Kamuvudine-9
Kamuvudine-9 is a central nervous system-penetrant NLRP3/NLRC4 inhibitor and nucleoside reverse transcriptase inhibitor derivative. Kamuvudine-9 inhibits inflammasome assembly, Caspase-1 cleavage, and the release of IL-1β/18 and Interferon-γ. Kamuvudine-9 is non-mutagenic and non-clastogenic, and does not inhibit KV11.1/hERG currents. Kamuvudine-9 reduces Amyloid β and phosphorylated Tau. Kamuvudine-9 improves memory and learning in Alzheimer's disease models. Kamuvudine-9 can be used in research on multiple sclerosis, rhegmatogenous retinal detachment, viral infections, and sclerotic chronic graft-versus-host disease.
For research use only. We do not sell to patients.
- Formula: C11H17N3O3S
- Molecular Weight:271.34
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
Caspase-1 |
IL-1β |
IL-18 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Bioavailability |
|---|---|---|---|
| Pig[1] | 50 mg/kg | p.o. | 57 % |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:wild-type[1]
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Dosage:60 mg/kg
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Administration:i.p.; from day of MOG35-55 immunization; 28 days
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Result:Induced near-complete protection against neurologic deficits throughout the 28-day study.
Disease burden (area under the curve) was reduced by 92%.
Prevented spinal cord demyelination by Luxol Fast Blue and myelin basic protein staining, reduced Iba1+ cell abundance, and reduced cleaved caspase-1 in spinal cord.
Serum IL-1β and IFN-γ concentrations were reduced.
Preserved retinal ganglion cells in the prevention model.
Axonal degeneration was reduced by 82% in the optic nerve and by 89% in the spinal cord.
Serum NfL was reduced by 98%.
After cessation, neurologic score increased by 1.43 points (n = 7) over one week.
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Animal Model:C57BL/6J (male and female, 6-10 weeks old)[3]
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Dosage:90 mg/kg (low dose); 60 mg/kg (high dose)
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Administration:intraperitoneal; once daily or twice daily
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Result:At 3 days after RRD induction, mice exhibited a dose-dependent and complete reduction in retinal cleaved caspase-1 compared with PBS-treated mice.
Produced a dose-dependent reduction in TUNEL-positive cells in the outer nuclear layer.
High dose conferred 56% photoreceptor protection.
Inhibited retinal IL-18 levels compared with PBS, while IL-18 was not detected in attached retina.
Inhibited caspase-8 cleavage in detached retina at 1 day compared with PBS.
Chemical Information
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Molecular Weight 271.34
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Formula C11H17N3O3S
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SMILES
COCC1OC(CS1)N2C=CC(N(C)C)=NC2=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Kamuvudine-9 Related Classifications
HY-190457 Related Classifications
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Keywords
- Kamuvudine-9
- Kamuvudine9
- Kamuvudine 9
- NOD-like Receptor (NLR)
- Caspase
- Interleukin Related
- IFNAR
- Amyloid-β
- Tau Protein
- Drug Derivative
- Nucleoside Antimetabolite/Analog
- IL
- Interferon-α/β receptor
- Interferon-alpha/beta receptor
- β-amyloid peptide
- Aβ
- Abeta
- Drug derivative
- Alzheimer's disease
- NEK7
- NLRC4 inflammasome
- NLRP3 inflammasome
- graft-versus-host disease
- interferon-γ
- interleukin-1β
- multiple sclerosis
- neuroinflammation
- rhegmatogenous retinal detachment
- Inhibitor
- inhibitor
- inhibit