规格

价格

库存

数量

25 mg

待询

3-6月

50 mg

待询

3-6月

100 mg

待询

3-6月

生物活性

产品描述	RTI-13951-33 hydrochloride is a potent, selective, and brain-penetrant GPR88 agonist. RTI-13951-33 hydrochloride exhibited an EC 50 of 25 nM in vitro cAMP functional assay. RTI-13951-33 hydrochloride significantly reduces alcohol reinforcement and intake behaviors in rats [1].
靶点活性	GPR88:（EC50）25 nM
体外活性	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 however not in membranes from GPR88 KO mice [1]. 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) but RTI-13951-33 poorly inhibits SERT (IC 50, 25.1±2.7 μM) [1].
体内活性	RTI-13951-33 (10 and 20 mg/kg, i.p.) decreases alcohol lever responses in a rat model of alcohol self-administration in a dose-dependent manner [1]. RTI-13951-33 (10 mg/kg, i.p.) shows sufficient brain penetration, with t 1/2 of 48 min and 87 min in rat plasma and brain [1].
别名	RTI-13951-33 hydrochloride (2244884-08-8 free base)

化学信息

分子量	532.5
分子式	C₂₈H₃₅Cl₂N₃O₃
Smiles	COCC1=CC=C(C2=CC=C(N(C[C@@H](N)[C@@H](C)OC)C([C@H]3[C@H](C4=CC=CC=N4)C3)=O)C=C2)C=C1.Cl.Cl
密度	no data available

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 125 mg/mL (234.74 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (6.2 mM), Sonication is recommeded.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO