Product Details
Product Name:
AMG-0347 |
CAS No.:
946615-43-6 |
Purity:
99.7% |
Supply Ability:
10g |
Release date:
2024/11/16 |
Product Introduction
Bioactivity
名稱 | AMG-0347 |
描述 | AMG-0347 (UNII-CD7L9290QR) is a small molecule inhibitor targeting TRPA1(transient receptor potential ankyrin 1) ion channels, a receptor found in sensory neurons and involved in the detection of pain and environmental stimuli. AMG-0347 acts by blocking the function of TRPA1 and has analgesic effects. |
體外活性 | The inhibitory effects of AMG-0347 on the activation of TRPV1 channels by heat (45°C), protons (pH5), or capsaicin (500 nM) were evaluated using the 45 Ca2+ uptake assay in Chinese hamster ovary cells stably expressing rat or human TRPV1 channels.[1]
AMG-0347 demonstrated potent and selective antagonism against TRPV1 in vitro. Concentration-dependent inhibition was observed with IC50 values of 0.2 nM for heat-induced activation, 0.8 nM for proton-induced activation, and 0.7 nM for capsaicin-induced activation of rat TRPV1 channels. AMG-0347 did not exhibit blocking activity against other TRP channels, including TRPV2, TRPV3, TRPV4, TRP ankyrin-1, and TRP melastatin-8, with IC50 values of 10 μM.[1] |
體內(nèi)活性 | AMG0347 did not change the withdrawal threshold to mechanical stimulation or the guarding pain score. The withdrawal latency to heat increased from 3 h through 1 day after AMG0347 administration. AMG0347 prevented the decreases in heat withdrawal latency and mechanical withdrawal threshold caused by capsaicin infiltration and prevented the increase in activity caused by intrathecal capsaicin injection.[2] |
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 : 27.5 mg/mL (61.73 mM)
|
關(guān)鍵字 | AMG 0347 | AMG-0347 | AMG0347 |
相關(guān)產(chǎn)品 | (+)-Camphor | AP 18 | Methyl syringate | Caffeic Acid | Oleoyl Serotonin | (-)-Menthol | Camphor | Pregnenolone | Probenecid | 1,4-Cineole | Methyl salicylate | SKF-96365 hydrochloride |
相關(guān)庫 | 疼痛相關(guān)化合物庫 | 經(jīng)典已知活性庫 | 神經(jīng)信號分子庫 | 膜蛋白靶向化合物庫 | 抑制劑庫 | 已知活性化合物庫 | 離子通道庫 |
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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Recommended supplier
Product name |
Price |
|
Suppliers |
Update time |
|
$380.00/1mg |
VIP3Y
|
TargetMol Chemicals Inc.
|
2024-11-16 |
|
$0.00/1KG |
VIP2Y
|
Wuhan Haorong Biotechnology Co.,Ltd
|
2023-08-07 |