MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

VU0364770

CAS No. : 61350-00-3

MCE 国际站：VU0364770

产品活性：VU0364770 是一种有效的选择性 mGlu4 正变构调节剂 (PAM)。VU0346770 对大鼠 mGlu4 和人 mGlu4 受体的 EC₅₀ 分别为 290 nM 和 1.1 μM。VU0364770 对 mGlu5 具有拮抗活性，EC₅₀ 为 17.9 μM，VU0364770 对 mGlu6 具有正变构调节活性，EC₅₀ 为 6.8 μM。VU0364770 还对 MAO 具有活性，作用于人 MAO-A 和 MAO-B 的 K_i 值分别为8.5 和 0.72 μM。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：mGluR

In Vitro: VU0364770 is a selective positive allosteric modulator of mGlu₄ in recombinant systems. VU0364770 is a potent PAM of multiple signaling pathways that enhances the response of the rat and human mGlu₄ receptors to the endogenous agonist glutamate. VU0364770 produces a concentration-dependent potentiation of the response to an EC₂₀ concentration of glutamate with EC₅₀ of 1.1±0.2 μM and increases the maximal response to glutamate from 100 to 227±17%. Because of concerns that this chemical scaffold might possess activity at MAO, full IC₅₀ determinations is performed for VU0364770 at the MAO-A and MAO-B isoforms; these studies result in K_is of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively. When tested at a 10 μM concentration at each mGlu receptor, VU0364770 exhibits weak PAM activity (4.3-fold left shift of the glutamate CRC) at mGlu6 and antagonist activity (3.3-fold right shift of the glutamate CRC) at mGlu5 (compare to the 16.5-fold left shift of the glutamate concentration-response for mGlu₄ at 10 μM). When further evaluated in a full concentration-response curve format, VU0364770 exhibits antagonist activity at mGlu₅ with a potency of 17.9±5.5 μM and PAM activity at mGlu₆ with a potency of 6.8±1.7 μM (compare with the potency of VU0364770 on the rat mGlu₄ receptor of 290±80 nM).

In Vivo: VU0364770 exhibits suitable pharmacokinetic properties for systemic dosing in animal models. After intravenous administration, VU0364770 is rapidly clears from the systemic circulation (165 ml/min/kg) and exhibits a volume of distribution of 2.92 L/kg. VU0364770 is a highly protein-bound ligand displaying free fractions of 2.7 and 1.8% in human and rat plasma, respectively. VU0364770 also shows an improved pharmacokinetic profile relative to previously reported mGlu₄ PAMs with enhanced central penetration and a total brain-to-plasma ratio of more than 1 after systemic administration of a 10 mg/kg dose. VU0364770 produces a dose-dependent reversal of haloperidol-induced catalepsy. VU0364770 dose-dependently reverses haloperidol (0.75 mg/kg)-induced catalepsy in rats, significant at doses of 10 to 56.6 mg/kg, after subcutaneous dosing (F_6,69=8.04; p<0.001).

相关产品：Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Neuronal Signaling Compound Library  |  Neurotransmitter Receptor Compound Library  |  Heterocyclic Compound Library  |  Membrane Protein-targeted Compound Library  |  Membrane Receptor-targeted Compound Library  |  Highly Selective Activators Library  |  Decoglurant  |  VU6010572  |  FPTQ  |  (S)-MCPG  |  L-Glutamine-d₅  |  Mavoglurant racemate  |  L-Glutamine-¹³C₅,¹⁵N₂  |  DFMTI  |  VU0360172  |  JNJ16259685  |  FITM  |  VU0483605  |  LSN2463359  |  mGlu4 receptor agonist 1  |  LSP4-2022  |  AMN082  |  JF-NP-26  |  Xanthurenic acid-d₄  |  Talaglumetad hydrochloride  |  ABP688  |  Fasoracetam  |  Kainic acid hydrate  |  VU 0364439  |  mGluR2 antagonist 1  |  3,3'-Difluorobenzaldazine  |  trans-ACPD  |  VU 0357121  |  PHCCC  |  DCG-IV  |  TCN238

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物  |  寡核苷酸  |  抗体  |  点击化学

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种全球独家化合物库，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；
•   50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
•   专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。