RTI-13951-33
- CAS号:2244884-08-8
- 英文名:RTI-13951-33
- 中文名:RTI-13951-33
- CBNumber:CB94668465
- 分子式:C28H33N3O3
- 分子量:459.58
- MOL File:2244884-08-8.mol
- 沸点 :637.3±55.0 °C(Predicted)
- 密度 :1.181±0.06 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :Soluble in DMSO
- 酸度系数(pKa) :6.99±0.13(Predicted)
RTI-13951-33性质、用途与生产工艺
- 生物活性 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。
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靶点
EC50: 25 nM (GPR88)
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体外研究
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). -
体内研究
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.
- 公司名称:TargetMol Chemicals Inc.
- 联系电话:+1-781-999-5354 +1-00000000000
- 电子邮件:marketing@targetmol.com
- 国家:美国
- 产品数:19892
- 优势度:58
- 公司名称:MedChemExpress
- 联系电话:--
- 电子邮件:sales@medchemexpress.com
- 国家:美国
- 产品数:6398
- 优势度:58