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39

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T12715	Reverse transcriptase-IN-1	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	Reverse transcriptase-IN-1 是一种二芳基苯并嘧啶类似物，是一种有效的 HIV-1 非核苷类逆转录酶抑制剂，IC50 为 13.7 nM。
T2330	Rilpivirine TMC278,R278474,利匹韦林,DB08864	HIV Protease; Reverse Transcriptase	Microbiology/Virology; Proteases/Proteasome
	Rilpivirine (R278474) 是一种二芳基嘧啶衍生物和非核苷逆转录酶抑制剂，具有抗 HIV-1 的抗病毒活性，用于治疗 HIV 感染。
T0682	Lamivudine GR109714X,BCH-189,拉米夫定	HIV Protease; Reverse Transcriptase	Microbiology/Virology; Proteases/Proteasome
	Lamivudine (BCH-189) 是一种核苷逆转录酶抑制剂，可抑制HIV 逆转录酶1和2 以及乙型肝炎病毒的逆转录酶。
T3632	Doravirine 多拉维林,多拉韦林,MK-1439	HIV Protease; Reverse Transcriptase	Microbiology/Virology; Proteases/Proteasome
	Doravirine (MK-1439) 是一种高度特异性的HIV-1非核苷逆转录酶抑制剂，对野生型以及K103N 和Y181C 逆转录酶突变体的IC50值分别为 4.5 nM，5.5 nM 和 6.1 nM。
T1595	Nevirapine NSC 641530,奈韦拉平,BI-RG 587,奈伟拉平,NVP	HIV Protease; Reverse Transcriptase	Microbiology/Virology; Proteases/Proteasome
	Nevirapine (NVP) 是一种 HIV-1逆转录酶非核苷抑制剂，Ki 值为 270 μM，可用于研究 HIV/AIDS。
T29037	UC-781 NSC 675186,UC781,UC 781	Antiviral; HIV Protease	Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	UC-781 (NSC-675186) 是一种高效且具有选择性的人类免疫缺陷病毒 HIV-1 非核苷类逆转录酶(NNRTI)I抑制剂，C50 值为 5 nM。UC-781 具有抗病毒活性和耐药性。UC-781状态稳定，较低的 PH 或不同温度对其影响较小。
T14313	Apricitabine AVX754,SPD754	HIV Protease; DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology; Proteases/Proteasome
	Apricitabine (SPD754) 是一种具有高选择性和口服活性的HIV-1逆转录酶抑制剂(Ki=0.08μM)，是2′-脱氧-3′-氧-4′-硫代胞苷(dOTC)的(-)对映体。 Apricitabine 对DNA 聚合酶α、β和γ具有抑制作用，Ki 值分别为300μM、12μM 和112.25μM。Apricitabine 在抗逆转录病毒HIV 感染者中显示出良好的抗逆转录病毒治疗效果，具有良好的耐受性和较低的选择性抗性。
T15776	Loviride R 89439	Others	Others
	Loviride is a non-nucleoside reverse transcriptase inhibitor (IC50: 0.3 µM). Loviride inhibits HIV-1, HIV-2 and SIV replication in MT-4 cells. It is used for reverse transcriptase from HIV-1.
T72206	Reverse transcriptase-IN-4
	Reverse transcriptase-IN-4 是一种有效的选择性非核苷类逆转录酶 (NNRT) 抑制剂，作用于野生型HIV-1的EC50值为 0.053 μM，作用于HIV-1突变株 E138K 的EC50值为 0.26 μM。
T27442	GSK 224876 GSK-224876,GSK224876
	GSK 224876 is a novel next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI). It has activity against efavirenz-resistant strains in the treatment of treatment-naive HIV-1-infected subjects.
T28811	SM111 SM 111,SM-111
	SM111 inhibits in vitro replication of HIV-1, including strains resistant to reverse transcriptase, licensed protease, and integrase inhibitors, without major cellular toxicity.
T10141	4'-Ethynyl-2'-deoxyadenosine	Others	Others
	4'-Ethynyl-2'-deoxyadenosine (4'-E-dA) is a nucleoside reverse transcriptase (RT) inhibitor. It is potent against drug-resistant HIV variants (EC50: 98 nM in MT-4 cells for anti-HIV-1 activity).
T24839	Stampidine HI-113,HI 113,HI113
	Stampidine can prevent the sexual transmission of HIV-1. It exhibited remarkable subnanomolar to low nanomolar in vitro antiretroviral potency against nucleoside reverse transcriptase inhibitor-resistant primary clinical HIV isolates, non-nucleoside RT-re
T72203	Reverse transcriptase-IN-3
	Reverse transcriptase-IN-3, 作为一种嘧啶-5-羧酰胺衍生物，主要用于抑制HIV-1。它对HIV-1野生型及其突变型病毒株均展示出高效的抑制活性。
T69382	INDOPY-1
	INDOPY-1 is a Nucleotide-Competing Reverse Transcriptase Inhibitor. INDOPY-1 was the first NcRTI discovered, displaying reversible competitive inhibition of dNTP binding. 3,4 Biochemical studies showed that INDOPY-1 arrests RT/DNA in a post-translocated (P site) complex.
T64303	ZLM-66
	ZLM-66 是一种多拉维林 (Doravirine) 类似物，也是一种 non-nucleoside reverse transcriptase (NNRTIs) 的有效抑制剂，能够作用于野生型 HIV-1 逆转录酶 (IC50: 41 nM)、野生型 HIV-1 (EC50: 13 nM)。ZLM-66 能够用于研究艾滋病 (AIDS)。
T61679	Abacavir monosulfate
	Abacavir monosulfate is an orally active, competitive nucleoside reverse transcriptase inhibitor that effectively inhibits HIV replication. Additionally, it exhibits anticancer properties in prostate cancer cell lines, and has the ability to penetrate the blood-brain-barrier and suppress telomerase activity [1] [2] [3].
T28494	R-82913 NSC 637653, 9-Cl-Tibo,R 82913,R82913. 9-Cmbib
	R-82913 is a RNA-directed DNA polymerase inhibitor. R 82913 reduce 5-HT2 receptor-mediated DOI-head-shakes in mice. R82913 inhibited the replication of thirteen different strains of HIV-1 in CEM cells with a median IC50 of 0.15 microM. R82913 was 20-fold
T26581	AIC-292
	AIC-292 is a potent reverse transcriptase inhibitor with well tolerated in different cell lines. In addition, activity of AIC292 could be demonstrated against a broad panel of wild-type HIV-1 group. AIC292 also retained activity against viruses harboring
FL0097	beta-L-D4A 2'3'-didehydro-2'3'-dideoxyadenosine
	beta-L-D4A 是一种核苷类型的HIV-1逆转录酶抑制剂。
T69627	Dapivirine HCl
	Dapivirine HCl is the salt form of Dapivirine, also known as TMC120, a non-nucleoside inhibitor for HIV reverse transcriptase with IC50 of 24 nM. The HIV-1 replication inhibitor dapivirine (DPV) is one of the most promising drug candidates being used in topical microbicide products for prevention of HIV-1 sexual transmission.
T41110	EFdA-TP
	EFdA-TP, a highly potent nucleoside reverse transcriptase (RT) inhibitor, exerts its inhibitory effect on RT-catalyzed DNA synthesis through both immediate and delayed chain termination mechanisms, commonly referred to as ICT and DCT, respectively. Additionally, EFdA-TP demonstrates its efficacy in inhibiting HIV-1 RT through multiple pathways.
T78737	NNRTIs-IN-3	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	NNRTIs-IN-3（化合物8）作为一种HIV-1非核苷逆转录酶抑制剂，表现出较高的效力（EC50=0.01 µM）。
T62690	HIV-1 inhibitor-46
	HIV-1 inhibitor-46 (compound 13d) 是一种 HIV-1 非核苷类逆转录酶的有效抑制剂 (EC50: 1.425 μM)。HIV-1 inhibitor-46 能够用于研究艾滋病 (AIDS)。
T27768	L-696229 L696,229,L-696,229,L 696229,L696229,L 696,229
	L-696229 is a specific inhibitor of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT). L-696229 inhibited RT activity in a mutually exclusive manner with respect to either phosphonoformate or azidothymidine triphosphate and was a weak
T72563	HIV-1 inhibitor-49
	HIV-1inhibitor-49 是一种口服有效的 HIV-1抑制剂，是一种 HEPT 类似物。HIV-1inhibitor-49 具有良好的药代动力学特征和有效的非核苷类逆转录酶 (Reverse Transcriptase ; IC50=30 nM) 抑制活性。HIV-1inhibitor-49 具有潜在的安全性，对小鼠无急性毒性。
T64048	HIV-IN-5
	HIV-IN-5 (compound 5r) 是 HIV-1 的有效抑制剂 (IC50: 0.16 μM)。HIV-IN-5 能够与 NNIBP (NNRTIs (非核苷逆转录酶抑制剂) 结合位点) 相结合。HIV-IN-5 能够抑制 HIV DNA 依赖的 DNA 聚合作用 (IC50: 2.18 μM)。
T64009	HIV-1 inhibitor-23
	HIV-1 inhibitor-23 是 HIV-1 非核苷逆转录酶的高效抑制剂，能够作用于野生型 HIV-1 (EC50: 24.9 nM) 和突变病毒株 K103N (EC50: 10.4 nM)。HIV-1 inhibitor-23 的细胞毒性较低 (CC50> 221 μM)，并具有良好的体外微粒体稳定性。
T83837	Rp-Thymidine-5'-O-(1-thiotriphosphate) sodium Rp-dTTP-α-S
	Rp-Thymidine-5'-O-(1-thiotriphosphate) (Rp-TTP-α-S) 是含硫核苷酸衍生物 TTP-α-S 的一个异构体。它能与HIV-1逆转录酶结合（在镁、锰酸盐和钴存在下的Kds分别为45.7、27.32和39.44 µM）。
T78979	HIV-1 inhibitor-56
	HIV-1 inhibitor-56 (compound 12126065)为一有效HIV-1非核苷逆转录酶抑制剂，其在TZM细胞中对野生型HIV-1显示出高效的抗病毒活性，EC50仅为0.24 nM，并能穿透血脑屏障。
T62452	HIV-1 inhibitor-40
	HIV-1 inhibitor-40 (Compound 4ab) 是一种 HIV-1 非核苷型逆转录酶抑制剂 (NNRTI) (EC50: 1.9 nM)，体内没有明显急性毒性。HIV-1 inhibitor-40 对 CYP 的敏感性较低，作用于 CYP2C9 (IC50: 5.16 μM) 和 CYP2C19 (IC50: 4.51 μM)。
T78948	NNRTIs-IN-1
	NNRTIs-IN-1是一种非核苷逆转录酶抑制剂, 对野生型HIV-1及五种突变株表现出有效抑制作用, 其EC50值处于纳摩尔量级。该化合物同时展现出优良的药代动力学性质, 并具备显著的抗抗药性特点。
T78749	HIV-1 inhibitor-57
	HIV-1 inhibitor-57（Compound 12g）是抗HIV药物。该化合物对野生型及五种常见NNRTI耐药HIV-1株均表现出抗病毒活性，具有0.024至0.0010 μM的EC 50值。HIV-1 inhibitor-57能够与HIV-1RT的结合位点附近残基形成附加相互作用。
T35428	β-Rubromycin
	β-Rubromycin is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities.1 It inhibits the growth of HMO2, KATO-III, and MCF-7 cells with GI50 values of 0.5, 0.84, and <0.1 μM, respectively. β-rubromycin inhibits HIV-1 reverse transcriptase activity by 39.7% when used at a concentration of 10 μM. It also has antibacterial activity against Gram-positive bacteria. The structure of β-rubromycin was originally described as containing an ortho-quinone group,...
T81431	Pol (476-484), HIV-1 RT Epitope
	Pol (476-484),HIV-1RT Epitope 是具有生物活性的肽，对应逆转录酶 (RT) 的主要HLA A*0201限制性表位（Pol 残基 476-484）。其在HIV-1 RT中的角色涉及分析CTL逃逸机制。实际表位IV9在HIV-1感染的细胞系中被加工和呈现。
T83838	Sp-Thymidine-5'-O-(1-thiotriphosphate) sodium Sp-TTP-α-S
	Sp-Thymidine-5'-O-(1-thiotriphosphate)（Sp-TTP-α-S）是含硫核苷酸衍生物TTP-α-S的一个异构体。它能够结合HIV-1逆转录酶（在镁、锰酸盐和钴存在时，Kds分别为2.88、4.23和20.21 µM）。Sp-TTP-α-S抑制脱氧核苷酸三磷酸三磷酸水解酶SAMHD1（Ki为46 nM）。
T83818	Isoguanosine-5'-O-triphosphate sodium 2-Hydroxyadenosine 5’-triphosphate,2-hydroxy ATP,isoGTP
	Isoguanosine-5'-O-triphosphate是guanosine 5'-triphosphate（GTP）的一个异构体且是crotonoside的磷酸化形式。与GTP不同，Isoguanosine-5'-O-triphosphate不促进微管组装。在逆转录酶实验中，Isoguanosine-5'-O-triphosphate（2 mM）能抑制转录并诱导T到C的突变。它已被用于确定phosphofructokinase和mutT homolog 1（MTH1）的底物特异性。
T78925	HIV-1 inhibitor-58
	HIV-1inhibitor-58（Compound 10c）是一款抗逆转录病毒活性的广谱非核苷逆转录酶抑制剂，有效抑制MT-4细胞中的HIV-1 WT株IIIB以及NNRTI耐药菌株，如K103N和E138K（EC50 < 50 nM）。此外，HIV-1inhibitor-58对CYP2C9与CYP2C19也表现出抑制作用（IC50分别为2.06 μM与1.91 μM），适用于HIV感染研究。
T81738	Murabutide
	Murabutide是一种合成的安全免疫调节剂，能够降低CD4和CCR5受体的表达，并促使β-趋化因子的高水平分泌，从而增强机体对病毒感染的非特异性防御能力。此外，Murabutide不会干扰病毒的进入过程、逆转录酶的活性或是在感染细胞的细胞质中早期前病毒DNA的形成。

化合物

Reverse transcriptase-IN-1

Cat.No: T12715

Target: HIV Protease

Cat.No: T2330

Synonym: TMC278,R278474,利匹韦林,DB08864

Target: HIV Protease, Reverse Transcriptase

Cat.No: T0682

Synonym: GR109714X,BCH-189,拉米夫定

Target: HIV Protease, Reverse Transcriptase

Cat.No: T3632

Synonym: 多拉维林,多拉韦林,MK-1439

Target: HIV Protease, Reverse Transcriptase

Cat.No: T1595

Synonym: NSC 641530,奈韦拉平,BI-RG 587,奈伟拉平,NVP

Target: HIV Protease, Reverse Transcriptase

Cat.No: T29037

Synonym: NSC 675186,UC781,UC 781

Target: Antiviral, HIV Protease

Cat.No: T14313

Synonym: AVX754,SPD754

Target: HIV Protease, DNA/RNA Synthesis

Cat.No: T15776

Synonym: R 89439

Target: Others

Reverse transcriptase-IN-4

Cat.No: T72206

Cat.No: T27442

Synonym: GSK-224876,GSK224876

Cat.No: T28811

Synonym: SM 111,SM-111

4'-Ethynyl-2'-deoxyadenosine

Cat.No: T10141

Target: Others

Cat.No: T24839

Synonym: HI-113,HI 113,HI113

Reverse transcriptase-IN-3

Cat.No: T72203

Cat.No: T69382

Cat.No: T64303

Abacavir monosulfate

Cat.No: T61679

Cat.No: T28494

Synonym: NSC 637653, 9-Cl-Tibo,R 82913,R82913. 9-Cmbib

Cat.No: T26581

Cat.No: FL0097

Synonym: 2'3'-didehydro-2'3'-dideoxyadenosine

Cat.No: T69627

Cat.No: T41110

Cat.No: T78737

Target: HIV Protease

HIV-1 inhibitor-46

Cat.No: T62690

Cat.No: T27768

Synonym: L696,229,L-696,229,L 696229,L696229,L 696,229

HIV-1 inhibitor-49

Cat.No: T72563

Cat.No: T64048

HIV-1 inhibitor-23

Cat.No: T64009

Rp-Thymidine-5'-O-(1-thiotriphosphate) sodium

Cat.No: T83837

Synonym: Rp-dTTP-α-S

HIV-1 inhibitor-56

Cat.No: T78979

HIV-1 inhibitor-40

Cat.No: T62452

Cat.No: T78948

HIV-1 inhibitor-57

Cat.No: T78749

Cat.No: T35428

Pol (476-484), HIV-1 RT Epitope

Cat.No: T81431

Sp-Thymidine-5'-O-(1-thiotriphosphate) sodium

Cat.No: T83838

Synonym: Sp-TTP-α-S

Isoguanosine-5'-O-triphosphate sodium

Cat.No: T83818

Synonym: 2-Hydroxyadenosine 5’-triphosphate,2-hydroxy ATP,isoGTP

HIV-1 inhibitor-58

Cat.No: T78925

Cat.No: T81738

Cat. No.	Product Name	Target	Signaling Pathways
T4S1718	Punicalin	HBV; HIV Protease	Microbiology/Virology; Proteases/Proteasome
	Punicalin 是从Punica granatumL. 或Terminalia catappaL. 的叶子中分离的，一种可水解的单宁，具有抗炎活性。它是一种抗乙型肝炎病毒药物。
TN5243	Vitexilactone	NADPH-oxidase; HIV Protease; Antifection	Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	Vitexilactone is a HIV-1 reverse transcriptase inhibitor in virtual screening against Indonesian Herbal Database using AutoDock4 performed on HIV-1 reverse transcriptase. It has trypanocidal activity, the minimum lethal concentration against epimastigotes
T74196	Inophyllum B
	Inophyllum B ((+)-Inophyllum B) 是一种有效的HIV 逆转录酶 (Reverse Transcriptase) 抑制剂，IC50为 38 nM。Inophyllum B 在体外细胞培养中抑制HIV-1(IC50=1.4 μM)。Inophyllum B 可从非洲大蜗牛Achatina fulica 的丙酮提取物中分离得到。
TN5133	3',5,5',7-Tetrahydroxy-4',6-dimethoxyflavone	HIV Protease; Topoisomerase	DNA Damage/DNA Repair; Microbiology/Virology; Proteases/Proteasome
	5,7,3',5'-tetrahydroxy-6,4'-dimethoxyflavone exhibits anti-HIV-1 activity in the anti-syncytium assay using (∆Tat/rev)MC99 virus and 1A2 cell line system, it shows considerably activity against HIV-1 reverse transcriptase. It exhibits cytotoxic activity against P-388 cell lines, it can inhibit DNA topoisomerase IIα activity, which may be responsible for the observed cytotoxicity.

天然产物

Cat.No: T4S1718

Target: HBV, HIV Protease

Cat.No: TN5243

Target: NADPH-oxidase, HIV Protease, Antifection

Cat.No: T74196

3',5,5',7-Tetrahydroxy-4',6-dimethoxyflavone

Cat.No: TN5133

Target: HIV Protease, Topoisomerase

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