2. GPCR/G Protein
  3. GPR88
  4. RTI-122 dihydrochloride

RTI-122 dihydrochloride 是一种具有血脑屏障通透性的 GPR88 激动剂。RTI-122 dihydrochloride 可通过增加 cAMP 积累及 GTPγS 结合活性，激活 GPR88 介导的 G 蛋白信号通路。RTI-122 dihydrochloride 可减弱啮齿类动物的狂饮样饮酒行为、减少酒精摄入、降低操作性酒精自饮行为及酒精摄入动机，并可抑制觅酒行为复燃。RTI-122 dihydrochloride 可用于酒精使用障碍的相关研究。

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RTI-122 dihydrochloride

RTI-122 dihydrochloride Chemical Structure

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规格 价格 是否有货 数量
1 mg ￥2400
In-stock
5 mg ￥4640
In-stock
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100 mg   询价  

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Customer Review

Other Forms of RTI-122 dihydrochloride:

RTI-122 dihydrochloride 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RTI-122 dihydrochloride is a blood-brain barrier-permeable GPR88 agonist. RTI-122 dihydrochloride activates the G protein signaling pathway mediated by GPR88 by increasing cAMP accumulation and GTPγS binding activity. RTI-122 dihydrochloride attenuates binge-like drinking behavior, reduces alcohol intake, decreases operant alcohol self-administration and alcohol consumption motivation, and inhibits relapse of alcohol-seeking behavior in rodents. RTI-122 dihydrochloride is applicable to research related to alcohol use disorder[1][2].

体外研究
(In Vitro)

RTI-122 dihydrochloride (Compound 30a) 在稳定表达 PPLS-HA-GPR88 的 CHO 细胞中作为强效 GPR88 激动剂，在 cAMP 累积实验中的 EC50 为 10.8 nM[1]。
RTI-122 dihydrochloride 可在 PPLS-HA-hGPR88-CHO 细胞膜中强效激活人源 GPR88 介导的 G 蛋白信号通路，在[35S]GTPγS 结合实验中的 EC50 为 11.5 nM[1]。
RTI-122 dihydrochloride 在野生型小鼠纹状体膜中作为 GPR88 激动剂，在[35S]GTPγS 结合实验中的 EC50 为 155 nM，且在 GPR88 敲除小鼠纹状体膜中无活性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

RTI-122 dihydrochloride 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Tmax (Plasma) CL T1/2 AUC0-inf Tmax (Brain)
Mice[1] 10 mg/kg i.p. 662 ng/mL 2.0 h 23 mL/min/kg 5.8 h 7292 ng·h/mL 4.0 h
体内研究
(In Vivo)

RTI-122 dihydrochloride (10 mg/kg；腹腔注射；单次给药) 可显著减少雄性 C57BL/6J 小鼠在暗期饮酒范式中的狂饮样酒精摄入[1][2]。
RTI-122 dihydrochloride (2.5-20 mg/kg，腹腔注射，单次给药) 可剂量依赖性地减少雄性野生型 C57BL/6J 小鼠的自主活动[2]。
RTI-122 dihydrochloride (2.5-10 mg/kg；腹腔注射；单次给药) 减少嗜酒雌雄大鼠的操作性酒精自身给药行为，而对蔗糖自身给药无影响，对奖赏的调控具有酒精特异性，减少 Yohimbine (HY-N0127 ) 诱导的嗜酒雄鼠和雌鼠的酒精复吸行为[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J (male, 8−9 weeks of age)[1]
Dosage: 10 mg/kg
Administration: i.p.; single dose
Result: Significantly reduced binge-like alcohol intake compared to saline controls, with magnitude matching that of reference compound RTI-13951-33 at 30 mg/kg dose.
Showed no effect on water intake.
Animal Model: C57BL/6J (male, 3-5 months old, 25-35 g)[2]
Dosage: 2.5 mg/kg; 5 mg/kg; 10 mg/kg; 20 mg/kg
Administration: i.p.; single dose
Result: Reduced spontaneous locomotion dose-dependently during the first 20 min post-injection, with significant effects at 10 mg/kg and 20 mg/kg.
Reduced locomotion only at 20 mg/kg during the 20-40 min period.
Showed no effects on locomotion during the 40-60 min period.
Animal Model: alcohol-preferring (P) (male and female)[2]
Dosage: 2.5 mg/kg; 5 mg/kg; 10 mg/kg
Administration: i.p.; single dose
Result: Reduced alcohol lever responses with significant reductions at 5 mg/kg and 10 mg/kg.
Reduced alcohol intake with significant reductions at 5 mg/kg and 10 mg/kg.
Reduced locomotor rate at 10 mg/kg during alcohol self-administration testing.
Showed no effect on sucrose lever responses or sucrose intake.
Reduced locomotor rate at 10 mg/kg during sucrose self-administration testing.
Reduced lever responding in the seeking phase at 20 mg/kg.
Reduced lever responding in the reinitiation phase at both 10 mg/kg and 20 mg/kg.
Reduced locomotor rate during the seeking phase at both doses.
分子量

564.52

Formula

C29H36Cl2FN3O3
性状

固体

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

H2O 中的溶解度 : 100 mg/mL (177.14 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7714 mL 8.8571 mL 17.7142 mL
5 mM 0.3543 mL 1.7714 mL 3.5428 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
纯度 & 产品资料
参考文献

RTI-122 dihydrochloride 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 1.7714 mL 8.8571 mL 17.7142 mL 44.2854 mL
5 mM 0.3543 mL 1.7714 mL 3.5428 mL 8.8571 mL
10 mM 0.1771 mL 0.8857 mL 1.7714 mL 4.4285 mL
15 mM 0.1181 mL 0.5905 mL 1.1809 mL 2.9524 mL
20 mM 0.0886 mL 0.4429 mL 0.8857 mL 2.2143 mL
25 mM 0.0709 mL 0.3543 mL 0.7086 mL 1.7714 mL
30 mM 0.0590 mL 0.2952 mL 0.5905 mL 1.4762 mL
40 mM 0.0443 mL 0.2214 mL 0.4429 mL 1.1071 mL
50 mM 0.0354 mL 0.1771 mL 0.3543 mL 0.8857 mL
60 mM 0.0295 mL 0.1476 mL 0.2952 mL 0.7381 mL
80 mM 0.0221 mL 0.1107 mL 0.2214 mL 0.5536 mL
100 mM 0.0177 mL 0.0886 mL 0.1771 mL 0.4429 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RTI-122RTI122RTI 122GPR88G Protein-Coupled Receptor 88GPR88 agonistalcohol use disorderC57BL/6Jmicealcohol-preferring ratInhibitorinhibitorinhibit

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