1. Neuronal Signaling
  2. Sigma Receptor
  3. σ1 Receptor antagonist 4

σ1 Receptor antagonist 4 (compound TC1) is a selective sigma1 (σ1) receptor antagonist with a Ki of 10 nM. σ1 Receptor antagonist 4 is weakly active at σ2 receptor (Ki of 370 nM) and has no activity at dopamine (DAT), serotonin (SERT), and norepinephrine (NET) transporters.

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σ1 Receptor antagonist 4 Chemical Structure

σ1 Receptor antagonist 4 Chemical Structure

CAS No. : 362512-81-0

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Description

σ1 Receptor antagonist 4 (compound TC1) is a selective sigma1 (σ1) receptor antagonist with a Ki of 10 nM. σ1 Receptor antagonist 4 is weakly active at σ2 receptor (Ki of 370 nM) and has no activity at dopamine (DAT), serotonin (SERT), and norepinephrine (NET) transporters[1].

IC50 & Target[1]

σ1R

10 nM (Ki)

σ2

370 nM (Ki)

In Vivo

σ1 Receptor antagonist 4 (compound TC1; 3-100 mg/kg; ip; once) attenuats the stimulatory locomotor effect of 20 mg/kg Cocaine with a half-maximal depressant activity (ID50) of 38.6 mg/kg[1].

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

Animal Model: Male Swiss-Webster mice (Hsd:ND4, aged 2-3 month) injected with Cocaine[1]
Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg
Administration: i.p.; once
Result: Attenuated the stimulatory locomotor effect of 20 mg/kg Cocaine.
Molecular Weight

297.37

Formula

C19H20FNO

CAS No.
SMILES

OC12[C@H]3[C@@H]4C(C5C2C6[C@@H]3[C@H]4C5C6)N1CCC7=CC(F)=CC=C7

Shipping

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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σ1 Receptor antagonist 4 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.

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Product Name:
σ1 Receptor antagonist 4
Cat. No.:
HY-108513
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