1. GPCR/G Protein
    Neuronal Signaling
  2. Sigma Receptor
  3. Sigma-1 receptor antagonist 1

Sigma-1 receptor antagonist 1 

Cat. No.: HY-125821 Purity: 99.76%
Handling Instructions

Sigma‑1 receptor antagonist 1 (compound 137) is a potent and selective sigma-1 receptor (σ1R) antagonist, with a high binding affinity to σ1R receptor (Ki = 1.06 nM). Sigma‑1 receptor antagonist 1 exhibits antineuropathic pain activity and acts as a promising agent for the treatment of neuropathic pain.

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

Sigma-1 receptor antagonist 1 Chemical Structure

Sigma-1 receptor antagonist 1 Chemical Structure

CAS No. : 1639220-19-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 820 In-stock
Estimated Time of Arrival: December 31
1 mg USD 550 In-stock
Estimated Time of Arrival: December 31
5 mg USD 980 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Sigma‑1 receptor antagonist 1 (compound 137) is a potent and selective sigma-1 receptor (σ1R) antagonist, with a high binding affinity to σ1R receptor (Ki = 1.06 nM). Sigma‑1 receptor antagonist 1 exhibits antineuropathic pain activity and acts as a promising agent for the treatment of neuropathic pain[1].

IC50 & Target

Ki: 1.06 nM (σ1R)[1]

In Vitro

Sigma‑1 receptor antagonist 1 exhibits a high binding affinity to σ1R receptor (Ki = 1.06 nM) and good σ-1/2 selectivity (1344-fold)[1].

In Vivo

Sigma‑1 receptor antagonist 1 exerts dose-dependent antinociceptive effects in mice formalin model and rats CCI models of neuropathic pain[1].

Molecular Weight

380.31

Formula

C₁₉H₂₃Cl₂N₃O

CAS No.

1639220-19-1

SMILES

CC1=NC(C2=CC=C(Cl)C=C2)=NC(OCCCN3CCCCC3)=C1Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 6.25 mg/mL (16.43 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6294 mL 13.1472 mL 26.2943 mL
5 mM 0.5259 mL 2.6294 mL 5.2589 mL
10 mM 0.2629 mL 1.3147 mL 2.6294 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

Sigma-1 receptor antagonist 1Sigma ReceptorInhibitorinhibitorinhibit

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Sigma-1 receptor antagonist 1
Cat. No.:
HY-125821
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