MCE 的所有产品仅用作科学研究，我们不为任何个人用途提供产品和服务。

JNJ16259685

CAS No. : 409345-29-5

MCE 站：JNJ16259685

产品活性：JNJ16259685 是一种选择性的 mGlu1 receptor 拮抗剂，能够浓度依赖性地抑制 mGlu1 的突触的活化，IC₅₀ 值为 19 nM。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：mGluR

In Vitro: JNJ16259685 potently and completely inhibits the glutamate (30 μM)-induced increase in intracellular Ca²⁺?concentrations at the rat mGlu1a receptor with an IC₅₀?value of 3.24±1.00 nM. IC₅₀?values for CPCCOEt and BAY 36-7620 are 17.8±10.3 μM and 161±38 nM, respectively. The potency of JNJ16259685 in blocking glutamate (30 μM)-induced Ca²⁺ mobilization at the human mGlu1a receptor is 1.21±0.53 nM (IC₅₀?n=3). JNJ16259685 inhibits the glutamate (3 μM)-induced rise in intracellular Ca²⁺?concentrations at the rat mGlu5a receptor with an IC₅₀?value of 1.31±0.39 μM (n=4). JNJ16259685 blocks glutamate (3 μM)-induced Ca²⁺?mobilization at the human mGlu5 receptor with an IC₅₀?of 28.3±11.7 μM (n=4). JNJ16259685 does not exhibit agonist activity at any of the group I mGlu receptors.

In Vivo: JNJ16259685 (0.125, 0.25, 0.5, 1, 2, 4 and 8?mg/kg, i.p) significantly reduces the time spent in digging behaviours (0.25-8 mg/kg), threat (all doses) and attack, in comparison with vehicle group. JNJ16259685 (30 mg/kg) produces very minimal effects on locomotor activity. JNJ16259685 dramatically reduces rearing behavior, exploration of a novel environment and lever pressing for a food reward (rat: 0.3 mg/kg; mouse: 1 mg/kg). Subcutaneously administered JNJ16259685 (30 mg/kg) has no effect on reflexive startle responses to loud auditory stimuli or foot shock in mice. JNJ16259685 exhibits high potencies in occupying central mGlu1 receptors in the rat cerebellum and thalamus (ED₅₀=0.040 and 0.014 mg/kg, respectively).

相关产品：GPCR/G Protein Compound Library  |  Neuronal Signaling Compound Library  |  Neurotransmitter Receptor Compound Library  |  Bioactive Compound Library Plus  |  L-Glutamine  |  Eglumegad  |  LY341495  |  MPEP Hydrochloride  |  DHPG  |  trans-ACPD  |  (S)-MCPG  |  Lu AF21934  |  Xanthurenic acid  |  FITM  |  ADX88178  |  CTEP  |  Mavoglurant  |  Dipraglurant  |  VU0364770  |  Basimglurant  |  Foliglurax monohydrochloride  |  JNJ-40411813  |  JNJ-46778212  |  L-APB  |  MTEP hydrochloride  |  VU0650786  |  LY2794193  |  LY404039  |  O-Phospho-L-serine  |  CPPHA  |  E4CPG  |  JNJ-42153605  |  JNJ-46281222

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 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域；
•   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 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*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。