1. Neuronal Signaling
  2. Sigma Receptor
  3. E1R

E1R is a positive allosteric modulator of sigma-1 receptors (Sig1R PAM) with cognition-enhancing activity.

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E1R Chemical Structure

E1R Chemical Structure

CAS No. : 1301211-78-8

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Solid + Solvent
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Description

E1R is a positive allosteric modulator of sigma-1 receptors (Sig1R PAM) with cognition-enhancing activity[1].

In Vitro

The only target for E1R (inhibition or enhancement of radioligand binding exceeding 20%) is the sigma receptor. 10 μM E1R does not displace the radioligand, but instead increases the specific binding of a non-selective radioligand ([3H]1,3-di(2-tolyl)guanidine) for the sigma receptor by 38% in Jurkat cells[1].

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

In Vivo

E1R demonstrates efficacy against scopolamine-induced cholinergic dysfunction in mice. Treatment with E1R (0.1-10 mg/kg; administered i.p. 60 min before the training session) significantly improves cognitive function in a dose-related manner in mice[1].

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

Animal Model: Male ICR and Balb/c mice weighed 23-25 g[1]
Dosage: 0.1, 1 and 10 mg/kg
Administration: Administered i.p. 60 min before the training session
Result: Treatment at doses of 1 and 10 mg/kg increased retention latency by 194 and 211%, respectively, compared with the control group.
Molecular Weight

232.28

Formula

C13H16N2O2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(CN1C(C[C@@H]([C@@H]1C)C2=CC=CC=C2)=O)N

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 : 60 mg/mL (258.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.3051 mL 21.5257 mL 43.0515 mL
5 mM 0.8610 mL 4.3051 mL 8.6103 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.3051 mL 21.5257 mL 43.0515 mL 107.6287 mL
5 mM 0.8610 mL 4.3051 mL 8.6103 mL 21.5257 mL
10 mM 0.4305 mL 2.1526 mL 4.3051 mL 10.7629 mL
15 mM 0.2870 mL 1.4350 mL 2.8701 mL 7.1752 mL
20 mM 0.2153 mL 1.0763 mL 2.1526 mL 5.3814 mL
25 mM 0.1722 mL 0.8610 mL 1.7221 mL 4.3051 mL
30 mM 0.1435 mL 0.7175 mL 1.4350 mL 3.5876 mL
40 mM 0.1076 mL 0.5381 mL 1.0763 mL 2.6907 mL
50 mM 0.0861 mL 0.4305 mL 0.8610 mL 2.1526 mL
60 mM 0.0718 mL 0.3588 mL 0.7175 mL 1.7938 mL
80 mM 0.0538 mL 0.2691 mL 0.5381 mL 1.3454 mL
100 mM 0.0431 mL 0.2153 mL 0.4305 mL 1.0763 mL
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E1R Related Classifications

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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E1R
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HY-116463
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