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馬來(lái)酸替諾福韋

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

馬來(lái)酸替諾福韋(1236287-04-9,Tenofovir maleate,GS 1278,PMPA)是一種抗逆轉(zhuǎn)錄病毒藥物，被稱為核苷酸類似物逆轉(zhuǎn)錄酶抑制劑（NRTIs），可阻斷逆轉(zhuǎn)錄酶，HIV-1和HBV中的關(guān)鍵病毒酶。IC50值：0.5-2.2 uM（HIV-1）；1.6-4.9 uM（HIV-2）；目標(biāo)：NRTI；體外：替諾福韋水合物可降低HIV-1（IIIB），HIV-2（ROD）和HIV（EHO）的病毒細(xì)胞病變作用，EC50為1.15μg/ mL，1.12μg/ mL和1.05μg/ mL。 MT-4細(xì)胞。

貨品編碼	規(guī)格	純度	價(jià)格 (￥)	現(xiàn)價(jià)(￥)	特價(jià)(￥)	庫(kù)存描述	數(shù)量	總計(jì) (￥)
YZM000693-10mg	10mg		￥ 708.00	￥ 708.00		Backorder	- +	￥ 0.00
YZM000693-5mg	5mg	>97%	￥ 453.38	￥ 453.38		2-3天	- +	￥ 0.00

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中文別名	馬來(lái)酸替諾福韋(1236287-04-9);替諾福韋(馬來(lái)酸酯);替諾福韋;替諾福韋富馬酸替索羅非酯;替諾福韋馬來(lái)酸鹽;
英文別名	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號(hào)	1236287-04-9
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
溶解度Solubility
性狀	Solid
儲(chǔ)藏條件 Storage conditions	請(qǐng)根據(jù)產(chǎn)品建議的存儲(chǔ)條件進(jìn)行存儲(chǔ),Please store the product under the recommended condition sin the description.

馬來(lái)酸替諾福韋(1236287-04-9,Tenofovir maleate,GS 1278,PMPA)實(shí)驗(yàn)注意事項(xiàng)：
1.實(shí)驗(yàn)前需戴好防護(hù)眼鏡，穿戴防護(hù)服和口罩，佩戴手套，避免與皮膚接觸。
2.實(shí)驗(yàn)過(guò)程中如遇到有毒或者刺激性物質(zhì)及有害物質(zhì)產(chǎn)生，必要時(shí)實(shí)驗(yàn)操作需要手套箱內(nèi)完成以免對(duì)實(shí)驗(yàn)人員造成傷害
3.實(shí)驗(yàn)后產(chǎn)生的廢棄物需分類存儲(chǔ)，并交于專業(yè)生物廢氣物處理公司處理，以免造成環(huán)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試劑,GS 1278雜質(zhì),GS 1278合成,GS 1278中間體,GS 1278密度,GS 1278溶解度,GS 1278旋光度,GS 1278購(gòu)買,GS 1278閃點(diǎn),

產(chǎn)品說(shuō)明	馬來(lái)酸替諾福韋(1236287-04-9,Tenofovir maleate,GS 1278,PMPA)是一種用于治療艾滋病毒和慢性乙型肝炎的核苷酸逆轉(zhuǎn)錄酶抑制劑.
Introduction	馬來(lái)酸替諾福韋(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)是一種核苷酸逆轉(zhuǎn)錄酶抑制劑，可用于治療HIV和慢性乙型肝炎。
Application3

馬來(lái)酸替諾福韋(1236287-04-9,Tenofovir maleate,GS 1278,PMPA)藥理學(xué)：

※馬來(lái)酸替諾福韋是一種用于治療艾滋病毒和慢性乙型肝炎的核苷酸逆轉(zhuǎn)錄酶抑制劑。

※馬來(lái)酸替諾福韋(1236287-04-9,Tenofovir maleate,GS 1278,PMPA)是一種抗逆轉(zhuǎn)錄病毒藥物，被稱為核苷酸類似物逆轉(zhuǎn)錄酶抑制劑（NRTIs），可阻斷逆轉(zhuǎn)錄酶，HIV-1和HBV中的關(guān)鍵病毒酶。IC50值：0.5-2.2 uM（HIV-1）；1.6-4.9 uM（HIV-2）；目標(biāo)：NRTI；體外：替諾福韋水合物可降低HIV-1（IIIB），HIV-2（ROD）和HIV（EHO）的病毒細(xì)胞病變作用，EC50為1.15μg/ mL，1.12μg/ mL和1.05μg/ mL。 MT-4細(xì)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.

警示圖
危險(xiǎn)性	warning
危險(xiǎn)性警示	Not available
安全聲明	H303吞入可能有害+H313皮膚接觸可能有害+H2413吸入可能對(duì)身體有害
安全防護(hù)	P264處理后徹底清洗+P280戴防護(hù)手套/穿防護(hù)服/戴防護(hù)眼罩/戴防護(hù)面具+P305如果進(jìn)入眼睛+P351用水小心沖洗幾分鐘+P338取出隱形眼鏡（如果有）并且易于操作,繼續(xù)沖洗+P337如果眼睛刺激持續(xù)+P2393獲得醫(yī)療建議/護(hù)理
備注	實(shí)驗(yàn)過(guò)程中防止吸入、食入，做好安全防護(hù)

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

馬來(lái)酸替諾福韋(1236287-04-9,Tenofovir maleate,GS 1278,PMPA)參考文獻(xiàn)：

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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