2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Dopamine Receptor 5-HT Receptor Histamine Receptor Arrestin
  4. UNC9994

UNC9994 是 Aripiprazole 的类似物，是一种功能选择性 β-阻遏蛋白偏向的多巴胺 D2 受体(β-arrestin-biased dopamine D2 receptor) 激动剂，对于 β-阻遏蛋白-2 向 D2 受体的募集的 EC50 <10 nM。UNC9994 同时是 β-arrestin-2 易位的部分激动剂和 Gi 调节的 cAMP 产生的拮抗剂。具有抗精神病活性。

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UNC9994 Chemical Structure

UNC9994 Chemical Structure

CAS No. : 1354030-51-5

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规格 价格 是否有货 数量
1 mg ￥1560
In-stock
5 mg ￥3125
In-stock
10 mg ￥4375
In-stock
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Customer Review

Other Forms of UNC9994:

UNC9994 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

查看 Dopamine Receptor 亚型特异性产品:

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Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

查看 5-HT Receptor 亚型特异性产品:

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

查看 Histamine Receptor 亚型特异性产品:

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC50 <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of Gi-regulated cAMP production. Antipsychotic Activity[1].

IC50 & Target[1]

D2 Receptor

79 nM (Ki)

D3 Receptor

17 nM (Ki)

D4 Receptor

138 nM (Ki)

5-HT2A Receptor

140 nM (Ki)

5-HT2B Receptor

25 nM (Ki)

5-HT2C Receptor

512 nM (Ki)

5-HT1F Receptor

26 nM (Ki)

H1 Receptor

2.1 nM (Ki)

体外研究
(In Vitro)

UNC9994 displays a lower binding affinity (Ki=79 nM) to D2R than UNC9975, UNC0006, and aripiprazole. At serotonin (as known as 5-HT) receptors, UNC9994 displays moderate to high binding affinities (Ki=25-512 nM) for 5HT2A, 5HT2B, 5HT2C, and 5HT1A, but is significantly less potent in functional assays (Ca2+ mobilization FLIPR or cAMP biosensor). UNC9994 is an antagonist at 5HT2A and 5HT2B and agonists at 5HT2C and 5HT1A. UNC9994 has relatively high affinities to H1-histamine receptor (Ki=2.4 nM) but is less potent antagonists in H1 functional assays[1].

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

UNC9994 相关抗体:
体内研究
(In Vivo)

The antipsychotic-like activity displayed by UNC9994 (2 mg/kg; i.p.) in wild-type mice is completely abolished in β-arrestin-2 knockout mice[1].

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

Animal Model: C57BL/6J wild-type and β-arrestin-2 knockout mice (phencyclidine-induced hyperlocomotion)[1]
Dosage: 2 mg/kg
Administration: I.p. followed 30 min later with 6 mg/kg phencyclidine
Result: Markedly inhibited PCP-induced hyperlocomotion in wild-type mice. This significant antipsychotic-like activity of UNC9994 was completely abolished in β-arrestin-2 knockout mice.
分子量

421.38

Formula

C21H22Cl2N2OS
CAS 号
性状

固体

颜色

White to off-white

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
纯度 & 产品资料
参考文献

UNC9994 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 *
= × ×

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.

Keywords:

UNC99941354030-51-5UNC 9994UNC-9994Dopamine Receptor5-HT ReceptorHistamine ReceptorArrestinSerotonin Receptor5-hydroxytryptamine Receptorantipsychoticβ-arrestinligandprobeselectivecAMPproductionInhibitorinhibitorinhibit

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