GTPγS binding (EC
50
， 535 nM) in mouse striatal membranes but not in membranes from GPR88 KO mice.
RTI-13951-33 has weak affinities at kappa opioid receptor (KOR; K
i
, 2.29 μM), vesicular monoamine transporter (VMAT; K
i
, 4.23 μM), and moderate affinity at serotonin transporter (SERT; K
i
, 0.75 μM), however, RTI-13951-33 poorly inhibits SERT (IC
50
, 25.1 ± 2.7 μM).
RTI-13951-33 (10 mg/kg, i.p.) has sufficient brain penetration, with t
1/2
of 48 min and 87 min in rat plasma and brain.
RTI-13951-33 (10 and 20 mg/kg, i.p.) dose-dependently decreases alcohol lever responses in a rat model of alcohol self-administration.
RTI-13951-33
上下游产品信息
上游原料
下游产品
2244884-08-8, RTI-13951-33 相关搜索:
- 抑制剂
- 化合物 RTI-13951-33
- 化合物 T12778L
- 2244884-08-8
- Cyclopropanecarboxamide, N-[(2R,3R)-2-amino-3-methoxybutyl]-N-[4'-(methoxymethyl)[1,1'-biphenyl]-4-yl]-2-(2-pyridinyl)-, (1R,2R)-
- RTI1395133,RTI 13951 33
- RTI-13951-33