1236287-04-9|马来酸替诺福韦|Tenofovir maleate|-范德生物科技公司

马来酸替诺福韦

NMR下载 COA and HPLC MSDS下载
names：
Tenofovir maleate
CAS号：
1236287-04-9
MDL Number：
MF(分子式)： C13H18N5O8P MW(分子量)： 403.28
EINECS: Reaxys Number:
Pubchem ID:53302693 Brand:BIOFOUNT

马来酸替诺福韦(1236287-04-9,Tenofovir maleate,GS 1278,PMPA)是一种抗逆转录病毒药物，被称为核苷酸类似物逆转录酶抑制剂（NRTIs），可阻断逆转录酶，HIV-1和HBV中的关键病毒酶。IC50值：0.5-2.2 uM（HIV-1）；1.6-4.9 uM（HIV-2）；目标：NRTI；体外：替诺福韦水合物可降低HIV-1（IIIB），HIV-2（ROD）和HIV（EHO）的病毒细胞病变作用，EC50为1.15μg/ mL，1.12μg/ mL和1.05μg/ mL。 MT-4细胞。

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中文别名	马来酸替诺福韦(1236287-04-9);替诺福韦(马来酸酯);替诺福韦;替诺福韦富马酸替索罗非酯;替诺福韦马来酸盐;
英文别名	Tenofovir maleate(1236287-04-9);Tenofovir (maleate);SCHEMBL16628568;HY-13910B;CS-1875; Viread maleate; GS 1278 maleate; GS1278 maleate; GS-1278 maleate; PMPA maleate; TDF maleate;
CAS号	1236287-04-9
SMILES	C[C@@H](OCP(O)(O)=O)CN1C=NC2=C(N)N=CN=C12.O=C(O)/C=C\C(O)=O
Inchi	InChI=1S/C9H14N5O4P.C4H4O4/c1-6(18-5-19(15,16)17)2-14-4-13-7-8(10)11-3-12-9(7)14;5-3(6)1-2-4(7)8/h3-4,6H,2,5H2,1H3,(H2,10,11,12)(H2,15,16,17);1-2H,(H,5,6)(H,7,8)/b;2-1-/t6-;/m1./s1
InchiKey	OPQKUDVCYGLXAH-REVJHSINSA-N
分子式 Formula	C13H18N5O8P
分子量 Molecular Weight	403.28
闪点 FP	No data available
熔点 Melting point	No data available
沸点 Boiling point	No data available
Polarizability极化度
密度 Density	No data available
蒸汽压 Vapor Pressure
溶解度Solubility
性状	Solid
储藏条件 Storage conditions	请根据产品建议的存储条件进行存储,Please store the product under the recommended condition sin the description.

马来酸替诺福韦(1236287-04-9,Tenofovir maleate,GS 1278,PMPA)实验注意事项：
1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

Tags:GS 1278试剂,GS 1278杂质,GS 1278合成,GS 1278中间体,GS 1278密度,GS 1278溶解度,GS 1278旋光度,GS 1278购买,GS 1278闪点,

产品说明	马来酸替诺福韦(1236287-04-9,Tenofovir maleate,GS 1278,PMPA)是一种用于治疗艾滋病毒和慢性乙型肝炎的核苷酸逆转录酶抑制剂.
Introduction	马来酸替诺福韦(1236287-04-9,Tenofovir maleate,GS 1278,PMPA)is a nucleotide reverse transcriptase inhibitor used to treat HIV and chronic hepatitis B.
Application1	Tenofovir (Maleate) is anucleotide reverse transcriptase inhibitorto treat HIV and chronic Hepatitis B.
Application2	Tenofovir (Maleate)是一种核苷酸逆转录酶抑制剂，可用于治疗HIV和慢性乙型肝炎。
Application3

马来酸替诺福韦(1236287-04-9,Tenofovir maleate,GS 1278,PMPA)药理学：

※马来酸替诺福韦是一种用于治疗艾滋病毒和慢性乙型肝炎的核苷酸逆转录酶抑制剂。

※马来酸替诺福韦(1236287-04-9,Tenofovir maleate,GS 1278,PMPA)是一种抗逆转录病毒药物，被称为核苷酸类似物逆转录酶抑制剂（NRTIs），可阻断逆转录酶，HIV-1和HBV中的关键病毒酶。IC50值：0.5-2.2 uM（HIV-1）；1.6-4.9 uM（HIV-2）；目标：NRTI；体外：替诺福韦水合物可降低HIV-1（IIIB），HIV-2（ROD）和HIV（EHO）的病毒细胞病变作用，EC50为1.15μg/ mL，1.12μg/ mL和1.05μg/ mL。 MT-4细胞。

※Tenofovir hydrate reduces the viral cytopathic effect of HIV-1(IIIB), HIV-2(ROD) and HIV(EHO) with EC50 of 1.15 μg/mL, 1.12 μg/mL and 1.05 μg/mL in MT-4 cells. Tenofovir hydrate also reduces the viral cytopathic effect of SIV(mac251) , SIV(B670) ,SHIV(89.6) and SHIV(RTSHIV). Tenofovir hydrate inhibits hepatitis B virus (HBV) activity in HepG2 2.2.15, HepAD38 and HepAD79 cells. Tenofovir hydrate (4 μM) completely inhibits the growth of HIVIIIB in MT-2 cells. Tenofovir hydrate inhibits synthesis of negative strand strong-stop DNA with IC50 of 9 ?M for wild-type RT, 6 ?M for M184V RT and 50 ?M for K65R RT.
Tenofovir hydrate (30 mg/kg) completely prevents SIV infection in all macaques without toxicity. Tenofovir hydrate treatment reduces plasma viral RNA levels to undetectable, with parallel decreases in the infectivity of plasma and infectious cells in peripheral blood mononuclear cells and cerebrospinal fluid (CSF) and stabilization of CD4+ T-cell numbers. Tenofovir hydrate (30 mg/kg, s.c.) completely abrogates HIV infection via intravaginal exposure in pig-tailed macaques.

警示图
危险性	warning
危险性警示	Not available
安全声明	H303吞入可能有害+H313皮肤接触可能有害+H2413吸入可能对身体有害
安全防护	P264处理后彻底清洗+P280戴防护手套/穿防护服/戴防护眼罩/戴防护面具+P305如果进入眼睛+P351用水小心冲洗几分钟+P338取出隐形眼镜（如果有）并且易于操作,继续冲洗+P337如果眼睛刺激持续+P2393获得医疗建议/护理
备注	实验过程中防止吸入、食入，做好安全防护

Murphy RA, et al. Establishment of HK-2 Cells as a Relevant Model to Study Tenofovir-Induced Cytotoxicity. Int J Mol Sci. 2017 Mar 1;18(3).

Musumeci G, et al. M48U1 and Tenofovir combination synergistically inhibits HIV infection in activated PBMCs and human cervicovaginal histocultures. Sci Rep. 2017 Feb 1;7:41018.

Wahl A, et al. Predicting HIV Pre-exposure Prophylaxis Efficacy for Women using a Preclinical Pharmacokinetic-Pharmacodynamic In Vivo Model. Sci Rep. 2017 Feb 1;7:41098.

Menne S, Cote PJ, Korba BE, Antiviral effect of oral administration of tenofovir disoproxil fumarate in woodchucks with chronic woodchuck hepatitis virus infection. Antimicrob Agents Chemother. 2005 J

马来酸替诺福韦(1236287-04-9,Tenofovir maleate,GS 1278,PMPA)参考文献：

1、An improved process for the preparation of tenofovir disoproxil and pharmaceutically acceptable salts thereof

JANEBA ZLATLO (CZ)JANSA PETR (CZ)KOLMAN VICTOR (CZ)BASZCZYNSKI ONDREJ (CZ)RAK JAKUB (CZ)

Abstract An improved process for the preparation of Tenofovir disoproxil and pharmaceutically acceptable salts thereof, comprising following steps: a) alkylation of adenine with ( R )-4-methyl-1,3-dioxolan-2-one and isolation of ( R )-1-(6-amino-9H-purin-9-yI)propan-2-ol; b) alkylation of ( R )-1-(6-amino-9H-purin-9-yl) propan-2-ol with a dialkyl p-toluenesulphonyloxymethylphosphonate or dialkyl halomethylphosphonate to give dialkylester of ( R )-9-[2-(phosphonomethoxy)propyl]adenine; c) preparation of ( R )-9-[2-(phosphonomethoxy)propyl]adenine (( R )-PMPA; Tenofovir) by dealkylation of the phosphonate moiety with a mineral acid under microwave irradiation; d) preparation of Tenofovir disoproxil; e) preparation of the fumarate salt or other pharmaceutically acceptable salt of Tenofovir disoproxil.

2、An improved process for the preparation of Tenofovir disoproxil and pharmaceutically acceptable salts thereof

JANEBA ZLATKO (CZ)JANSA PETR (CZ)KOLMAN VIKTOR (CZ)BASZCZYNSKI ONDREJ (CZ)RAK JAKUB (CZ)

Abstract An improved process for the preparation of Tenofovir disoproxil and pharmaceutically acceptable salts thereof, comprising following steps: na) alkylation of adenine with ( R )-4-methyl-1,3-dioxolan-2-one and isolation of ( R )-1-(6-amino-9 H -purin-9-yl)propan-2-ol; nb) alkylation of ( R )-1-(6-amino-9 H -purin-9-yl) propan-2-ol with a dialkyl p-toluenesulphonyloxymethylphosphonate or dialkyl halomethylphosphonate to give dialkylester of (R)-9-[2-(phosphonomethoxy)propyl]adenine; nc) preparation of (R)-9-[2-(phosphonomethoxy)propyl]adenine (( R )-PMPA; Tenofovir) by dealkylation of the phosphonate moiety with a mineral acid under microwave irradiation; nd) preparation of Tenofovir disoproxil; ne) preparation of the fumarate salt or other pharmaceutically acceptable salt of Tenofovir disoproxil.

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