Home GPCR & G Protein Sigma Receptor agonist 4-IBP

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4-IBP Sigma Receptor agonist

Cat.No.S6561

4-IBP is a selective σ1 receptor agonist with a high level of affinity for the σ1 receptor (Ki = 1.7 nM) and a moderate affinity for the σ2 receptor (Ki = 25.2 nM).
4-IBP Sigma Receptor agonist Chemical Structure

Chemical Structure

Molecular Weight: 420.29

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Quality Control

Batch: S656101 DMSO]84 mg/mL]false]Ethanol]5 mg/mL]false]Water]Insoluble]false Purity: 99.92%
99.92

Solubility

In vitro
Batch:

DMSO : 84 mg/mL (199.86 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Chemical Information, Storage & Stability

Molecular Weight 420.29 Formula

C19H21IN2O

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 155798-08-6 -- Storage of Stock Solutions

Synonyms N/A Smiles C1CN(CCC1NC(=O)C2=CC=C(C=C2)I)CC3=CC=CC=C3

Mechanism of Action

Targets/IC50/Ki
σ1 receptor
1.7 nM(Ki)
σ2 receptor
25.2 nM(Ki)
In vitro

4-IBP decreases the migration levels of various types of cancer cells, including C32 melanoma, U373-MG glioblastoma, A549 NSCLC, and PC3 prostate cancer cells. This compound modifies the sensitivity of U373-MG cells in vitro to proapoptotic lomustin and proautophagic temozolomide, and markedly decreases the expression of two proteins involved in drug resistance: glucosylceramide synthase and Rho guanine nucleotide dissociation inhibitor.
In vivo

In vivo, 4-IBP increases the antitumor effects of temozolomide and irinotecan in immunodeficient mice that are orthotopically grafted with invasive cancer cells.
References

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