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Peramivir Trihydrate Neuraminidase inhibitor

Name: Peramivir Trihydrate
Brand: Selleck Chemicals
SKU: S2716
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S2716

Peramivir Trihydrate (BCX-1812, RWJ-270201, S-021812) is a trihydrate of the anti-infection agent peramivir which is a transition-state analogue and a potent, specific influenza viral neuraminidase inhibitor with an IC50 of median 0.09 nM.

Chemical Structure

Molecular Weight: 382.45

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Quality Control

Batch: S271601 5%TFA]3 mg/mL]false]DMSO]0.2 mg/mL]false]Water]Insoluble]false Purity: 100%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

100

Related Targets	Integrase Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite Reverse Transcriptase HIV
Other Neuraminidase Inhibitors	Laninamivir Octanoate Laninamivir

Solubility

In vitro
Batch:

5%TFA : 3 mg/mL

DMSO : 0.2 mg/mL (0.52 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Clear solution	5%TFA 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.15mg/ml (0.39mM)	Taking the 1 mL working solution as an example, add 50 μL of 3 mg/ml clarified TFA stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	382.45	Formula	C₁₅H₂₈N₄O₄.3H₂O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1041434-82-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	BCX-1812, RWJ-270201, S-021812			Smiles	CCC(CC)C(C1C(CC(C1O)C(=O)O)N=C(N)N)NC(=O)C.O.O.O

Mechanism of Action

In vivo

Peramivir protects mice against severe disease outcomes following infection with highly pathogenic avian influenza and multi-dose treatment was efficacious in ferrets. Peramivir combined with Oseltamivir perform better than suboptimal doses of each compound alone to treat influenza infections in mice. Peramivir (30 mg/kg) is effective in promoting the survival of mice infected with systemically replicating H5N1 virus. Peramivir is 30% protective against H1N1 virus in mice at 0.5 mg/kg/d, but ineffective at lower doses when used as monotherapy. Peramivir combined with favipiravir increases the numbers of survivors by 10-50% when the 0.025 mg/kg/d, 0.05 mg/kg/d, and 0.1 mg/kg/d doses of Peramivir are combined with 20 mg/kg/d Favipiravir and when all doses of Peramivir are combined with 40 mg/kg/d Favipiravir. Peramivir combined with favipiravir results in an increase in lifespan, improved body weight and significant reductions in lung hemorrhage score and lung weight in H1N1 infected mice. Peramivir (1 mg/kg/d) combined with Rimantadine (5 mg/kg/d and 10 mg/kg/d) produces weight losses of 1.69 and 0.69, respectively, whereas the combination of 3.0 mg/kg/d Peramivir with 10 and 30 mg/kg/d Rimantadine does not show any weight loss in sub-lethal influenza A (H3N2) virus mouse model.

References

[1] https://pubmed.ncbi.nlm.nih.gov/18234269/
[2] https://pubmed.ncbi.nlm.nih.gov/20633577/
[3] https://pubmed.ncbi.nlm.nih.gov/18573280/

[4] https://pubmed.ncbi.nlm.nih.gov/22429564/
[5] https://pubmed.ncbi.nlm.nih.gov/20943201/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02635724	Completed	Influenza	BioCryst Pharmaceuticals	December 2015	Phase 3
NCT02369159	Completed	Influenza	BioCryst Pharmaceuticals	March 11 2015	Phase 3
NCT01224795	Terminated	Influenza	BioCryst Pharmaceuticals\|Department of Health and Human Services	October 2010	Phase 3
NCT01146353	Withdrawn	Influenza\|Renal Failure	Midwestern University\|Northwestern University\|BioCryst Pharmaceuticals	February 2010	--
NCT01063933	Withdrawn	Influenza	National Institute of Allergy and Infectious Diseases (NIAID)		Phase 1\|Phase 2

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