1. GPCR/G Protein
  2. GPR88
  3. RTI-13951-33

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。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 RTI-13951-33 hydrochloride 通常具有更好的水溶性和稳定性。

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RTI-13951-33 Chemical Structure

RTI-13951-33 Chemical Structure

CAS No. : 2244884-08-8

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RTI-13951-33 的其他形式现货产品:

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RTI-13951-33 is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 reduces alcohol reinforcement and intake behaviors in rats[1].

IC50 & Target

EC50: 25 nM (GPR88)[1]

体外研究
(In Vitro)

RTI-13951-33 is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 elevates [35S]-GTPγS binding (EC50, 535 nM) in mouse striatal membranes but not in membranes from GPR88 KO mice[1].
RTI-13951-33 has weak affinities at kappa opioid receptor (KOR; Ki, 2.29 μM), vesicular monoamine transporter (VMAT; Ki, 4.23 μM), and moderate affinity at serotonin transporter (SERT; Ki, 0.75 μM), however, RTI-13951-33 poorly inhibits SERT (IC50, 25.1 ± 2.7 μM)[1].

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

体内研究
(In Vivo)

RTI-13951-33 (10 mg/kg, i.p.) has sufficient brain penetration, with t1/2 of 48 min and 87 min in rat plasma and brain[1].
RTI-13951-33 (10 and 20 mg/kg, i.p.) dose-dependently decreases alcohol lever responses in a rat model of alcohol self-administration[1].

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

分子量

459.58

Formula

C28H33N3O3

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

RTI-13951-33 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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RTI-13951-33
目录号:
HY-112612
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