2. Membrane Transporter/Ion Channel Neuronal Signaling MAPK/ERK Pathway Stem Cell/Wnt
  3. GABA Receptor ERK
  4. CLH304a

CLH304a  (Synonyms: (E)-GABAB receptor antagonist 1)

目录号: HY-129636
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CLH304a (compound 14) 是一种特异性、非竞争性的 GABAB 受体负变构调节剂 (NAM)。CLH304a 可降低 GABA 诱导的 IP3 生成，IC50 为 37.9 μM。CLH304a 对其他 GPCR C 类成员，如 mGluR1、mGluR2 和 mGluR5，没有影响。CLH304a 作用于 GB2 亚基的七螺旋结构域，具有反向激动剂特性。CLH304a 可抑制过表达 GABAB 受体的 HEK293 细胞中巴氯芬 (HY-B0007) 诱导的 ERK1/2 磷酸化。

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CLH304a

CLH304a Chemical Structure

CAS No. : 1611483-29-4

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规格 价格 是否有货
1 mg ￥2900
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Other Forms of CLH304a:

CLH304a 相关抗体

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ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

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生物活性

CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor[1][2].

体外研究
(In Vitro)

(E)-GABAB receptor antagonist 1 (compound 14) 可降低过度表达 GABAB 受体和 Gqi9 蛋白的 HEK293 细胞中激动剂 GABA 诱导的 IP3 产生的最大效应，而不改变 EC50[1]。

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

CLH304a 相关抗体:
分子量

304.38

Formula

C18H24O4
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献

CLH304a 相关分类

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Keywords:

CLH304a1611483-29-4(E)-GABAB receptor antagonist 1GABA ReceptorERKGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorExtracellular signal regulated kinasesGABABnegative allosteric modulatorNAMIP3mGluR1mGluR2mGluR5GB2ERK1/2Inhibitorinhibitorinhibit

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