化學信息:
化學名 | ethyl 4-[2-[1-(6-methylpyridazin-3-yl)piperidin-4-yl]ethoxy]benzoate | |
簡稱 | Pirodavir | |
別名 | R-77975, R77975, R 77975 | |
中文名 | 吡羅達韋 | |
化學式 | C21H27N3O3 | |
分子量 | 396.46 | |
CAS號 | 124436-59-5 | |
純度 | 98% | |
溶劑/溶解度 | Water<1mg/ml; DMSO67mg/ml; Ethanol7mg/ml | |
溶液配制 | 5mg加入1.26ml DMSO,或者每3.96mg加入1ml DMSO,配制成10mM溶液。SC3274-10mM用DMSO配制。 |
生物信息:
產品描述 | Pirodavir (R 77975) is the prototype of a novel class of broad-spectrum antipicornavirus compounds; potent human rhinovirus (HRV) capsid-binding inhibitor. | ||||
信號通路 | Anti-infection | ||||
靶點 | broad-spectrum antipicornavirus | capsid-binding | - | - | - |
IC50 | - | - | - | - | - |
體外研究 | R-77975's predecessor, R 61837, a substituted phenyl-pyridazinamine, was effective in inhibiting 80% of 100 serotypes tested (EC80) at concentrations above 32 micrograms/ml, pirodavir inhibits the same percentage of viruses at 0.064 micrograms/ml. Pirodavir is also effective in inhibiting 16 enteroviruses, with an EC80 of 1.3 micrograms/ml. Pirodavir acts at an early stage of the viral replication cycle (up to 40 min after infection) and reduces the yield of selected rhinoviruses 1,000- to 100,000-fold in a single round of replication. | ||||
體內研究 | Adults with symptoms of < or =2 days' duration were randomly assigned to intranasal sprays of pirodavir (2mg per treatment) or placebo six times daily for 5 days. In people with laboratory-documented rhinovirus colds (53 in the pirodavir group, 55 in the placebo group), no significant differences in the resolution of respiratory symptoms were apparent between the groups. The median duration of illness was 7 days in each group. Similarly, scores for individual symptoms found no differences in favor of pirodavir during or after treatment. | ||||
臨床實驗 | N/A | ||||
特征 | N/A |
相關實驗數據(此數據來自于公開文獻,并不保證其有效性):
酶活性檢測實驗 | |
方法 | N/A |
細胞實驗 | |
細胞系 | N/A |
濃度 | N/A |
處理時間 | N/A |
方法 | N/A |
動物實驗 | |
動物模型 | N/A |
配制 | N/A |
劑量 | N/A |
給藥方式 | N/A |
參考文獻:
1. Barnard DL, Hubbard VD, Smee DF. Antimicrob Agents Chemother. 2004 May, 48(5), 1766-72.2. Andries K, Dewindt B, Snoeks J. Antimicrob Agents Chemother. 1992 Jan, 36(1), 100-7.3. Hayden FG, Hipskind GJ, Woerner DH. Antimicrob Agents Chemother. 1995 Feb, 39(2), 290-4.包裝清單:
產品編號 | 產品名稱 | 包裝 |
SC3274-10mM | Pirodavir (HRV capsid-binding抑制劑) | 10mM×0.2ml |
SC3274-5mg | Pirodavir (HRV capsid-binding抑制劑) | 5mg |
SC3274-25mg | Pirodavir (HRV capsid-binding抑制劑) | 25mg |
— | 說明書 | 1份 |
保存條件:
-20℃保存,至少一年有效。5mg和25mg包裝也可室溫保存,至少6個月有效。如果溶于非DMSO溶劑,建議分裝后-80℃保存,預計6個月內有效。
注意事項:
本產品對人體有刺激性,操作時請小心,并注意適當防護以避免直接接觸人體或吸入體內。本產品僅限于專業人員的科學研究用,不得用于臨床診斷或治療,不得用于食品或藥品,不得存放于普通住宅內。為了您的安全和健康,請穿實驗服并戴一次性手套操作。
使用說明:
1.收到產品后請立即按照說明書推薦的條件保存。使用前可以在2,000-10,000g離心數秒,以使液體或粉末充分沉降至管底后再開蓋使用。
2.對于10mM溶液,可直接稀釋使用。對于固體,請根據本產品的溶解性及實驗目的選擇相應溶劑配制成高濃度的儲備液(母液)后使用。
3.具體的最佳工作濃度請參考本說明書中的體外、體內研究結果或其它相關文獻,或者根據實驗目的,以及所培養的特定細胞和組織,通過實驗進行摸索和優化。