DREADD agonist 21 NEW
| Price | $53 | $77 | $143 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-04 |
Product Details
| Product Name: DREADD agonist 21 | CAS No.: 56296-18-5 |
| Purity: 99.88% | Supply Ability: 10g |
| Release date: 2024/11/04 |
Product Introduction
Bioactivity
| 名稱 | DREADD agonist 21 |
| 描述 | DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (EC50=1.7 nM). |
| 體外活性 | DREADD agonist 21 is a highly selective and potent agonist for muscarinic DREADDs (pEC50 for hM1Dq=6.54 and that for hM4Di=7.77 in pERK assays)[2]. DREADD agonist 21 potently activates hM3Dq in Chinese hamster ovary (CHO) cells transfected cells in vitro (pEC50: 8.48±0.05) and it also potently activates hM1Dq, hM3Dq, and hM4Di. DREADD agonist 21 does not activate human M3 receptor (hM3). DREADD agonist 21 displays high binding affinities to 5HT2A and 5HT2C serotonin receptor, α1A adrenergic receptor, and H1 histamine receptor with Ki values of 66, 170, 280, and 6 nM, respectively[1]. In addition to being inactive at hM3, DREADD agonist 21, a potent full agonist of hM3Dq (EC50=1.7 nM), is only 3.5-fold selective for hM3Dq over H1, 40-fold selective over 5HT2A, 100-fold selective over 5HT2C, and 165-fold selective over α1A. DREADD agonist 21 binds to hM1, hM4, hM1Dq and hM4Di receptors (pKis of 5.97, 5.44, 7.20, and 6.75, respectively). |
| 體內(nèi)活性 | DREADD agonist 21 has excellent pharmacokinetic properties, bioavailability and brain penetrability. DREADD agonist 21 (0.3, 1.0, and 3.0 mg/kg; i.p.) activates neuronal hM3Dq in mice. DREADD agonist 21 (0.1, 1, and 10 mg/kg; i.p.) shows 95.1% plasma protein binding and 95% brain protein bounding in mice[2]. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 75 mg/mL (269.44 mM) |
| 關(guān)鍵字 | Muscarinic acetylcholine receptor | schizophrenia | mAChR | DREADD agonist 21 | Inhibitor | muscarinic | disease | inhibit | DREADD agonist21 | neurodegenerative | acetylcholine | DREADD | neuronal | hM3Dq | DREADD agonist-21 | activation | receptors |
| 相關(guān)產(chǎn)品 | Adiphenine hydrochloride | Alverine citrate | Dapoxetine hydrochloride | Meclizine dihydrochloride | Ribavirin | Lidocaine | Famotidine | Octopamine hydrochloride | Sodium butanoate | Choline chloride | Propoxur | Alginic acid |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 神經(jīng)退行性疾病化合物庫(kù) | 疼痛相關(guān)化合物庫(kù) | 膜蛋白靶向化合物庫(kù) | 抗帕金森病化合物庫(kù) | 神經(jīng)遞質(zhì)受體化合物庫(kù) | 已知活性化合物庫(kù) | GPCR靶點(diǎn)分子庫(kù) | 抗癌化合物庫(kù) | 5-羥色胺分子庫(kù) |
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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