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。

FITM

CAS No. : 932737-65-0

MCE 国际站：FITM

产品活性：FITM是mGlu1受体的负变构调节剂，K_i值为2.5 nM。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：mGluR

In Vitro: FITM fits tightly into the long and narrow pocket. Most of the ligand-receptor interactions are hydrophobic with the exception of the contacts of the pyrimidine-amine group with the T815 ^7.38 side chain. The mGlu1 binding pocket for FITM largely corresponds to mutagenic data for the common allosteric site in mGlus and likely extends to other class C GPCRs. FITM which shows high affinity and selectivity for mGlu1 over mGlu5. FITM has the high hydrogen bonds occupancy with Thr815 and Tyr805 in dimer A and B of mGlu1 during molecular dynamics simulations. The nitrogen and hydrogen atoms of FITM form the dynamical hydrogen bonds with the hydrogen atom of Tyr805 and oxygen atom of Thr815, respectively. It indicates that there is a strong attraction interaction between FITM and allosteric sites.

In Vivo: The pretreatment of rats with unlabeled FITM (1 mg/kg) occupies an mGluR1 binding site of 18F-FITM by more than 99% and does not affect the input function. The K_d (nM) and B_max (pmol/mL) obtained by the Scatchard analyses with the multidose ligand assays are 2.1 and 36.3, respectively, for the thalamus; 2.1 and 27.5, respectively, for the hippocampus; 1.5 and 22.2, respectively, for the striatum; and 1.5 and 20.5, respectively, for the cingulate cortex with a high confidence. ¹⁸F-FITM shows excellent pharmacokinetics, namely the dense and specific accumulation in mGlu1-positive melanomas versus mGlu1-negative hepatoma and normal tissues. Furthermore, the accumulation levels of radioactivity corresponded to the extent of tumor and to levels of mGlu1 protein expression in melanomas and melanoma metastasis.

相关产品：Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Neuronal Signaling Compound Library  |  Anti-Cancer Compound Library  |  Neurotransmitter Receptor Compound Library  |  Neuroprotective Compound Library  |  Anti-Parkinson's Disease Compound Library  |  Neurodegenerative Disease-related Compound Library  |  Targeted Diversity Library  |  Antidepressant Compound Library  |  Heterocyclic Compound Library  |  Membrane Protein-targeted Compound Library  |  Membrane Receptor-targeted Compound Library  |  Highly Selective Inhibitors Library  |  Decoglurant  |  VU6010572  |  FPTQ  |  (S)-MCPG  |  L-Glutamine-d₅  |  Mavoglurant racemate  |  L-Glutamine-¹³C₅,¹⁵N₂  |  DFMTI  |  VU0360172  |  JNJ16259685  |  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。