D-Altrononitrile, 2-C-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-2,5-anhydro-, 6-(2-methylpropanoate)

Product Name: D-Altrononitrile, 2-C-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-2,5-anhydro-, 6-(2-methylpropanoate)
CAS No.: 2647441-36-7
Chemical Name: D-Altrononitrile, 2-C-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-2,5-anhydro-, 6-(2-methylpropanoate)
Synonyms: SHEN26;Obeldesivir;SHEN26, 10 mM in DMSO;D-Altrononitrile, 2-C-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-2,5-anhydro-, 6-(2-methylpropanoate);((2R,3S,4R,5R)-5-(4-Aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxytetrahydrofuran-2-yl)methyl isobutyrate;RNA,SHEN26,viral load,ATV 006,ATV006,antiviral,SARS coronavirus,Vero E6 cells,podrugs,Inhibitor,ATV-006,SARS-CoV,inhibit
CBNumber: CB810690992
Molecular Formula: C16H19N5O5
Formula Weight: 361.36
MOL File: 2647441-36-7.mol

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D-Altrononitrile, 2-C-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-2,5-anhydro-, 6-(2-methylpropanoate) Property

Density: 1.59±0.1 g/cm3(Predicted)
storage temp.: 4°C, protect from light
solubility: DMSO : 250 mg/mL (691.85 mM; Need ultrasonic)
form: Solid
pka: 12.00±0.70(Predicted)
color: White to off-white

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Hazard and Precautionary Statements (GHS)

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D-Altrononitrile, 2-C-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-2,5-anhydro-, 6-(2-methylpropanoate) Chemical Properties,Usage,Production

Uses

Obeldesivir (ATV006) is a potent, orally active antiviral agent and ester proagents of GS-441524. Obeldesivir inhibits the replication of SARS-CoV-2 and its variants. Obeldesivir can be used for SARS-CoV-2 research[1].

in vivo

Obeldesivir (5-25 mg/kg; p.o. and i.v.; Sprague Dawley rats) has favorable pharmacokinetic profiles in rats with high oral bioavailability (F %) of 81.5% and maximum blood concentration (C_max) of 8.2 μM^[1].
Obeldesivir (250-500 mg/kg; p.o.; daily, for 4 days; hACE2 knock-in and Ad5-hACE2 mice) has antiviral activity and inhibits SARS-CoV-2 replication in mouse models^[1].
Obeldesivir (100-250 mg/kg; p.o.; daily, for 10 days) reduces lung damage and protects K18-hACE2 mice^[1].
Obeldesivir (10-150 mg/kg; p.o.; daily, for 3 days) reduces virus titers and lung damage caused by Delta variant infection in K18-hACE2 mice^[1].

Animal Model:

Sprague Dawley rats^[1]

Dosage:

5 and 25 mg/kg

Administration:

Oral administration (25 mg/kg) and intravenous injection (5 mg/kg)

Result:

1.19

parameters	i.v. (5 mg/kg)	p.o. (25 mg/kg)
AUC_last (μM·h)	5.6	22.8
T_1/2 (h)	1.5	1.2
T_max (h)		0.5
C_max (μM)	8.7	8.2
F %		81.5

Animal Model:	hACE2 knock-in and Ad5-hACE2 mice^[1]
Dosage:	250 and 500 mg/kg
Administration:	Oral administration; daily, for 4 days
Result:	Inhibited gRNA and sgRNA, which is Biomarkers of coronavirus replication. Reduced the viral load and pathological damage of the lung.

Animal Model:	K18-hACE2 mice^[1]
Dosage:	100 and 250 mg/kg
Administration:	Oral administration; daily, for 10 days
Result:	Reduced viral RNA and increased the survival rate of mice. Reduced evidence of lung pathology and the production of inflammatory cytokines and chemokines in the lung tissues.

Animal Model:	K18-hACE2 mice^[1]
Dosage:	10, 30, 80 and 150 mg/kg
Administration:	Oral administration; daily, for 3 days
Result:	Reduced viral load in a dose-dependent manner and alleviated the symptoms in the lung.

References

[1] Cao L, et, al. The adenosine analog prodrug ATV006 is orally bioavailable and has preclinical efficacy against parental SARS-CoV-2 and variants. Sci Transl Med. 2022 May 17:eabm7621. DOI:10.1126/scitranslmed.abm7621

D-Altrononitrile, 2-C-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-2,5-anhydro-, 6-(2-methylpropanoate) Preparation Products And Raw materials

Raw materials

Preparation Products

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D-Altrononitrile, 2-C-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-2,5-anhydro-, 6-(2-methylpropanoate) Suppliers

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2647441-36-7, D-Altrononitrile, 2-C-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-2,5-anhydro-, 6-(2-methylpropanoate)Related Search:

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D-Altrononitrile, 2-C-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-2,5-anhydro-, 6-(2-methylpropanoate)

SHEN26

Obeldesivir

RNA,SHEN26,viral load,ATV 006,ATV006,antiviral,SARS coronavirus,Vero E6 cells,podrugs,Inhibitor,ATV-006,SARS-CoV,inhibit

((2R,3S,4R,5R)-5-(4-Aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxytetrahydrofuran-2-yl)methyl isobutyrate

SHEN26, 10 mM in DMSO

2647441-36-7