1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. Calcium Channel Sodium Channel
  3. LY393615

LY393615 (NCC1048) is a novel neuronal Ca2+ (calcium channel) and Na + channel (sodium channel) blocker with IC50s of 1.9 μΜ and 5.2 μΜ for α1A and α1B calcium channel subunits. LY393615 has good brain penetration and neuroprotective effects in models of in cerebral ischemia that can be used for neurological disease research.

For research use only. We do not sell to patients.

LY393615 Chemical Structure

LY393615 Chemical Structure

CAS No. : 325819-97-4

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Description

LY393615 (NCC1048) is a novel neuronal Ca2+ (calcium channel) and Na + channel (sodium channel) blocker with IC50s of 1.9 μΜ and 5.2 μΜ for α1A and α1B calcium channel subunits. LY393615 has good brain penetration and neuroprotective effects in models of in cerebral ischemia that can be used for neurological disease research[1].

IC50 & Target

P/Q-type calcium channel

4 μM (IC50)

In Vitro

LY393615 (0-10 μΜ) inhibits calcium flux in HEK 293 cells with α1A and α1B calcium channel subunits with IC50s of 1.9 μΜ and 5.2 μΜ, and inhibits P-type calcium channels in isolated Purkinje cells with IC50 of 4.0 μΜ[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

LY393615 (10 or 12.5 or 15 mg/kg; i.p., single dose) protects against hypoxiahypoglycaemic insults in brain slices and also provided significant protection against ischaemia-induced hippocampal damage in gerbil global cerebral ischaemiasup[1]. LY393615 (15 mg/kg; i.p., 1 mg/kg; i.v.; single dose) has good brain penetration with T1/2s of 2.04 hours (i.v.) and 2.5 hours (i.p.)[1]. Pharmacokinetic parameters for LY393615 in Gerbils[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Route Dose (mg/kg) T1/2 (h)
i.v. 1 2.04
i.p. 15 2.5
Animal Model: Gerbils global cerebral ischaemia[1]
Dosage: 10, 12.5 or 15 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Protected against hypoxiahypoglycaemic insults in brain slices and also provided significant protection against ischaemia-induced hippocampal damage in gerbil global cerebral ischaemia.
Animal Model: Gerbils (Pharmacokinetic assay)[1]
Dosage: 1.0 or 15 mg/kg
Administration: Intraperitoneal injection (i.p.) ; Intravenous injection (i.v.)
Result: Had good brain penetration with T1/2s of 2.04 hours (i.v.) and 2.5 hours (i.p.)[1].
Molecular Weight

381.89

Formula

C21H26ClF2NO

CAS No.
SMILES

FC1=CC=C(C2(C3=CC=C(F)C=C3)CCC(CNCCCC)O2)C=C1.[H]Cl

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    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.

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LY393615
Cat. No.:
HY-135478
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