701213-36-7|坦姆沙韦|Temsavir|MFCD22665723-范德生物科技公司

坦姆沙韦

NMR下载 COA and HPLC MSDS下载
names：
Temsavir
CAS号：
701213-36-7
MDL Number： MFCD22665723
MF(分子式)： C24H23N7O4 MW(分子量)： 473.484
EINECS:No data available Reaxys Number:No data available
Pubchem ID:11317439 Brand:BIOFOUNT

坦姆沙韦(701213-36-7,Temsavir,BMS-626529)是目前正在开发的HIV-1附着抑制剂新药类别的成员。BMS-663068是BMS-626529的膦酰氧甲基前药，BMS-626529是一种靶向HIV-1 gp120并防止其与CD4（+）T细胞结合的新型小分子附着抑制剂。由于gp120中的异质性，BMS-626529的活性取决于病毒。研究结果表明，BMS-626529应该对大多数HIV-1病毒具有活性，并支持该化合物的持续临床开发。

货品编码	规格	纯度	价格 (¥)	现价(¥)	特价(¥)	库存描述	数量	总计 (¥)
HCC346125-1mg	1mg	97%	¥ 532.00	¥ 532.00		4-7周	- +	¥ 0.00

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中文别名	坦姆沙韦(701213-36-7);BMS-626529;坦沙韦;
英文别名	Temsavir(701213-36-7);BMS-626529;BMS626529; BMS 626529;
CAS号	701213-36-7
Inchi	InChI=1S/C24H23N7O4/c1-15-27-14-31(28-15)22-20-19(18(35-2)13-26-22)17(12-25-20)21(32)24(34)30-10-8-29(9-11-30)23(33)16-6-4-3-5-7-16/h3-7,12-14,25H,8-11H2,1-2H3
InchiKey	QRPZBKAMSFHVRW-UHFFFAOYSA-N
分子式 Formula	C24H23N7O4
分子量 Molecular Weight	473.484
溶解度Solubility	生物体外In Vitro:DMSO溶解度≥ 16.67 mg/mL(35.21 mM)*"≥" means soluble可溶, but saturation unknown溶解度未知.
性状	No data available
储藏条件 Storage conditions	storage at -4℃ (1-2weeks), longer storage period at -20℃ (1-2years)

坦姆沙韦(701213-36-7,Temsavir,BMS-626529)

坦姆沙韦(701213-36-7,Temsavir,BMS-626529)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.

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产品说明	坦姆沙韦(701213-36-7,Temsavir,BMS-626529)可以作为药物杂质对照品以及生物医药类试剂。
Introduction	坦姆沙韦(701213-36-7,Temsavir,BMS-626529)can be used as a reference substance for drug impurities and reagents，only for research.
Application1
Application2
Application3

坦姆沙韦(701213-36-7,Temsavir,BMS-626529)药理学：
坦姆沙韦(701213-36-7,Temsavir,BMS-626529)抗感染,BMS-626529是一种靶向HIV-1 gp120并防止其与CD4 + T细胞结合的新型小分子附着抑制剂; IC50值：;目标：HIVBMS-626529是HIV-1附着新药物类别的成员目前正在开发抑制剂。BMS-663068是BMS-626529的膦酰氧甲基前药，BMS-626529是一种靶向HIV-1 gp120并防止其与CD4（+）T细胞结合的新型小分子附着抑制剂。由于gp120中的异质性，BMS-626529的活性取决于病毒。研究结果表明，BMS-626529应该对大多数HIV-1病毒具有活性，并支持该化合物的持续临床开发。

警示图
危险性	warning
危险性警示	Not available
安全声明	H303+H313+H333
安全防护	P264+P280+P305+P351+P338+P337+P313
备注	实验过程中防止吸入、食入，做好安全防护

Nowicka-Sans B, et al. In vitro antiviral characteristics of HIV-1 attachment inhibitor BMS-626529, the active component of the prodrug BMS-663068. Antimicrobial Agents and Chemotherapy (2012), 56(7)

Nettles RE, et al. Pharmacodynamics, safety, and pharmacokinetics of BMS-663068, an oral HIV-1 attachment inhibitor in HIV-1-infected subjects. J Infect Dis. 2012 Oct 1;206(7):1002-11.

Erster Attachment-Inhibitor gegen HIV-1-Infektion zur Zulassung eingereicht MMW - Fortschritte der Medizin 2020

Drugs in Clinical Development for HIV: Summary and Table Pharmaceutical Medicine 2015

Antivirale Therapie der Zukunft: Was ist in der Pipeline? MMW - Fortschritte der Medizin 2020

坦姆沙韦(701213-36-7,Temsavir,BMS-626529)参考文献：

1.与gp120结合的HIV-1附着抑制剂BMS-626529的同源性模型表明了其独特的作用机理。
Langley DR1, Kimura SR, Sivaprakasam P, Zhou N, Dicker I, McAuliffe B, Wang T, Kadow JF, Meanwell NA, Krystal M. Proteins. 2015 Feb;83(2):331-50. doi: 10.1002/prot.24726. Epub 2014 Dec 23.
HIV-1 gp120 undergoes multiple conformational changes both before and after binding to the host CD4 receptor. BMS-626529 is an attachment inhibitor (AI) in clinical development (administered as prodrug BMS-663068) that binds to HIV-1 gp120. To investigate the mechanism of action of this new class of antiretroviral compounds, we constructed homology models of unliganded HIV-1 gp120 (UNLIG), a pre-CD4 binding-intermediate conformation (pCD4), a CD4 bound-intermediate conformation (bCD4), and a CD4/co-receptor-bound gp120 (LIG) from a series of partial structures. We also describe a simple pathway illustrating the transition between these four states. Guided by the positions of BMS-626529 resistance substitutions and structure-activity relationship data for the AI series, putative binding sites for BMS-626529 were identified, supported by biochemical and biophysical data. BMS-626529 was docked into the UNLIG model and molecular dynamics simulations were used to demonstrate the thermodynamic stability of the different gp120 UNLIG/BMS-626529 models.

2. HIV-1 B和非B亚型的附着抑制剂BMS-626529抗性的遗传屏障。
Fofana DB1, Charpentier C2, Maïga AI3, Lambert-Niclot S1, Sayon S1, Désiré N1, Simon A4, Yazdanpanah Y5, Katlama C6, Descamps D2, Calvez V1, Marcelin AG1, Soulié C7. J Antimicrob Chemother. 2015 Jan;70(1):130-5. doi: 10.1093/jac/dku360. Epub 2014 Sep 30.
OBJECTIVES: The genetic barrier (defined as the number of genetic transitions/transversions needed to produce a resistance mutation) can differ between HIV-1 subtypes. The genetic barrier for the new attachment inhibitor BMS-626529 was evaluated in five HIV-1 subtypes.

3. HIV-1附着抑制剂前药BMS-663068在经历过抗逆转录病毒治疗的受试者中的安全性：第24周分析。
Lalezari J1, Latiff GH2, Brinson C3, Echevarria J4, Treviño-Pérez S5, Bogner JR6, Stock D7, Joshi SR7, Hanna GJ8, Lataillade M7. J Int AIDS Soc. 2014 Nov 2;17(4 Suppl 3):19530. doi: 10.7448/IAS.17.4.19530. eCollection 2014.
INTRODUCTION: BMS-663068 is a prodrug of BMS-626529, an attachment inhibitor that binds directly to HIV-1 gp120, preventing initial viral attachment and entry into the host CD4+ T-cell. AI438011 is an ongoing, Phase IIb, randomized, active-controlled trial investigating the safety, efficacy and dose-response of BMS-663068 vs. atazanavir/ritonavir (ATV/r) in treatment-experienced (TE), HIV-1-positive subjects. At Week 24, response rates across the BMS-663068 arms were consistent with ATV/r.

4，对HIV-1附着抑制剂BMS-626529（前药BMS-663068的活性剂）的易感性的基因型相关性。
Zhou N1, Nowicka-Sans B, McAuliffe B, Ray N, Eggers B, Fang H, Fan L, Healy M, Langley DR, Hwang C, Lataillade M, Hanna GJ, Krystal M. J Antimicrob Chemother. 2014 Mar;69(3):573-81. doi: 10.1093/jac/dkt412. Epub 2013 Oct 14.
OBJECTIVES: In an 8 day monotherapy study of subjects infected with HIV-1 (subtype B) (NCT01009814), BMS-626529 (an attachment inhibitor that binds to HIV-1 envelope glycoprotein gp120), administered as the prodrug BMS-663068, produced substantial declines in plasma HIV-1 RNA. However, large variability in susceptibility to BMS-626529 was noted and virus with low susceptibility was less likely to be suppressed by BMS-663068 administration. The current analysis sought to investigate the genotypic correlates of susceptibility to BMS-626529.METHODS: In vitro selection experiments, evaluation of clinical samples of subtype B from the monotherapy study and evaluation of intrinsically resistant subtype AE viruses were conducted. Reverse genetics was used to identify key substitutions in envelope clones responsible for reduced susceptibility.

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