TelbivudineCAS# 3424-98-4 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 3424-98-4 | SDF | Download SDF |
| PubChem ID | 159269 | Appearance | Powder |
| Formula | C10H14N2O5 | M.Wt | 242.23 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Epavudine; L-Thymidine; NV 02B | ||
| Solubility | DMSO : 50 mg/mL (206.42 mM; Need ultrasonic) H2O : 33.33 mg/mL (137.60 mM; Need ultrasonic) | ||
| Chemical Name | 1-[(2S,4R,5S)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-methylpyrimidine-2,4-dione | ||
| SMILES | CC1=CN(C(=O)NC1=O)C2CC(C(O2)CO)O | ||
| Standard InChIKey | IQFYYKKMVGJFEH-CSMHCCOUSA-N | ||
| Standard InChI | InChI=1S/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 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Telbivudine, a specific inhibitor of hepatitis B virus (HBV) replication, is an antiviral drug used in the treatment of hepatitis B infection.
Target: HBV
Telbivudine is an antiviral drug used in the treatment of hepatitis B infection. It is marketed by Swiss pharmaceutical company Novartis under the trade names Sebivo (Europe) and Tyzeka (United States). Clinical trials have shown it to be significantly more effective than lamivudine or adefovir, and less likely to cause resistance. Telbivudine is a synthetic thymidine nucleoside analogue, it is the L-isomer of thymidine. It is taken once daily.
Telbivudine is a potent antiviral that provides effective and sustained viral suppression in patients with compensated CHB. In clinical trials, treatment outcomes were improved significantly more with telbivudine 600 mg once daily than with lamivudine 100 mg or adefovir 10 mg once daily, and telbivudine-treated patients had significantly less viral resistance than lamivudine-treated patients. Telbivudine is associated with a medium genetic barrier to resistance and, as patients with undetectable HBV DNA levels have significantly improved outcomes, it is recommended that HBV DNA levels are monitored at week 24 (and 6 monthly thereafter), with the addition of a nucleoside/nucleotide analogue without cross resistance (such as adefovir dipivoxil) if viraemia is present to reduce the risk of resistance (Roadmap concept). Telbivudine was generally well tolerated in clinical trials for periods of up to 4 years, and has a similar tolerability profile to that of lamivudine. References: | |||||
Telbivudine Dilution Calculator
Telbivudine Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 4.1283 mL | 20.6415 mL | 41.2831 mL | 82.5662 mL | 103.2077 mL |
| 5 mM | 0.8257 mL | 4.1283 mL | 8.2566 mL | 16.5132 mL | 20.6415 mL |
| 10 mM | 0.4128 mL | 2.0642 mL | 4.1283 mL | 8.2566 mL | 10.3208 mL |
| 50 mM | 0.0826 mL | 0.4128 mL | 0.8257 mL | 1.6513 mL | 2.0642 mL |
| 100 mM | 0.0413 mL | 0.2064 mL | 0.4128 mL | 0.8257 mL | 1.0321 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Nucleoside analog. A specific inhibitor of hepatitis B virus (HBV) replication. Antiviral.
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[Effect of telbivudine on infants born to HBsAg-positive mothers with non-/hypo-response to hepatitis B vaccine during their second and third trimesters of pregnancy].[Pubmed:28231660]
Zhonghua Liu Xing Bing Xue Za Zhi. 2017 Feb 10;38(2):168-172.
Objective: To explore the effect of Telbivudine treatment in a prevention program on infants born to HBsAg-positive mothers with non-/hypo-responsiveness to hepatitis B vaccine. Methods: A retrospective cohort study with a total of 321 HBsAg-positive pregnant women and their infants enrolled, was conducted. The mothers were recruited from the Third People' s Hospital of Taiyuan, from July 2011 to January 2013. According to the situation of Telbivudine intake in second and third trimesters of pregnancy, the participants were divided into two groups: with Telbivudine-treated or as control. The neonates were followed up till the age of 12 months. Maternal, neonatal and infantile HBV-M together with HBV DNA in serum were measured using the electro-chemiluminescence immuno-assay (ECLIA) kits and fluorescence quantitative polymerase chain reaction (FQ-PCR) assay, respectively. Results: The rate of non-/hypo-response was 17.99%. After adjusting the potential confounding factors, the Telbivudine treatment on HBsAg-positive mothers in the second and third trimesters of pregnancy seemed as the protective factor for non-/hypo-response to hepatitis B vaccine in infants (aRR=0.119, 95% CI: 0.014-0.974). Levels of IFN-gamma and IL-10 in Telbivudine-treated group were higher than those in the controls (aRR=8.684, 95%CI: 1.977-38.140; aRR=5.330, 95% CI: 1.278-22.236). When the serum levels of IFN-gamma and IL-10 in neonatal peripheral blood were higher than 228.47 pg/ml and 174.05 pg/ml respectively, the infants were less likely to be non-/hypo-responsive to the hepatitis B vaccine (aRR=0.300, 95%CI: 0.105-0.857) (aRR= 0.104, 95% CI: 0.030-0.354). Conclusion: Telbivudine treatment provided for the HBsAg-positive mothers in second and third trimesters of pregnancy were less likely to develop non-/low-responsive to hepatitis B vaccine in infants since IFN-gamma and IL-10 might have played a vital role in this process.
Entecavir to Telbivudine Switch Therapy in Entecavir-Treated Patients with Undetectable Hepatitis B Viral DNA.[Pubmed:28332360]
Yonsei Med J. 2017 May;58(3):552-556.
PURPOSE: This study examined 2-year outcome of consecutive therapy using entecavir (ETV) followed by Telbivudine (LdT) in subjects with undetectable hepatitis B virus (HBV) DNA level and normal alanine aminotransferase level after the initial 6 months of ETV treatment. MATERIALS AND METHODS: Sixty subjects were randomized to continue with ETV or switch to LdT. Significant difference in baseline characteristics was not found between the two groups. Persistent HBV DNA level of 20-60 IU/mL in three consecutive samples collected three months apart or singly measured HBV DNA level of >60 IU/mL was defined as virological rebound. RESULTS: During 96 weeks of follow-up, all subjects of the ETV-only group (n=30) resulted in undetectable HBV DNA level. On the other hand, 83.3% (n=25) of the LdT-switched group showed treatment success. Virological rebound time varied from week 24 to 84 after switching to LdT. HBV DNA level was 180 to 2940 IU/mL at rebound time. All subjects with virological rebound (n=5) showed drug-resistant mutation: three had mutation rtM204I, and two had mutation rtM204V. Consecutive treatment using ETV followed by LdT showed virological rebound in 16.7% of subjects during 96 weeks of follow-up. HBV DNA negativity during initial ETV therapy could not be achieved in patients who switched to LdT. CONCLUSION: Consecutive treatment using ETV followed by lamivudine was ineffective for treating chronic hepatitis B. LdT was found as a more potent antiviral agent than lamivudine. However, this conclusion requires larger-scale, long-term prospective reviews of the treatment effects of ETV-LdT switch therapy.
Telbivudine attenuates gentamicin-induced kidney injury in rats.[Pubmed:28373116]
Int J Antimicrob Agents. 2017 May;49(5):595-602.
Nephrotoxicity has been associated with nucleos(t)ide analogues other than Telbivudine (LdT). This study investigated the potential effects of LdT and lamivudine (LAM) on renal function in an experimental rat model of gentamicin-induced acute nephrotoxicity. A total of 28 healthy Wistar albino rats were randomly divided into four experimental groups: negative control; positive control (PC); LdT; and LAM. Nephrotoxicity was induced by gentamicin in the LdT, LAM and PC groups. LdT and LAM were administered to two groups for 6 weeks starting on the ninth day. Blood samples were collected weekly and cystatin C levels were measured by ELISA. Animals were sacrificed on the 50th day and the kidneys were removed for histological examination. Serum cystatin C levels differed significantly between the LdT and LAM groups (P <0.007) and between the LdT and PC groups (P <0.001). Renal function was significantly improved in the LdT group at the start of antiviral treatment on Day 8 and at the end of treatment on Day 50 (P = 0.001 and 0.007). Glomerular injury, acute tubular necrosis and total injury score were significantly reduced in the LdT group relative to the PC and LAM groups upon histopathological examination. LdT was associated with significant improvements in renal function as measured by biochemical and histopathological methods. The acute kidney injury model data should be supported by clinical studies to suggest that LdT treatment may have advantages for patients with underlying chronic kidney disease receiving chronic hepatitis B treatment.
Comparison of telbivudine and entecavir on the change of off- treatment eGFR after 3 years of treatment in non-cirrhotic chronic hepatitis B patients.[Pubmed:28137301]
BMC Gastroenterol. 2017 Jan 31;17(1):22.
BACKGROUND: The change of estimated glomerular filtration rate (eGFR) with off-treatment nucleos(t)ide analogues (NA) in chronic hepatitis B patients (CHB) is unclear. This study is aimed to evaluate the off-treatment eGFR after 3 years of therapy with Telbivudine (LdT) or entecavir (ETV) and to assess predictive factors for eGFR improvement. METHODS: From January 2009 to December 2011, we identified NA-naive patients who were at least 20 years of age diagnosed with compensated CHB. All patients received a 3-year NA treatment and 1 year off-treatment follow-up; the initial selection of patients for LdT or ETV treatment was at the physicians' discretion. An increase of more than 10% in eGFR from the baseline was identified as an improvement. The change of chronic kidney disease stages were recorded and compared with baseline at year 3 and year 4, respectively. RESULTS: This study included two groups consisting of 46 patients each (each with3 years of treatment with LdT or ETV). In LdT-treated patients, the mean eGFR increased from 94.3 +/- 28.3 to 104.0 +/- 31.2 mL/min/1.73 m(2) in year 3 (p = 0.01) and from 104.0 +/- 31.2 to 104.0 +/- 28.8 mL/min/1.73 m(2) in year 4 (p = 0.99). However, in ETV-treated patients, the mean eGFR decreased from 93.1 +/- 26.1 to 85.5 +/- 25.1 mL/min/1.73 m(2) in year 3 (p = 0.0009) and from 85.5 +/- 25.1 to 87.7 +/- 24.8 mL/min/1.73 m(2) in year 4 (p = 0.2). After a multivariate analysis, the predictors for the off-treatment eGFR improvement were the LdT treatment (odds ratio [OR], 3.97 (1.37-11.5), p = 0.01) and pre-treated eGFR (OR, 0.98 (0.95-1.00), p = 0.04). CONCLUSIONS: At year 4, 48.8 and 21.3% patients had an improved eGFR from baseline in LdT and ETV patients, respectively. Telbivudine may have a protective renal effect that can last for one year after treatment in non-cirrhotic CHB patients without a virological breakthrough.
