Rolapitant NEW
| Price | $43 | $60 | $85 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-01 |
Product Details
| Product Name: Rolapitant | CAS No.: 552292-08-7 |
| Purity: 98.34% | Supply Ability: 10g |
| Release date: 2024/11/01 |
Product Introduction
Bioactivity
| 名稱 | Rolapitant |
| 描述 | Rolapitant (SCH619734) Hydrochloride is the hydrochloride salt form of rolapitant, an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of SP with the NK1-receptor plays a key role in the induction of nausea and vomiting caused by emetogenic cancer chemotherapy. Compared to other NK1-receptor antagonists, rolapitant has both a more rapid onset of action and a much longer half-life. |
| 激酶實驗 | Rolapitant is made at a stock concentration of 1 mM in 100% DMSO. For most receptor binding studies, the stock solution is diluted with the final concentrations ranged from 0.1 to 3 μM. Radioligand concentrations for competition binding studies ranged from 0.5 to 1 nM. For species comparison studies, 150 pM [125I]-BHSP is incubated with varying concentrations of protein (10-50 μg) prepared from gerbil, rabbit and monkey striata, and from cells expressing cloned rat, mouse and guinea pig NK receptors[1]. |
| 體外活性 | Rolapitant has a high affinity for the human NK1 receptor with a Ki of 0.66 nM and high selectivity over the human NK2 and NK3 subtypes of more than 1000-fold. Rolapitant has a preferential affinity for human, guinea pig, gerbil, and monkey NK1 receptors over rat, mouse, and rabbit[1]. |
| 體內(nèi)活性 | Rolapitant reverses NK1 agonist-induced foot tapping in gerbils following both intravenous and oral administration up to 24 hours at a minimal effective dose (MED) of 0.1 mg/kg. Rolapitant is active at 0.1 and 1 mg/kg in both acute and delayed emesis models in ferrets, respectively which is the same as clinical data for other NK1 antagonists. The clinical efficacy of anti-emetics is highly correlated with efficacy in the ferret emesis model, suggesting rolapitant is a viable clinical candidate for this indication[1]. |
| 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 : 55 mg/mL (109.89 mM), Sonication is recommended. |
| 關(guān)鍵字 | foot tapping | long-acting | emesis | retches | NK receptor | Neurokinin Receptor | SCH 619734 | vomits | SCH-619734 | Rolapitant | anti-emetic | Inhibitor | inhibit | orally active | Mongolian Gerbils | Tachykinin receptor | ferret |
| 相關(guān)產(chǎn)品 | Lanepitant 2HCl | Ezlopitant | (R)-CJ 11974 | N-Acetyl-L-tryptophan | Netupitant | Aprepitant | Befetupitant | Vofopitant | Fosaprepitant dimeglumine | Maropitant |
| 相關(guān)庫 | 高選擇性抑制劑庫 | 疼痛相關(guān)化合物庫 | 膜蛋白靶向化合物庫 | EMA 上市藥物庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | FDA 上市藥物庫 | 抗癌上市藥物庫 | 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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