S1RA hydrochloride NEW
| Price | $32 | $73 | $113 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-17 |
Product Details
| Product Name: S1RA hydrochloride | CAS No.: 1265917-14-3 |
| Purity: 99.78% | Supply Ability: 10g |
| Release date: 2024/11/17 |
Product Introduction
Bioactivity
| 名稱 | S1RA hydrochloride |
| 描述 | S1RA hydrochloride (E-52862 hydrochloride) is an effective and specific sigma-1 receptor(σ1R, Ki: 17 nM) antagonist, and has good selectivity against σ2R (Ki > 1000 nM). |
| 體外活性 | S1RA showed high affinity for the guinea pig (Ki: 23.5 nM) and human (Ki: 17 nM) σ1 receptors but no marked affinity for the σ2 receptors (Ki > 1000 nM for guinea pig and rat σ2 receptors). Moderate affinity (Ki: 328 nM) and antagonistic activity with very low potency (IC50: 4700 nM) were found at the human 5-HT2B receptor. S1RA showed a low affinity (Ki > 1 μM, IC50>1 μM) for other additional 170 targets (transporters, receptors, ion channels and enzymes). |
| 體內(nèi)活性 | Control (non-operated) and nerve-injured mice received a single or repeated (b.i.d, for 12 days) S1RA (25 mg/kg, i.p.), the same dose used for the assessment of behavioral hypersensitivity in the chronic treatment study. In the behavioral studies, acute treatment was given on day 12 post-surgery and repeated treatment with S1RA started the day of surgery. Intrathecal pre-treatment with idazoxan prevented the systemic S1RA antinociceptive effect, suggesting that the S1RA antinociception depends on the activation of spinal α2 -adrenoceptors which, in turn, could induce an inhibition of formalin-evoked glutamate release. When administered locally, intrathecal S1RA inhibited only the flinching behavior, whereas intracerebroventricularly or intraplantarly injected also attenuated the lifting/licking behavior. |
| 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 : 50 mg/mL (133.74 mM) |
| 關(guān)鍵字 | Inhibitor | E 52862 | S1RA hydrochloride | E 52862 Hydrochloride | E52862 | S1RA | E-52862 | E-52862 Hydrochloride | inhibit | S1RA Hydrochloride | S-1RA hydrochloride | Sigma Receptor | E52862 Hydrochloride |
| 相關(guān)產(chǎn)品 | KB-5492 free base | Cutamesine dihydrochloride | Blarcamesine hydrochloride | Sigma-1 receptor antagonist 2 | Amitriptyline hydrochloride | S1R agonist 2 | Ditolylguanidine | 4-PPBP maleate | Sigma-1 receptor antagonist 1 | Glycerol phenylbutyrate | KSK67 | AB21 HCl |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 疼痛相關(guān)化合物庫 | 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 | NO PAINS 化合物庫 | 已知活性化合物庫 | GPCR靶點(diǎn)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
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