Ledipasvir D-tartrate
(Synonyms: 雷迪帕韦 D-酒石酸; GS-5885 D-tartrate) 目录号 : GC36437
An HCV NS5A inhibitor
Cas No.:1502654-87-6
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Ledipasvir is an inhibitor of hepatitis C virus (HCV) non-structural protein 5A (NS5A).1,2 It inhibits viral replication in genotype 1a and 1b HCV replicon cells (EC50s = 0.031 and 0.004 nM, respectively). It also inhibits viral replication in genotype 2a, 2b, 3a, 4a, 4d, 5a, 6a, and 6e HCV replicon cells (EC50s = 0.11-530 nM).2 Lepidasvir acts synergistically with IFN-α, ribavirin , or GS-9669 and additively with GS-9451, simeprevir , daclatasvir , or sofosbuvir to inhibit viral replication in genotype 1a HCV replicon cells. Formulations containing ledipasvir have been used in combination therapy for the treatment of chronic HCV infection.
1.Link, J.O., Taylor, J.G., Xu, L., et al.Discovery of ledipasvir (GS-5885): A potent, once-daily oral NS5A inhibitor for the treatment of hepatitis C virus infectionJ. Med. Chem.57(5)2033-2046(2014) 2.Cheng, G., Tian, Y., Doehle, B., et al.In vitro antiviral activity and resistance profile characterization of the hepatitis C virus NS5A inhibitor ledipasvirAntimicrob. Agents Chemother.60(3)1847-1853(2016)
Animal experiment: | Rats, Dogs and Monkeys[1]Pharmacokinetic studies are performed in male naı̈ve Sprague-Dawley(SD) rats, non-naı̈ve beagle dogs, and cynomolgus monkeys (three animals per dosing route). Intravenous (IV) administration is dosed via infusion over 30 min in a vehicle containing 5% ethanol, 20% PEG400, and 75% water (pH adjusted to 3.0 with HCl). Oral dosing is administered by gavage in a vehicle containing 5% ethanol, 45% PEG 400, and 50% of 50 mM citrate buffer, pH 3. Blood samples are collected over a 24 h period postdose into Vacutainer tubes containing EDTA-K2. Plasma was isolated, and the concentration of the test compound in plasma was determined with LC/MS/MS after protein precipitation with acetonitrile. |
References: [1]. Link JO, et al. Discovery of ledipasvir (GS-5885): a potent, once-daily oral NS5A inhibitor for the treatment of hepatitis C virus infection. J Med Chem. 2014 Mar 13;57(5):2033-46 | |
| Cas No. | 1502654-87-6 | SDF | |
| 别名 | 雷迪帕韦 D-酒石酸; GS-5885 D-tartrate | ||
| Canonical SMILES | O=C(OC)N[C@H](C(N([C@H](C1=NC=C(C2=CC(C(F)(F)C3=C4C=CC(C5=CC=C6N=C([C@H]7N(C([C@@H](NC(OC)=O)C(C)C)=O)[C@]8([H])CC[C@@]7([H])C8)NC6=C5)=C3)=C4C=C2)N1)C9)CC%109CC%10)=O)C(C)C.O[C@@H]([C@@H](C(O)=O)O)C(O)=O | ||
| 分子式 | C53H60F2N8O12 | 分子量 | 1039.09 |
| 溶解度 | DMSO: ≥ 28 mg/mL (26.95 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 0.9624 mL | 4.8119 mL | 9.6238 mL |
| 5 mM | 0.1925 mL | 0.9624 mL | 1.9248 mL |
| 10 mM | 0.0962 mL | 0.4812 mL | 0.9624 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet