GS 441524,(2R,3R,4S,5R)-2-(4-aminopyrrolo[1,2-f][1,2,4]triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-carbonitrile CAS 1191237-69-0

GS 441524,(2R,3R,4S,5R)-2-(4-aminopyrrolo[1,2-f][1,2,4]triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-carbonitrile CAS 1191237-69-0

CAS NO: 1191237-69-0
Molecular Formula: C12H13N5O4
Molecular Weight: 291.26
EINECS NO: N/A
MDL NO: MFCD291237690
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Product Details

Product Description

Product Name: GS 441524,(2R,3R,4S,5R)-2-(4-aminopyrrolo[1,2-f][1,2,4]triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-carbonitrile CAS 1191237-69-0

 

 

Synonyms:

Remdesivir intermediate;

GS-441524;

 

 

Chemical & Physical Properties

Appearance : off-white powder.

Assay : ≥99%

Density:1.84±0.1 g

Water Solubility:Soluble in DMSO

 

 

 

Description: GS-441524 could strongly inhibits feline infectious peritonitis virus (FIPV), with an EC50 of 0.78 μM.

 

Target

EC50: 0.78 μM (FIPV)[1].

 

In Vitro

The cells appear and grow normally at all concentrations of GS-441524 and fail to uptake the fluorescent dye CellTox Green at 24 h. The cytotoxic concentration-50% (CC50) is therefore>100 μM. The effective concentration-50% (EC50) of GS-441524 is calculated to be 0.78 μM[1].

 

In Vivo

         All 10 treated cats have a rapid response to treatment and lymphocyte levels and rectal temperatures return to pre-infection levels and levels of the two asymptomatic cats. Two of the 10 treated cats, 16-116 (Group A) and 16-127 (Group B), have recurrences disease at four and six weeks post treatment. These two cats are treated a second time for two weeks and their response is identical to that of primary treatment. All ten of the once or twice treated cats have remained normal to date (more than eight months post infection). Injections cause a transient "stinging" reaction in some cats within 10 s of compound administration. Localized and transient pain is evidenced by unusual posturing, licking at the injection site and/or vocalizations that last for approximately 30-60 s after injection. Injection reactions are more pronounced in some animals relative to others and reactions are inconsistent from one injection to the next and decreas over time[1].

 

Cell Assay   

To determine the toxicity of GS-441524 to CRFK cells n, CRFK cells are treated with 100, 33.3, 11.1, 3.7 or 1.2 μM GS-441524 for 24 h[1].

 

Animal Admin

Cats[1] The 10 cats that developed disease signs are divided into two groups and treated with either 5 mg/kg (Group A; n=5) or 2 mg/kg (Group B; n=5) GS-441524 SC q24 h starting three days after unequivocal clinical evidence of FIP (days 12-19 post infection). The two cats that do not develop disease signs serve as controls for normal blood lymphocyte counts and rectal temperature[1].

 

References

[1]. Murphy BG, et al. The nucleoside analog GS-441524 strongly inhibits feline infectious peritonitis (FIP) virus in tissue culture and experimental cat infection studies. Vet Microbiol. 2018 Jun;219:226-233.

 

What is GS-441524?

Gs-441524 is the second targeted antiviral drug after gc376 in the treatment of feline infectious peritonitis (FIP). Gs-441524 is a small nucleotide analogue provided by Gilead Sciences (Global antiviral field No.1) to perdersencjiaoshou2 and its research topic of abdominal transmission. Gs-441524 is a reverse transcriptase inhibitor that can inhibit the replication of feline abdominal transmission virus (FIP), and a prerequisite molecule for the synthesis of nucleoside triphosphate with pharmacological activity. Gs-441524 is a small molecule, also known as nucleoside triphosphate competitive inhibitor, which has strong antiviral activity against many RNA viruses. It can inhibit the replication of several different types of chemical Book RNA virus, such as severe acute respiratory syndrome (SARS) coronavirus, Middle East respiratory syndrome virus, Ebola virus, Lassa fever virus, Junin virus and respiratory syncytial virus, and has low cytotoxicity in a wide range of cell lines.

 

The mechanism of action is that GS-441524 is phosphorylated into nucleoside monophosphate (NMP) through cell kinase, and then transformed into active three phosphate metabolite (NTP structure analogue). In viral RNA synthesis, the active NTP structural analogue acts as the competition of natural nucleoside triphosphate and the competition of natural nucleoside (ATP, TTP, CTP, GTP) to participate in RNA transcription. When gs-441524 is inserted into the transcription product, the transcription will be terminated in advance, thus inhibiting the viral RNA transcription process.

 

 

 

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