2. Membrane Transporter/Ion Channel
  3. Potassium Channel
  4. 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.

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LY3972406

LY3972406 Chemical Structure

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Description

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[1][2].

IC50 & Target[1]

Kv1.3

 

In Vivo

LY3972406 (300 mg/kg/day; p.o.; daily; 28 days) at 300 mg/kg/day (administered as the HG salt) is well-tolerated in Sprague-Dawley rats over 28 days, with nonadverse salivation and equivalent exposure to the HCl salt form[2].
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.

Animal Model: Sprague-Dawley (male and female, aged 7 to 11 weeks, males 187 to 514 g, females 146 to 308 g)[2]
Dosage: 300 mg/kg/day
Administration: p.o.; daily; 28 days
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).
Molecular Weight

417.15

Formula

C21H33ClN2O9
SMILES

OC(CCCC(O)=O)=O.ClC1=C(C)C=C(O)C([C@H](N)C2CCN(C([C@H](O)CO)=O)CC2)=C1.[1/2].O.[1/2]
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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LY3972406 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LY3972406LY 3972406LY-3972406Potassium ChannelKcsAKv1.3 voltage-gated potassium channelrepeat-dose toxicity studiesratseffector memory T cellsSprague-Dawley ratsBeagle dogsocular irritationautoimmune diseasesnaive central memory T cellsdermal irritationInhibitorinhibitorinhibit

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