L-Thymidine(Telbivudine)
2'-Deoxy-L-thymidine
CAS: 3424-98-4
Molecular Formula: C10H14N2O5
L-Thymidine(Telbivudine) - Names and Identifiers
| Name | 2'-Deoxy-L-thymidine |
| Synonyms | Epavudine Telbivudine L-Thymidine BETA-L-THYMIDINE 2'-Deoxy-L-thymidine 2'-DEOXY-L-THYMIDINE Β-L-2'-DEOXY-THYMIDINE L-Thymidine(Telbivudine) Telbivudine intermediates Telbivudine(Tyzeka, Sebivo) 2'-Deoxy-L-thyMidine(Telbivudine) 1-(2-deoxy--L-erythro-pentofuranosyl)thymine 1-(2-Deoxy-β-L-erythro-pentofuranosyl)-5-Methyl- 1-(2-Deoxy--L-erythro-pentofuranosyl)-5-methyl-2,4(1H,3H)-pyrimidinedione 1-(2-deoxy-beta-L-erythro-pentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione 1-[(2S,4R,5S)-4-Hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-methylpyrimidine-2,4-dione 1-[(2S,4R,5S)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-methyl-pyrimidine-2,4-dione |
| CAS | 3424-98-4 |
| EINECS | 608-961-3 |
| InChI | InChI=1/C10H14N2O5/c1-5-3-12(10(16)11-9(5)15)8-2-6(14)7(4-13)17-8/h3,6-8,13-14H,2,4H2,1H3,(H,11,15,16)/t6-,7+,8+/m1/s1 |
| InChIKey | IQFYYKKMVGJFEH-CSMHCCOUSA-N |
L-Thymidine(Telbivudine) - Physico-chemical Properties
| Molecular Formula | C10H14N2O5 |
| Molar Mass | 242.23 |
| Density | 1.452±0.06 g/cm3(Predicted) |
| Melting Point | 188-190°C |
| Specific Rotation(α) | D20 -20.3° (c = 0.192 in water) |
| Solubility | H2O: soluble10mg/mL (clear solution) |
| Appearance | powder |
| Color | white to beige |
| pKa | 9.55±0.10(Predicted) |
| Storage Condition | Sealed in dry,2-8°C |
| Refractive Index | 1.584 |
| In vitro study | Telbivudine exhibits potent, selective, and specific antiviral activity against HBV and other hepatitis DNA viruses. Telbivudine is phosphorylated by intracellular thymidine kinase to the active triphosphate form, which has an intracellular half-life of 14 hours. Telbivudine 5 ′-triphosphate inhibits HBV DNA polymerase (reverse transcriptase) by competing with the natural substrate dTTP. Telbivudine significantly increased the production of tumor necrosis factor alpha and interleukin-2 in MHV-3-induced macrophages. Telbivudine significantly increased serum levels of interferon gamma. Telbivudine treatment enhanced the ability of T cells to proliferate and secrete cellular molecules, but did not affect the cytotoxicity of infected hepatocytes. Telbivudine treatment inhibits programmed death ligand 1 expression in T cells. Telbivudine were 0.5 (N236T) and 1.0 (A181V and A194T) fold change, still have activity. Telbivudine had no activity against the lamivudine-resistant HBV strain mutant L180M/M204V/I, but it still had activity against the M204V single mutant in vitro, which may explain the difference in the resistance of the strains to telbivudine and lamivudine. |
L-Thymidine(Telbivudine) - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | 22 - Harmful if swallowed |
| Safety Description | 24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 3 |
| RTECS | UV9048500 |
| HS Code | 29349990 |
L-Thymidine(Telbivudine) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 4.128 ml | 20.642 ml | 41.283 ml |
| 5 mM | 0.826 ml | 4.128 ml | 8.257 ml |
| 10 mM | 0.413 ml | 2.064 ml | 4.128 ml |
| 5 mM | 0.083 ml | 0.413 ml | 0.826 ml |
Last Update：2024-01-02 23:10:35
L-Thymidine(Telbivudine) - Reference Information
| antiviral drugs for hepatitis B | telbivudine, lamivudine, adefovir dipivoxil and entecavir are several antiviral drugs for hepatitis B commonly used in clinical practice in China. this product is the natural L enantiomer of natural thymidine deoxynucleoside and is a synthetic thymidine deoxynucleoside anti-hepatitis B virus DNA polyenzyme drug. Under the action of cell kinase, it is phosphorylated to the active metabolite adenosine, which inhibits the activity of hepatitis B virus DNA polymerase by competing with the natural substrate thymine 5 '-adenosine in hepatitis B virus; Through integration into hepatitis B virus DNA, the hepatitis B virus DNA chain is prolonged and terminated. Simultaneously inhibit the synthesis of the first and second strands of hepatitis B virus DNA. It is suitable for the treatment of adult chronic hepatitis B patients with liver function compensation with evidence of hepatitis B virus activity and replication, accompanied by continuous elevation of transaminase or liver histologically active lesions. clinical research results show that among the newly treated patients receiving telbivudine 600 mg daily, the HBV DNA of 59% HBeAg positive patients and 89% HBeAg negative patients reached undetectable levels (<300 copies/ml) at week 52. viral mutations may occur during treatment, mainly rtM204I mutations. There are not enough controlled studies to observe the efficacy of telbivudine in the treatment of lamivudine-resistant hepatitis B virus infection. telbivudine is used in patients with chronic hepatitis B who have evidence of viral replication and evidence of persistent elevation of serum ALT or AST or active liver tissue. |
| dosage | patients must use this product under the guidance of a doctor with experience in the treatment of chronic hepatitis B. The recommended dose of this product for adults and adolescents (≥ 16 years old) is 600mg once a day, and it can be taken orally before or after meals. The optimal course of treatment has not been determined. Do not exceed the recommended dose. Patients with renal function injury and creatinine clearance ≥ 50mL/min can be taken according to the recommended dosage and usage. Patients with renal function injury and creatinine clearance <50mL/min include patients undergoing hemodialysis for end-stage renal disease (ESRD), and the dosage and usage should be adjusted under the guidance of doctors. Patients with end-stage renal disease (ESRD) should take this product after hemodialysis. Patients with liver function impairment do not need to change the recommended dose and usage. During the period of taking this product, the biochemical indicators, virological indicators and serum markers of hepatitis B should be monitored regularly, at least once every 6 months. |
| drug resistance | telbivudine resistance rate is lower than lamivudine. Both lamivudine and entecavir have a certain degree of cross-resistance, while lamivudine, telbivudine and entecavir are effective for adefovir-resistant HBV strains. In cytological tests, the sensitivity of telbivudine to lamivudine-resistant rtm204I mutations or rtLl80M/rtm204V double mutations was reduced by ≥ 1000 times; for rtm204V single mutations associated with lamivudine resistance, telbivudine retained activity similar to the phenotype of wild strains (reduced by 1.2 times). |
| adverse reactions | nucleoside drugs have been used alone or in combination with other antiretroviral drugs. There have been reports of lactic acidosis and severe fatty hepatomegaly, including death cases. In clinical studies, telbivudine was generally well tolerated, with most adverse events being mild or moderate. Frequent adverse events include upper respiratory tract infection, fatigue and discomfort, abdominal pain, nasopharyngitis, headache, creatine kinase (CK) elevation, cough, nausea and vomiting, influenza and flu-like symptoms, postoperative pain, diarrhea and loose stools, sore throat, fever, and arthralgia. There are reports of myalgia with or without complications (uncomplicated myagia) in patients treated with telbivudine, and CK elevation is more frequent. It is recommended that patients report unexplained muscle weakness, tenderness or pain in time. Renal function should be monitored in elderly patients and dose adjusted according to renal function. Studies of telbivudine in children under 16 years of age have not been conducted. |
| biological activity | Telbivudine is an HBV reverse transcriptase inhibitor used to treat hepatitis B infection. |
| Target | Value |
Last Update：2024-04-09 19:05:11
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CAS: 3424-98-4
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CAS: 3424-98-4
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: Telbivudine Visit Supplier Webpage Request for quotationCAS: 3424-98-4
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Email: 3008007409@qq.com
Mobile: 18021002903
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