Rolapitant hydrochloride NEW
| Price | $155 | $385 | $548 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-17 |
Product Details
| Product Name: Rolapitant hydrochloride | CAS No.: 858102-79-1 |
| Purity: 99.79% | Supply Ability: 10g |
| Release date: 2024/11/17 |
Product Introduction
Bioactivity
| 名稱 | Rolapitant hydrochloride |
| 描述 | Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting, and orally active neurokinin 1 (NK1) receptor antagonist with a K_i of 0.66 nM, which does not interact with CYP3A4 and demonstrates potent centrally-mediated anti-emetic activity in both acute and delayed ferret emesis models [1] [2]. |
| 體外活性 | In vitro studies indicate that rolapitant has a high affinity for the human NK1 receptor of 0.66 nM and high selectivity over the human NK2 and NK3 subtypes of >1000-fold, as well as preferential affinity for human, guinea pig, gerbil and monkey NK1 receptors over rat, mouse and rabbit [1]. Rolapitant (1-1000 nM) inhibits the GR-73632 (an NK1 receptor agonist)-induced calcium efflux with a concentration-dependent and competitive manner in CHO cells expressing the human NK1 receptor [1]. |
| 體內(nèi)活性 | Rolapitant, administered orally (0.03-1 mg/kg) or intravenously (0.3-1 mg/kg) as a single dose, effectively mitigates the GR-73632-induced foot-tapping in Mongolian Gerbils and prevents acute emesis triggered by apomorphine and cisplatin in ferrets, with observations lasting up to 72 hours. In the Mongolian Gerbil model, the compound, when given orally, significantly reduces the foot-tapping response, achieving an ID90 at 0.3 mg/kg and maintaining inhibition for over 24 hours. Intravenous administration resulted in a complete cessation of foot-tapping at a dose of 1 mg/kg. In ferrets, rolapitant dose-dependently inhibits vomiting and retching induced by both emetic agents over a 72-hour period, illustrating its potential as an effective clinical antiemetic. This aligns with the ferret emesis model's predictive value for clinical antiemetic efficacy, endorsing rolapitant as a promising candidate for this purpose. |
| 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 (93.12 mM) |
| 關(guān)鍵字 | Rolapitant hydrochloride | Rolapitant Hydrochloride |
| 相關(guān)產(chǎn)品 | Rolapitant | Ezlopitant | (R)-CJ 11974 | N-Acetyl-L-tryptophan | Netupitant | Aprepitant | Befetupitant | Vofopitant | Fosaprepitant dimeglumine | Maropitant |
| 相關(guān)庫 | 疼痛相關(guān)化合物庫 | 經(jīng)典已知活性庫 | 膜蛋白靶向化合物庫 | EMA 上市藥物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | 抗癌上市藥物庫 | 已知活性化合物庫 | GPCR靶點分子庫 | 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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