Product Details
| Product Name:
EMPA |
CAS No.:
680590-49-2 |
| Purity:
99.91% |
Supply Ability:
10g |
| Release date:
2024/11/17 |
Product Introduction
Bioactivity
| 名稱 | EMPA |
| 描述 | EMPA is a selective, high-affinity and reversible antagonist of orexin OX2 receptor(human and rat OX2-HEK293 membranes with KD values of 1.1 and 1.4 nM respectively) |
| 體外活性 | EMPA displaces the EMPA binding from cell membranes containing human and rat OX2 receptors, with Ki values of 1.10±0.24 nM and 1.45±0.13 nM, respectively. EMPA shows an IC50=5.75 μM, Ki=2.63 μM, and IC50=12.8 μM, Ki=5.8 μM in the binding assay at human and mouse V1a receptors, respectively. In CHO(dHFr-) cells stably expressing hOX2 receptors, EMPA inhibits orexin-A-or orexin-B-evoked [Ca2+]i response with IC50s of 8.8±1.7 nM and 7.9±1.7 nM, respectively.EMPA competitively antagonizes orexin-A-and orexin-B-evoked accumulation of inositol phosphates (IP) at hOX2 receptors with pA2 values of 8.6 and 8.8 respectively. |
| 體內(nèi)活性 | EMPA (3-30 mg/kg;i.p.) induces a significant and dose-dependent reduction in the baseline LMA in france and male Wistar rats.EMPA (3-30 mg/kg;i.p.) demonstrates a clear dose-dependent inhibition of spontaneous activity as compared with vehicle-treated animals.EMPA (1-300 mg/kg; i.p.) dose-dependently reverses this [Ala11,D-Leu15]orexin-B-induced hyperlocomotion without itself significantly affecting locomotor activity (LMA) in male NMRI mice. |
| 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 : 230 mg/mL (506 mM), Sonication is recommended.
|
| 關(guān)鍵字 | Hypocretin Receptor | Orexin Receptor (OX Receptor) | HCRT Receptor | EMPA | inhibit | Inhibitor |
| 相關(guān)產(chǎn)品 | L-368,899 hydrochloride | YNT-185 | IPSU | MK-3697 | Filorexant | DORA-22 | Orexin B, rat, mouse Acetate | OXA (17-33) acetate | PF3274167 | ACT-462206 | Seltorexant | TCS 1102 |
| 相關(guān)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 | NO PAINS 化合物庫 | 已知活性化合物庫 | GPCR靶點分子庫 |
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 |
|
|
$47.00/1mg |
VIP3Y
|
TargetMol Chemicals Inc.
|
2024-11-17 |
United States