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GS-441524

Description Mechanism of action Pharmacokinetics
GS-441524
GS-441524 structure
CAS No.
1191237-69-0
Chemical Name:
GS-441524
Synonyms
NUC;GS-4;GS-441;EVO984;GS441525;S-441524;GS-441524;Remdesivir-011;GS 441524(acid);remdesivir power
CBNumber:
CB04808604
Molecular Formula:
C12H13N5O4
Formula Weight:
291.26
MOL File:
Mol file

GS-441524 Properties

Density 
1.84±0.1 g/cm3(Predicted)
pka
12.13±0.70(Predicted)
CAS DataBase Reference
1191237-69-0

GS-441524 price More Price(4)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 30469 GS-441524 1191237-69-0 1mg $29 2021-03-22 Buy
Cayman Chemical 30469 GS-441524 1191237-69-0 25mg $471 2021-03-22 Buy
Cayman Chemical 30469 GS-441524 1191237-69-0 5mg $123 2021-03-22 Buy
Cayman Chemical 30469 GS-441524 1191237-69-0 10mg $232 2021-03-22 Buy

GS-441524 Chemical Properties,Uses,Production

Description

GS-441524 is a nucleoside analogue that terminates the RNA chain of viral RNA-dependent RNA polymerase.
GS-441524 was developed by Gilead Sciences, Inc as part of their research into human RNA virus disease such as Ebola.
GS-441524 is a small molecule that exhibits potent antiviral activity against a number of RNA viruses, including the zoonotic severe acute respiratory syndrome (SARS) coronavirus ( Cho et al., 2012). A phosphoramidate prodrug of GS-441524 (GS-5734) has been previously shown to inhibit the replication of several taxonomically diverse RNA viruses such as Middle East respiratory syndrome virus, Ebola virus, Lassa fever virus, Junin virus and respiratory syncytial virus, while having low cytotoxicity in a wide-range of cell lines ( Sheahan et al., 2017 ). GS-5734 has also been shown to protect rhesus monkeys from experimental Ebola virus infection ( Warren et al., 2016 ).

Mechanism of action

GS-441524 requires intracellular phosphorylation via cellular kinases to a nucleoside monophosphate and subsequently to the active triphosphate metabolite (NTP) ( Cho et al., 2012 ; Sheahan et al., 2017; Warren et al., 2016). The active NTP analog functions as a competitor of the natural nucleoside triphosphates in viral RNA synthesis. The active form of GS-441524 has been shown to inhibit RSV RNA-dependent RNA polymerase mediated transcription by incorporating into the nascent viral transcript and causing premature termination ( Sheahan et al., 2017 ). We hypothesized that GS-441524 would be activated in feline cells, attenuate FIPV replication, have low cytotoxicity in feline cells in vitro and effectively treat cats with experimentally induced FIP.

Pharmacokinetics

A pharmacokinetic (PK) study was performed in laboratory cats to determine the metabolism and acute animal toxicity of GS-441524. GS-441524 was dissolved at a concentration of 12.5 mg/ml in 5% ethanol, 30% propylene glycol, 45% PEG 400, 20% water, and adjusted to pH 1.9 with concentrated HCl. Six laboratory cats were randomly divided into group A (n = 3; IV administration) or B (n = 3; SC administration). At time point zero, Group A cats were administered 5 mg compound/kg body weight intravenously while Group B cats received 5 mg com- pound/kg subcutaneously. Cats were then monitored for signs of acute toxicity (elevated pulse, respiratory distress, cyanosis, diarrhea, anorexia, drooling, vomiting, ataxia, weight loss, and changes in rectal temperature) daily for five days. Serial 0.5 ml whole blood samples in EDTA were obtained by lateral saphenous, superficial brachial or jugular venipuncture from each cat at 0.25, 0.5, 1, 2, 4, 6, 8, 12 and 24 h. After collection, blood samples were immediately placed onice and then centrifuged at 5000 rpm for 5 min. The isolated plasma was pipetted into a 1.5 ml microcentrifuge tube and frozen at − 70 °C for further analysis of free GS-441524. The buffy coat fraction from each blood collection was suspended in 1.5 ml phosphate free Tris-buffered saline (TBS, 50 mM Tris-Cl, pH 7.5, 150 mM NaCl) and PBMC isolated by Ficoll Hypaque density gradient centrifugation. The plasma and PBMC fractions were snap frozen in liquid nitrogen and shipped on dry ice to Gilead Sciences, Inc. (Foster City, CA) for further analyses. (plasma drug concentration and intracellular phosphorylation analyses).

GS-441524 Preparation Products And Raw materials

Raw materials

Preparation Products


GS-441524 Suppliers

Global( 178)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Jiangsu Aikon Biooharmaceutical R&D CO.Ltd
--
-- darren.wang@angenetech.com China 5 12
Hebei Ruiyao Biotechnology Co. Ltd
15532235888 15632182983
031188180881 admin@ruiyaobio.com CHINA 846 58
Hebei Yirun Sega Biological Technology Co. Ltd
19932103556 +8619932103556
+8619932103556 linda@yrsjbiotech.com CHINA 727 58
Shandong Natural Micron Pharm Tech Co.,LTD
13752232623
info@nmpharmtech.com CHINA 2737 58
NANJING SUNSHINE BIOTECH CO.,LTD
+86-25-86189929
+86-25-86189616 brian@sunshine-bio.com CHINA 128 58
HEBEI YINGONG NEW MATERIAL TECHNOLOGY CO.,LTD
+86 19930599843
cindy@hbyingong.com CHINA 408 58
Baoji Guokang Healthchem co.,ltd
09178656283
cngksw@aliyun.com CHINA 9483 58
Hebei Lingding Biological Technology Co., Ltd
19933155420
sales1@hbldbiotech.com CHINA 973 58
Suzhou Ryan Pharmachem Technology Co.,Ltd.
0512-68780025-8002
0512-68780025-8004 yybi@ryanchem.com;sales@ryanchem.com CHINA 188 58
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 26734 60

View Lastest Price from GS-441524 manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2021-10-18 GS-441524
1191237-69-0
US $10.00 / Kg/Bag 1KG 99% 10Tons Hebei Senko Biotechnology Co., Ltd.
2021-10-18 (2R,3R,4S,5R)-2-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-carbonitrile
1191237-69-0
US $0.00 / Kg/Drum 10g 99% 20mt/year Jinan Finer Chemical Co., Ltd
2021-10-11 2-?C-?(4-?Aminopyrrolo[2,?1-?f]?[1,?2,?4]?triazin-?7-?yl)?-?2,?5-?anhydro-D-?altrononitrile
1191237-69-0
US $3.90 / KG 1KG 99% 10kg Hong Kong Tiansheng New Material Trading Co., Ltd

1191237-69-0(GS-441524)Related Search:


  • (2R,3R,4S,5R)-2-(4-AMINOPYRROLO[2,1-F][1,2,4]TRIAZIN-7-YL)-3,4-DIHYDROXY-5-(HYDROXYMETHYL)OXOLANE-2-
  • (2R,3R,4S,5R)-2-(4-Aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)oxolane-2-carbonitrile
  • 2-C-(4-AMINOPYRROLO[2,1-F][1,2,4]TRIAZIN-7-YL)-2,5-ANHYDRO-3,4-O-(1-METHYLETHYLIDENE)-D-ALTRONONITRI
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  • 2-C-(4-Aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-2,5-anhydro-D-Altrononitrile
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  • GS-4
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  • (2R,3R,4S,5R)-2-(4-aminopyrrolo[1,2-f][1,2,4]triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-carbonitrile
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  • Remdesivir Triol Nitrile Impurity
  • Remdesivir intermediates
  • Radcivir intermediate n-3)
  • GS441524 Remdesivir metabolite
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  • Remdesivir-011
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  • Remdesivir Related Compound 6
  • (2R,3R,4S,5R)-2-(4-aminopyrrolo[1,2,4]triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-carbonitrile
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  • FIPV Nutrient Solution for R&D use only Liquid GS441524
  • (2 r, 3 r, 4 s, 5 r) - 2 - (4 - amino pyrrole and 4-trichlorobenzene [1] [2, 1 - F] triazine - 7 - base) - 2 hydroxy - 5-3, 4 - (hydroxymethyl) tetrahydrofuran - 2 - methyl acrylic
  • remdesivir power
  • GS-441524 USP/EP/BP
  • Remdesivir metabolite(GS-441524)
  • Remdesivir Intermediate(GS-441524)
  • Supply High Quality GS-441524
  • 1191237-69-0
  • 1354832-36-1
  • GS
  • API
  • null
  • Intermediates
  • API
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