1. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  2. REV-ERB
  3. BE2012

BE2012, SR8278 (HY-14415) derivative, is a potent and selective REV-ERBα/β Antagonist with EC50 values of 0.285 and 0.346 μM. BE2012 binds to the ligand-binding domain (LBD) of REV-ERB, preventing the receptor from recruiting co-inhibitory factors and thereby releasing the transcriptional repression on downstream target genes. BE2012 can upregulate the expression of myogenic transcription factors Myf5 and Myod, promoting muscle regeneration and repair in acute muscle injury micemodels.

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BE2012

BE2012 Chemical Structure

CAS No. : 667889-47-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
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10 mg In-stock
25 mg In-stock
50 mg In-stock
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Based on 1 publication(s) in Google Scholar

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Description

BE2012, SR8278 (HY-14415) derivative, is a potent and selective REV-ERBα/β Antagonist with EC50 values of 0.285 and 0.346 μM. BE2012 binds to the ligand-binding domain (LBD) of REV-ERB, preventing the receptor from recruiting co-inhibitory factors and thereby releasing the transcriptional repression on downstream target genes. BE2012 can upregulate the expression of myogenic transcription factors Myf5 and Myod, promoting muscle regeneration and repair in acute muscle injury micemodels[1].

IC50 & Target[1]

REV-ERBα

0.285 μM (EC50)

REV-ERBβ

0.346 μM (EC50)

Parmacokinetics
Species Dose Route Cmax Tmax T1/2 AUC0-last CL Vd
Mice[1] 30 mg/kg i.p. 1560 ng/mL 0.5 h 3.79 h 4023 h·ng/g 7.4 L/h/kg 40.5 L/kg
Molecular Weight

293.36

Formula

C18H19N3O

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

CC(C)(C)C(C=C1)=CC=C1C(N2N)=NC3=CC=CC=C3C2=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (68.18 mM; Need ultrasonic and warming; 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 3.4088 mL 17.0439 mL 34.0878 mL
5 mM 0.6818 mL 3.4088 mL 6.8176 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 (stored under nitrogen). 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
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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 (stored under nitrogen). 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 3.4088 mL 17.0439 mL 34.0878 mL 85.2195 mL
5 mM 0.6818 mL 3.4088 mL 6.8176 mL 17.0439 mL
10 mM 0.3409 mL 1.7044 mL 3.4088 mL 8.5220 mL
15 mM 0.2273 mL 1.1363 mL 2.2725 mL 5.6813 mL
20 mM 0.1704 mL 0.8522 mL 1.7044 mL 4.2610 mL
25 mM 0.1364 mL 0.6818 mL 1.3635 mL 3.4088 mL
30 mM 0.1136 mL 0.5681 mL 1.1363 mL 2.8407 mL
40 mM 0.0852 mL 0.4261 mL 0.8522 mL 2.1305 mL
50 mM 0.0682 mL 0.3409 mL 0.6818 mL 1.7044 mL
60 mM 0.0568 mL 0.2841 mL 0.5681 mL 1.4203 mL
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  • 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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BE2012
Cat. No.:
HY-180944
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