|(2R,3R,4S,5R)-2-(4-氨基吡咯并[2,1-f][1,2,4]三嗪-7-基)-3,4-二羟基-5-(羟甲基)四氢呋喃-2-腈|CsnPharm

CAS No.: 1191237-69-0

(2R,3R,4S,5R)-2-(4-Aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-carbonitrile Catalog No. CSN25250

Synonyms: Remdesivir-metabolite;GS-5734-metabolite

GS-441524, a small molecule nucleoside analog, strongly inhibits feline infectious peritonitis (FIP) virus in tissue culture and experimental cat infection. It acts as an alternative substrate and RNA-chain terminator of viral RNA dependent RNA polymerase.

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技术信息

生物活性

描述GS-441524 is an antiviral nucleoside analog with an EC50 value of 11.1μM for delayed brain tumor cells infected with murine hepatitis virus. The mean EC50 value of GS-441524 for SARS-CoV- and MERS-CoV-infected primary human airway epithelial cells is approximately 0.86μM^[1]. In Calu3 2B4 cells, GS-441524 inhibited SARS-CoV-2 replication with EC50 and EC90 values of 0.62μM and 1.34μM, respectively, as determined by infectious viral titer. The EC50 and EC90 values of GS-441524 for SARS-CoV-2 replication in Calu3 2B4 cells were 1.09μM and 1.37μM. respectively, as measured by qRT-PCR. In Vero E6 cells, the EC50 value of GS-441524 for SARS-CoV-2 replication was 0.47μM as determined by both infectious viral titer and qRT-PCR^[2].
作用机制GS-441524 is a 1’-cyano 4-aza-7,9-dideazaadenosine C-adenosine nucleoside analogue that inhibits multiple virus families in vitro^[1].
参考文献

[1] Agostini ML, Andres EL, Sims AC, Graham RL, Sheahan TP, Lu X, Smith EC, Case JB, Feng JY, Jordan R, Ray AS, Cihlar T, Siegel D, Mackman RL, Clarke MO, Baric RS, Denison MR. Coronavirus Susceptibility to the Antiviral Remdesivir (GS-5734) Is Mediated by the Viral Polymerase and the Proofreading Exoribonuclease. mBio. 2018 Mar 6;9(2):e00221-18. doi: 10.1128/mBio.00221-18
[2] Pruijssers AJ, George AS, Schäfer A, Leist SR, Gralinksi LE, Dinnon KH, Yount BL, Agostini ML, Stevens LJ, Chappell JD, Lu X, Hughes TM, Gully K, Martinez DR, Brown AJ, Graham RL, Perry JK, Du Pont V, Pitts J, Ma B, Babusis D, Murakami E, Feng JY, Bilello JP, Porter DP, Cihlar T, Baric RS, Denison MR, Sheahan TP. Remdesivir potently inhibits SARS-CoV-2 in human lung cells and chimeric SARS-CoV expressing the SARS-CoV-2 RNA polymerase in mice. bioRxiv [Preprint]. 2020 Apr 27:2020.04.27.064279. doi: 10.1101/2020.04.27.064279

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.4333 mL
- 17.1666 mL
- 34.3333 mL
- 5 mM
- 0.6867 mL
- 3.4333 mL
- 6.8667 mL
- 10 mM
- 0.3433 mL
- 1.7167 mL
- 3.4333 mL

技术信息

CAS号

1191237-69-0

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C12H13N5O4

运输

蓝冰

分子量

291.26

别名

Remdesivir-metabolite;GS-5734-metabolite

溶解度

DMSO	58.0 mg/mL (199.1 mM)
Water	Insoluble
Ethanol	Insoluble

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(2R,3R,4S,5R)-2-(4-Aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-carbonitrile Catalog No. CSN25250

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