2. GPCR/G Protein Neuronal Signaling Cell Cycle/DNA Damage
  3. Cannabinoid Receptor PERK
  4. GAT100

GAT100 是一种大麻素 1 型受体 (CB1R) 负别构调节剂与共价别构探针。GAT100 可作为正构激动剂 CP55,940 结合的正别构调节剂调控 CB1R 信号通路。GAT100 可降低正构 CB1R 激动剂在 β-抑制蛋白 1 招募、PLCβ3 与 ERK1/2 磷酸化、cAMP 积累及 CB1R 内化方面的效力和效能。GAT100 可用于心理行为和躯体疾病的研究。

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GAT100

GAT100 Chemical Structure

CAS No. : 1663564-42-8

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GAT100 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GAT100 is a negative allosteric modulator and covalent allosteric probe for cannabinoid receptor type 1 (CB1R). GAT100 acts as a positive allosteric modulator for orthosteric agonist CP55,940 binding to regulate the CB1R signaling pathway. GAT100 reduces the potency and efficacy of orthosteric CB1R agonists in terms of β-arrestin 1 recruitment, phosphorylation of PLCβ3 and ERK1/2, cAMP accumulation, and CB1R internalization. GAT100 is applicable to the research of psychobehavioral and somatic diseases[1][2].

体外研究
(In Vitro)

GAT100 (Compound 20) (30 min preincubation, 90 min co-incubation with CP55,940) 可强效抑制 CHO-K1 hCB1R 细胞中 CP55,940 依赖的 β-抑制蛋白募集、cAMP 积累，EC50 分别为 2.09、174 nM[1]。
GAT100 (37 °C 下处理 60 分钟) 是[3H]CP55,940 结合 CHO hCB1R 膜的正变构调节剂，其 EC50 为 19.6 nM[1]。
GAT100 (500 nM; 0-120 min) 可以时间依赖的方式共价标记 HEK293 细胞膜中的 hCB1R，与 hCB1R 发生共价结合[1]。
GAT100 (30 min) 可强效抑制 HEK293A、Neuro2a 和 STHdhQ7/Q7 细胞中 CB1 介导的 β-arrestin1 募集、 PLCβ3 磷酸化、ERK1/2 磷酸化作用[2]。
GAT100 (1-10000 nM; 4 h) 可强效抑制 HEK-CRE 细胞中由 CB1 介导、福司柯林刺激的 cAMP 积累[2]。
GAT100 (1 μM; 0.5-20 h) 可快速逆转 CP55,940 诱导的 STHdhQ7/Q7 细胞中 CB1 内吞作用，其恢复质膜 CB1 水平的速度快于参照别构调节剂[2]。

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

GAT100 相关抗体:

Western Blot Analysis[2]

Cell Line: HEK293A cells transiently transfected with hCB1-GFP2, Neuro2a cells endogenously expressing CB1, STHdhQ7/Q7 cells endogenously expressing CB1
Concentration: 1-10000 nM; 500 nM (co-treated with 2-AG, AEA, or CP55,940)
Incubation Time: 10 min
Result: Inhibited PLCβ3 phosphorylation in HEK293A cells with IC50 values of 56.1 nM (44.0-62.6 nM, with 2-AG), 50.2 nM (23.9-65.3 nM, with AEA), 76.6 nM (60.8-103 nM, with CP55,940), and Eₘₐₓ values of 0.39, 0.36, 0.39, respectively.
Inhibited PLCβ3 phosphorylation in Neuro2a cells with IC50 values of 50.1 nM (33.4-79.2 nM, with 2-AG), 60.3 nM (28.1-131 nM, with AEA), 49.0 nM (25.2-93.4 nM, with CP55,940), and Eₘₐₓ values of 0.34, 0.37, 0.39, respectively.
Inhibited PLCβ3 phosphorylation in STHdhQ7/Q7 cells with IC50 values of 52.7 nM (39.8-63.1 nM, with 2-AG), 57.4 nM (35.9-66.1 nM, with AEA), 71.0 nM (67.2-79.7 nM, with CP55,940), and Eₘₐₓ values of 0.37, 0.37, 0.38, respectively.
Showed no effect on basal PLCβ3 phosphorylation when tested alone (1 nM to 10 μM) in any cell type.\nInhibited ERK1/2 phosphorylation in HEK293A cells with IC50 values of 69.4 nM (50.2-76.5 nM, with 2-AG), 56.6 nM (29.3-71.6 nM, with AEA), 84.1 nM (78.3-96.1 nM, with CP55,940), and Eₘₐₓ values of 0.33, 0.31, 0.29, respectively.
Inhibited ERK1/2 phosphorylation in Neuro2a cells with IC50 values of 57.5 nM (29.1-112 nM, with 2-AG), 57.5 nM (32.9-72.1 nM, with AEA), 47.9 nM (24.4-94.8 nM, with CP55,940), and Eₘₐₓ values of 0.31, 0.28, 0.33, respectively.
Inhibited ERK1/2 phosphorylation in STHdhQ7/Q7 cells with IC50 values of 57.9 nM (28.4-75.1 nM, with 2-AG), 51.3 nM (19.6-136 nM, with AEA), 52.3 nM (21.8-74.2 nM, with CP55,940), and Eₘₐₓ values of 0.37, 0.32, 0.34, respectively.
Showed no effect on basal ERK1/2 phosphorylation when tested alone (1 nM to 10 μM) in any cell type.

Western Blot Analysis[2]

Cell Line: STHdhQ7/Q7 cells endogenously expressing CB1
Concentration: 1 μM (co-treated with 500 nM CP55,940)
Incubation Time: 0.5 h, 1 h, 5 h, 10 h, 15 h, 20 h
Result: Reversed CP55,940-induced CB1 internalization, increasing the fraction of CB1 at the plasma membrane to ~0.6 by 0.5 h.
Exhibited a more rapid effect than Org27569 or PSNCBAM-1.
分子量

432.59

Formula

C25H28N4OS
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

GAT100 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

GAT1001663564-42-8GAT 100GAT-100Cannabinoid ReceptorPERKProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseCannabinoid 1 Receptor Negative Allosteric ModulatorCHO-K1 hCB1R cellsHEK293 cellsSTHdhQ7/Q7 cellsHEK-CRE cellspsychobehavioral and somatic diseases
Inhibitorinhibitorinhibit

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