LY3972406
LY3972406 is an orally active, selective Kv1.3 antagonist. LY3972406 acts on chronically stimulated effector memory T cells without affecting naive central memory T cells. LY3972406 induces mild, non-adverse skin irritation in Rattus norvegicus. LY3972406 is applicable for the research of autoimmune diseases.
For research use only. We do not sell to patients.
- CAS No.: 3071928-57-6
- Formula: C16H23ClN2O4·1/2C5H8O4·1/2H2O
- Molecular Weight:492.95
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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
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
Kv1.3 |
In Vivo
LY3972406 (100 mg/kg; p.o.; single dose) achieves equivalent exposure to the HCl salt in female Sprague-Dawley rats, with slightly faster absorption[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male and female, aged 7 to 11 weeks, males 187 to 514 g, females 146 to 308 g)[2]
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Dosage:300 mg/kg/day
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Administration:p.o.; daily; 28 days
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Result:Observed 100% survival.
Caused minor, nonadverse salivation (slight intensity, Days 8 through 22) at similar incidence and severity as the LY3972406-HCl group.
Resulted in exposure comparable to the HCl salt (within 20% by AUC and Cmax) with no accumulation (R_AUC <1.2).
Chemical Information
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CAS No. 3071928-57-6
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Molecular Weight 492.95
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Formula C16H23ClN2O4·1/2C5H8O4·1/2H2O
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SMILES
ClC1=C(C)C=C(O)C([C@H](N)C2CCN(C([C@H](O)CO)=O)CC2)=C1.O=C(CCCC(O)=O)O.O.[1/2].[1/2]
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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.
Protocols
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Dermal Irritation/Dermal Toxicity Study
This protocol assesses dermal irritation using reconstructed human epidermis (RhE) models such as EpiDerm, EPISKIN, and SkinEthic RHE, in which a test substance is applied topically and tissue viability is measured after exposure; reduced viability reflects cytotoxic injury associated with skin irritation potential. The primary readout is MTT reduction, where viable cells convert tetrazolium salt into colored formazan measured by spectrophotometry; this signal is used as a quantitative viability endpoint for classifying irritant versus non-irritant responses. The historical in vivo comparator is the Draize rabbit skin irritation method, which scores erythema and edema after topical exposure, but validated RhE assays were developed to replace or reduce reliance on this animal-based endpoint.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LY3972406 Related Classifications
HY-184003 Related Classifications
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