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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
RT/2-8℃/-20℃
- 保质期：
3年
- 英文名：
Epivir-HBV
- 库存：
999
- 供应商：
北京康瑞纳生物科技有限公司
- CAS号：
134678-17-4
- 规格：
1g
拉米呋啶 134678-17-4 拉米呋啶 134678-17-4
产品名称：拉米呋啶 134678-17-4
产品编号：B2380
中文别称 拉米呋啶
英文别称 Epivir-HBV
CAS 134678-17-4
分子式 C8H.11N3O3S
分子量 229.25
储存条件 RT
纯度 98%
包装 瓶
规格 1g 5g
药理作用
拉米夫定是核苷类抗病毒药，对体外及实验性感染动物体内的乙型肝炎病毒（HBV）有较强的抑制作用。拉米夫定可在HBV感染细胞和正常细胞内代谢生成拉米夫定三磷酸盐，它是拉米夫定的活性形式，既是HBV聚合酶的抑制剂，亦是此聚合酶的底物。拉米夫定三磷酸盐掺入到病毒DNA链中，阻断病毒DNA的合成。拉米夫定三磷酸盐不干扰正常细胞脱氧核苷的代谢，它对哺乳动物DNA聚合酶α和β的抑制作用微弱，对哺乳动物细胞DNA含量几乎无影响。拉米夫定对线粒体的结构、DNA含量及功能无明显的毒性。对大多数乙型肝炎患者的血清HBV DNA检测结果表明，拉米夫定能迅速抑制HBV复制，其抑制作用持续于整个治疗过程。同时使血清转氨酶降至正常，长期应用可显著改善肝脏坏死炎症性改变并减轻或阻止肝脏纤维化的进展。
毒理信息
遗传毒性
拉米夫定在微生物致突变试验和体外细胞转化实验未显示致突变活性，但在体外培养人淋巴细胞和小鼠淋巴瘤实验中显示出其微弱的致突变活性。大鼠经口给予拉米夫定2000mg/kg（血药浓度为慢性乙型肝炎患者推荐临床剂量的60-70倍），未见明显的遗传毒性。
生殖毒性
大鼠经口给予拉米夫定4000mg/kg/天（血药浓度为人临床血药浓度的80-120倍），其生育力和断奶后仔代的存活、生长、发育未受明显影响。
大鼠和家兔分别经口给予拉米夫定4000和1000mg/kg/天（血药浓度约为人临床推荐剂量血药浓度的60倍），均未表现出明显的致畸作用。当家兔血药浓度与人临床推荐剂量的血药浓度相近时，出现早期胚胎死亡率升高。但大鼠血药浓度达到相当于人临床推荐剂量血药浓度的60倍时，未见此类现象发生。对妊娠大鼠和家兔的研究结果显示，拉米夫定可以穿过胎盘进入胎仔体内。尚无拉米夫定用于妊娠妇女的充分和严格对照的临床研究资料。
pharmacological action
Lamivudine is a nucleoside antiviral drug that has a strong inhibitory effect on hepatitis B virus (HBV) in vitro and in experimental infected animals. Lamivudine can be metabolized to produce lamivudine triphosphate in HBV infected cells and normal cells. It is the active form of lamivudine and serves as both an inhibitor and substrate of HBV polymerase. Lamivudine triphosphate is incorporated into the viral DNA strand to block the synthesis of viral DNA. Lamivudine triphosphate does not interfere with the metabolism of deoxyribonucleosides in normal cells, and it affects mammalian DNA polymerase α and β The inhibitory effect is weak and has almost no effect on the DNA content of mammalian cells. Lamivudine has no significant toxicity to the structure, DNA content, and function of mitochondria. The results of serum HBV DNA testing for most hepatitis B patients indicate that lamivudine can rapidly inhibit HBV replication, and its inhibitory effect persists throughout the entire treatment process. At the same time, reducing serum transaminases to normal, long-term use can significantly improve liver necrosis inflammatory changes and alleviate or prevent the progression of liver fibrosis.
Toxicological information
Genetic toxicity
Lamivudine did not show mutagenic activity in microbial mutagenesis experiments and in vitro cell transformation experiments, but showed weak mutagenic activity in vitro cultured human lymphocytes and mouse lymphoma experiments. Rats were orally administered lamivudine 2000mg/kg (blood concentration 60-70 times the recommended clinical dose for chronic hepatitis B patients), and no significant genetic toxicity was ob.served.
Reproductive toxicity
Rats were orally administered 4000mg/kg/day of lamivudine (blood drug concentration 80-120 times higher than human clinical blood drug concentration), but their fertility and survival, growth, and development of weaned offspring were not significantly affected.
Rats and rabbits were orally administered lamivudine 4000 and 1000mg/kg/day respectively (blood drug concentration is about 60 times the recommended clinical dose for humans), but neither showed significant teratogenic effects. When the blood drug concentration of domestic rabbits is similar to the recommended dosage for human clinical use, there is an increase in early embryonic mortality rate. However, no such phenomenon was ob.served when the blood drug concentration in rats reached 60 times the recommended dose for human clinical use. The research results on pregnant rats and rabbits show that lamivudine can penetrate the placenta and enter the fetal body. There is currently no sufficient and strictly controlled clinical research data on the use of lamivudine in pregnant women.
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1、我们保证向用户提供完全合格的产品。如您认为产品确实存在质量问题，请在收到产品7天内提出，否则将不予受理或赔偿。同时产品赔偿只限于产品价值本身，不涉及其他任何损失。我们承诺随时为您提供专业的技术指导。
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产品名称：拉米呋啶 134678-17-4
产品编号：B2380
中文别称 拉米呋啶
英文别称 Epivir-HBV
CAS 134678-17-4
分子式 C8H.11N3O3S
分子量 229.25
储存条件 RT
纯度 98%
包装 瓶
规格 1g 5g
药理作用
拉米夫定是核苷类抗病毒药，对体外及实验性感染动物体内的乙型肝炎病毒（HBV）有较强的抑制作用。拉米夫定可在HBV感染细胞和正常细胞内代谢生成拉米夫定三磷酸盐，它是拉米夫定的活性形式，既是HBV聚合酶的抑制剂，亦是此聚合酶的底物。拉米夫定三磷酸盐掺入到病毒DNA链中，阻断病毒DNA的合成。拉米夫定三磷酸盐不干扰正常细胞脱氧核苷的代谢，它对哺乳动物DNA聚合酶α和β的抑制作用微弱，对哺乳动物细胞DNA含量几乎无影响。拉米夫定对线粒体的结构、DNA含量及功能无明显的毒性。对大多数乙型肝炎患者的血清HBV DNA检测结果表明，拉米夫定能迅速抑制HBV复制，其抑制作用持续于整个治疗过程。同时使血清转氨酶降至正常，长期应用可显著改善肝脏坏死炎症性改变并减轻或阻止肝脏纤维化的进展。
毒理信息
遗传毒性
拉米夫定在微生物致突变试验和体外细胞转化实验未显示致突变活性，但在体外培养人淋巴细胞和小鼠淋巴瘤实验中显示出其微弱的致突变活性。大鼠经口给予拉米夫定2000mg/kg（血药浓度为慢性乙型肝炎患者推荐临床剂量的60-70倍），未见明显的遗传毒性。
生殖毒性
大鼠经口给予拉米夫定4000mg/kg/天（血药浓度为人临床血药浓度的80-120倍），其生育力和断奶后仔代的存活、生长、发育未受明显影响。
大鼠和家兔分别经口给予拉米夫定4000和1000mg/kg/天（血药浓度约为人临床推荐剂量血药浓度的60倍），均未表现出明显的致畸作用。当家兔血药浓度与人临床推荐剂量的血药浓度相近时，出现早期胚胎死亡率升高。但大鼠血药浓度达到相当于人临床推荐剂量血药浓度的60倍时，未见此类现象发生。对妊娠大鼠和家兔的研究结果显示，拉米夫定可以穿过胎盘进入胎仔体内。尚无拉米夫定用于妊娠妇女的充分和严格对照的临床研究资料。
pharmacological action
Lamivudine is a nucleoside antiviral drug that has a strong inhibitory effect on hepatitis B virus (HBV) in vitro and in experimental infected animals. Lamivudine can be metabolized to produce lamivudine triphosphate in HBV infected cells and normal cells. It is the active form of lamivudine and serves as both an inhibitor and substrate of HBV polymerase. Lamivudine triphosphate is incorporated into the viral DNA strand to block the synthesis of viral DNA. Lamivudine triphosphate does not interfere with the metabolism of deoxyribonucleosides in normal cells, and it affects mammalian DNA polymerase α and β The inhibitory effect is weak and has almost no effect on the DNA content of mammalian cells. Lamivudine has no significant toxicity to the structure, DNA content, and function of mitochondria. The results of serum HBV DNA testing for most hepatitis B patients indicate that lamivudine can rapidly inhibit HBV replication, and its inhibitory effect persists throughout the entire treatment process. At the same time, reducing serum transaminases to normal, long-term use can significantly improve liver necrosis inflammatory changes and alleviate or prevent the progression of liver fibrosis.
Toxicological information
Genetic toxicity
Lamivudine did not show mutagenic activity in microbial mutagenesis experiments and in vitro cell transformation experiments, but showed weak mutagenic activity in vitro cultured human lymphocytes and mouse lymphoma experiments. Rats were orally administered lamivudine 2000mg/kg (blood concentration 60-70 times the recommended clinical dose for chronic hepatitis B patients), and no significant genetic toxicity was ob.served.
Reproductive toxicity
Rats were orally administered 4000mg/kg/day of lamivudine (blood drug concentration 80-120 times higher than human clinical blood drug concentration), but their fertility and survival, growth, and development of weaned offspring were not significantly affected.
Rats and rabbits were orally administered lamivudine 4000 and 1000mg/kg/day respectively (blood drug concentration is about 60 times the recommended clinical dose for humans), but neither showed significant teratogenic effects. When the blood drug concentration of domestic rabbits is similar to the recommended dosage for human clinical use, there is an increase in early embryonic mortality rate. However, no such phenomenon was ob.served when the blood drug concentration in rats reached 60 times the recommended dose for human clinical use. The research results on pregnant rats and rabbits show that lamivudine can penetrate the placenta and enter the fetal body. There is currently no sufficient and strictly controlled clinical research data on the use of lamivudine in pregnant women.
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定购方式:
1、确认产品后可直接和我们在线联系确认您购买的产品。
2、可以把您需要购买的产品确认好以邮件的形式发给我们，这样您会在第一时间安排工作人员与您取得联系：给您回复确认的邮件，或者是电话。
邮寄产品:
现货,一般当天定购，24小时内由仓库统一出货
定制期货，出货前由专人通知，仓库备货，依其产品性能，路途等选择进行包装邮寄客户如有特别要求，可与销售人员提前沟通
质量保证与免责声明:
1、我们保证向用户提供完全合格的产品。如您认为产品确实存在质量问题，请在收到产品7天内提出，否则将不予受理或赔偿。同时产品赔偿只限于产品价值本身，不涉及其他任何损失。我们承诺随时为您提供专业的技术指导。
2、如发现产品有任何缺漏或破损，请在收到产品后2个工作日内通知我们。
3、产品使用方法: 详询客服
更多产品请详询客服
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文献和实验该产品被引用文献
Ren L, Liu J, Liu C, Yang T, Wu X, Zhang X, Yang L, Xia J, Li W. AIn Vitro
Cell（RAW264.7 cells；100 ng/mL LPS，24 h at 37 °C）
RAW264.7 cells were seeded in confocal dishes at a density of 1 × 105 cells per dish. After the culture of 24 h, cells were treated with 100 ng/mL LPS in different media, including a control medium, PACDFe extract, and PACDFe hydrogel extract supplemented with 1 μM LL-37 for another 24 h at 2897 °C. 更多文献信息请详询客服
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%1mg/9g细胞Rho1D4 IAC+SECOR131-2 G蛋白偶联受体可诱导的HEK293S细胞系（哺乳动物）90%2.9mg/10g细胞Rho1D4 IAC, +centrifugationhOR17-4 G蛋白偶联受体可诱导的HEK293S细胞系（哺乳动物）90%7.5mg/2.5L, 培养物Rho1D4 IAC+SEChOR17-4 G蛋白偶联受体无细胞小麦胚芽提取物70%*0.3mg/mL, 反应溶液*Rho1D4 IAC+SECCD81 四次跨膜
，周围没有新骨形成。外围型软骨肉瘤瘤体主要在骨外，其表面被覆一层薄而不完整的包膜。以上两型软骨肉瘤均常发生粘液变、出血及囊性变等继发性变化。 镜下观，肿瘤的分化程度差异很大，分化好的软骨肉瘤在镜下易误诊为软骨瘤，但在肿瘤的边缘可以找到瘤细胞的异型性，如核肥大、深染，出现较多的双核、巨核和多核瘤巨细胞，并可见明显核仁（图17-4）。在分化差的软骨肉瘤则上述瘤细胞的异型性很明显，核分裂像也多见。软骨肉瘤的基质可为与一般透明软骨相似的透明基质，也可为粘液样基质，常见于恶性程度高的软骨
光完全衰退后再行测定，所得信号完全为长寿命镧系螯合物的荧光，从而有效地消除非特异性本底荧光的干扰。TR-FIA的测定原理见图17-4。以双抗体夹心法为例的测定反应程序见图17-5。其中增强液的作用是使荧光信号增强。因为免疫反应完成后，生成的抗原－抗体－铕标记物复合物在弱碱性溶液中，经激发后所产生的荧光信号甚弱。在增强液中可至pH2～3，铕离子很容易解离出来，并与增强液中的β-二酮体生成带有强烈荧光的新的铕螯合物，大大有利于荧光测量。 图17-4 TR-FIA
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拉米呋啶 134678-17-4
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