2. GPCR/G Protein Neuronal Signaling Cell Cycle/DNA Damage
  3. Dopamine Receptor PERK
  4. MLS6357

MLS6357 是一种 D3 多巴胺受体 (D3R) 选择性正变构调节剂-拮抗剂 (PAM-antagonist)。MLS6357 在 D3R 介导和基于 BRET 的 β-Arrestin 募集试验中表现出拮抗活性，IC50 值分别为 13 和 14 μM，对其他 DAR亚型 (D1R、D2R、D4R 和 D5R) 几乎无活性 (IC50 > 100 μM)。MLS6357 在 D3R 介导的 Go-BRET 试验中也表现出拮抗活性，IC50 为 17 μM。MLS6357 可用于研究包括物质使用障碍在内的神经精神疾病。

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MLS6357

MLS6357 Chemical Structure

CAS No. : 932544-59-7

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MLS6357 相关抗体

Top Publications Citing Use of Products

查看 Dopamine Receptor 亚型特异性产品:

查看所有亚型
Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MLS6357 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist. MLS6357 exhibits antagonist activity in the D3R-mediated and the BRET-based β-arrestin recruitment assay with IC50s of 13 and 14 μM, and no activity for other DAR subtypes (D1R/D2R/D4R/D5R) (IC50 > 100 μM). MLS6357 is also an antagonist in the D3R-mediated Go-BRET assay with an IC50 of 17 μM. MLS6357 can be used for the study of neuropsychiatric disorders, including substance use disorder[1].

IC50 & Target[1]

Dopamine D3 receptor

13 μM (IC50)

Dopamine D1 receptor

 

Dopamine D2 receptor

 

Dopamine D4 receptor

 

Dopamine D5 receptor

 

体外研究
(In Vitro)

MLS6357 在HEK293 细胞中可完全拮抗 EC80 浓度的 Dopamine (HY-B0451) 诱导的 cAMP 蓄积衰减 (IC50 为 4.5 μM) 以及 D3R 刺激的 ERK1/2 磷酸化 (pERK) 衰减 (IC50 为 5.6 μM)[1]。 MLS6357 在人肝微粒体中表现出较好的微粒体稳定性 (CLint = 51 μL/min/mg；t1/2 = 13.6 min)[1]。

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

MLS6357 相关抗体:
分子量

395.90

Formula

C18H22ClN3O3S
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

MLS6357 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)

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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:

MLS6357932544-59-7MLS 6357MLS-6357Dopamine ReceptorPERKProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinasePositive Allosteric Modulator-Antagonistβ-Arrestin RecruitmentPharmacokineticStructure-Activity RelationshipInhibitorinhibitorinhibit

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产品名称：
MLS6357
目录号：
HY-175504
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