1. GPCR/G Protein Neuronal Signaling
  2. Cannabinoid Receptor
  3. AM12814

AM12814 是一种强效的部分 CB1CB2 激动剂,其 Ki 值分别为 0.7 nM 和 3.4 nM。AM12814 能够抑制 cAMP 的积累,并募集 β-arrestin 2。AM12814 具有拟大麻效应。AM12814 可用于神经系统疾病的研究,如僵住症。

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AM12814

AM12814 Chemical Structure

CAS No. : 3054511-18-8

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生物活性

AM12814 is a potent and partial CB1 and CB2 agonist with Ki values of 0.7 nM and 3.4 nM. AM12814 can inhibit cAMP accumulation and recruitse β-arrestin 2. AM12814 exhibits cannabimimetic effects. AM12814 can be used for the research of neurological disease, suah as catalepsy[1].

IC50 & Target[1]

rCB1-R

0.7 nM (Ki)

hCB2-R

3.4 nM (Ki)

体外研究
(In Vitro)

AM12814 (Compound 12) 以高亲和力与大麻素受体结合,其 Ki 值分别为 0.7 nM (rCB1) 和 3.4 nM (hCB2)[1]
AM12814 (30 mins) 可抑制 Forskolin (HY-15371) 刺激的 3xHA-hCB1-CHO 细胞和 3xHA-hCB2-CHO 细胞中 cAMP 的积累,EC50 值分别为 8.75 nM 和 22 nM[1]
AM12814 (90 mins) 在 hCB1-DRx-CHO 细胞和 hCB2-DRx-U2OS 细胞中募集 β-arrestin 2,EC50 值分别为 25 nM 和 5.6 nM[1]

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

体内研究
(In Vivo)

AM12814 (Compound 12) (0.3-3 mg/kg,腹腔注射) 在 CD1 小鼠中诱导由 CB1 介导的拟大麻行为[1]

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

Animal Model: CD1 mice[1]
Dosage: 0.3, 1 and 3 mg/kg
Administration: Intraperitoneally injection
Result: Increased immobility time in the ring test.
Reduced core body temperature.
Prolonged tail-flick latency in the hot water test.
Alleviated CFA (HY-153808)-induced mechanical hypersensitivity.
分子量

429.56

Formula

C24H38F3NO2

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
  • 摩尔计算器

  • 稀释计算器

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

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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)
× = ×
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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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产品名称:
AM12814
目录号:
HY-178203
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