JNJ-18038683 NEW
| Price | $46 | $83 | $173 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-08 |
Product Details
| Product Name: JNJ-18038683 | CAS No.: 851376-05-1 |
| Purity: 98.31% | Supply Ability: 10g |
| Release date: 2024/11/08 |
Product Introduction
Bioactivity
| 名稱 | JNJ-18038683 |
| 描述 | JNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT7) receptor antagonist with pKis of 8.19 and 8.20 for rat and human 5-HT7 in HEK293 cells, respectively. |
| 體外活性 | JNJ-18038683 produces a concentration-dependent decrease of 5-HT (100 nM)-stimulated adenylyl cyclase. The pKB values determined for JNJ-18038683 are in good agreement with the corresponding Ki values determined from [3H]5-CT binding studies.JNJ-18038683 displaced, with high affinity, specific [3H]5-CT binding sites from rat and human 5-HT7 receptor express in HEK293 cells (pKi=8.19±0.02 and 8.20±0.01, respectively). Similar values are obtained on the native 5-HT7 in membranes from rat thalamus (pKi=8.50±0.20). Hill slope values are close to unity, suggesting one-site competitive binding. Antagonist potency of JNJ-18038683 is determined by the measurement of adenylate cyclase activity in HEK293 cells expressing the human or rat 5-HT7 receptor. 5-HT stimulates adenylyl cyclase activity in rat and human 5-HT7/HEK293 cells with a pEC50 of 8.09 and 8.12, respectively. |
| 體內(nèi)活性 | JNJ-18038683 dose-dependently reduces REM sleep, particularly within the first 4 hours post-administration, with a significant decrease observed from a dosage of 1 mg/kg (P<0.05). Furthermore, it extends REM sleep latency, showing a significant prolongation at the highest dose tested (10 mg/kg; P<0.05), indicating that these effects are specific to the REM sleep state. An additional study evaluated the impact of administering JNJ-18038683 daily for 7 days (1 mg/kg s.c. per day) on EEG sleep patterns in rats, focusing on REM sleep both during treatment and after its cessation. Initial treatment significantly reduced REM sleep duration in the first 8 hours and increased REM latency, which remained elevated throughout the 7-day treatment but returned to normal after treatment stopped. While the reduction in REM sleep persisted during the treatment period, a rebound increase in REM sleep occurred upon treatment discontinuation. Neither the latency nor the total time of NREM sleep was impacted over the treatment course. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 200 mg/mL (358.51 mM), Sonication is recommended. |
| 關(guān)鍵字 | Inhibitor | 5-hydroxytryptamine Receptor | JNJ-18038683 | inhibit | Serotonin Receptor | 5-HT Receptor | JNJ18038683 | JNJ 18038683 |
| 相關(guān)產(chǎn)品 | Serotonin hydrochloride | Alverine citrate | Olanzapine | Dapoxetine hydrochloride | CLOZAPINE N-OXIDE | Mirtazapine | Amitriptyline hydrochloride | Cloperastine hydrochloride | Trazodone hydrochloride | Mianserin hydrochloride | Fluoxetine hydrochloride | Cinchonidine |
| 相關(guān)庫 | 疼痛相關(guān)化合物庫 | 神經(jīng)退行性疾病化合物庫 | 經(jīng)典已知活性庫 | 膜蛋白靶向化合物庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | 已知活性化合物庫 | GPCR靶點分子庫 | 抗癌藥物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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