SR9009

Name: SR9009
Brand: MedChemExpress
SKU: HY-16989
Rating: 5.0 (32 reviews)

Cat. No.: HY-16989 Purity: 99.61%: FAQs
Data Sheet SDS COA Handling Instructions

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SR9009 is a REV-ERBα/β agonist with IC₅₀s of 670 nM and 800 nM for REV-ERBα and REV-ERBβ, respectively.

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

SR9009 Chemical Structure

CAS No. : 1379686-30-2

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 77	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 77	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 33	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 320	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 560	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 32 publication(s) in Google Scholar

28 Publications Citing Use of MCE SR9009

Cell Viability Assay

: SR9009 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Nov 10;13(11):949. [Abstract]; SR9009 (0-50 μM; 48 h) markedly inhibits 22RV1, PC3 and DU145 cell viability in a dose-dependent manner but had no impact on RWPE-1 cells.

: SR9009 purchased from MedChemExpress. Usage Cited in: Chemosphere. 2021 Jan;263:128020. [Abstract]; SR9009 administration remarkably increases the protein expression levels of NR1D1 at both 24 and 48 h, while attenuating the protein expression levels of BMAL1. The protein expression levels of StAR are also elevated at 24 h.

: SR9009 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2018 Oct 12;9(1):4246. [Abstract]; Western blotting of peritoneal macrophages (PMs) after co-treatment of SR9009 (for 12 h) and LPS/ATP. LPS is added before or after SR9009 treatment for 3 h, followed by ATP addition for 30 min (added last).

: SR9009 purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2018;46(1):303-313. [Abstract]; Rev-erbα expression in relation to MMP-9 protein expression is induced by Ang II in THP-1 macrophages. MMP- 9 protein expression is analyzed by western blotting.

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Biological Activity
Protocol
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Description

SR9009 is a REV-ERBα/β agonist with IC₅₀s of 670 nM and 800 nM for REV-ERBα and REV-ERBβ, respectively.

IC₅₀ & Target

IC50: 670 nM (Rev-ErbBα), 800 nM (Rev-ErbBβ)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	0.7 μM Compound: 12e	Agonist activity at Rev-Erbalpha expressed in HEK293 cells coexpressing BamII promoter assessed as repression of transcription after 24 hrs by dual-Glo luciferase assay Agonist activity at Rev-Erbalpha expressed in HEK293 cells coexpressing BamII promoter assessed as repression of transcription after 24 hrs by dual-Glo luciferase assay	[PMID: 22633688]
HEK293	IC₅₀	670 nM Compound: 12e	Agonist activity at Rev-Erbalpha expressed in HEK293 cells coexpressing Gal4 ligand binding domain assessed as inhibition of transcription after 24 hrs by dual-Glo luciferase assay Agonist activity at Rev-Erbalpha expressed in HEK293 cells coexpressing Gal4 ligand binding domain assessed as inhibition of transcription after 24 hrs by dual-Glo luciferase assay	[PMID: 22633688]

In Vitro

SR9009 dose-dependently increases the REV-ERB-dependent repressor activity assessed in HEK293 cells expressing a chimeric Gal4 DNA Binding Domain (DBD)-REV-ERB ligand binding domain (LBD)α or β and a Gal4-responsive luciferase reporter (SR9009: REV-ERBα IC₅₀=670 nM, REV-ERBβ IC₅₀=800 nM). SR9009 potently and efficaciously suppresses transcription in a cotransfection assay using full-length REV-ERBα along with a luciferase reporter driven by the Bmal1 promoter (IC₅₀=710 nM). SR9009 suppresses the expression of BMAL1 mRNA in HepG2 cells in a REV-ERBα/β-dependent manner. Direct binding of the SR9009 to REV-ERBα is also confirmed using circular dichrosim analysis (K_d=800 nM)^[1].

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

In Vivo

SR9009 (100 mg/kg ,i.p.) treated mice exhibit a more severe reduction in adiposity. Plasma non-esterified fatty acids (NEFA) are also reduced (23%) along with plasma glucose (19%) in the SR9009 treated animals. In the white adipose tissue (WAT) , SR9009 treatment results in a decrease in expression of genes encoding enzymes involved in triglyceride (TG) synthesis as is also observed in lean mice^[1].

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

Molecular Weight

437.94

Formula

C₂₀H₂₄ClN₃O₄S

CAS No.

1379686-30-2

Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CC(CN(CC2=CC=C(Cl)C=C2)CC3=CC=C([N+]([O-])=O)S3)CC1)OCC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (228.34 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2834 mL	11.4171 mL	22.8342 mL
5 mM	0.4567 mL	2.2834 mL	4.5668 mL
10 mM	0.2283 mL	1.1417 mL	2.2834 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 10% Cremophor EL 85% ddH2O
Solubility: 20 mg/mL (45.67 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: 2.5 mg/mL (5.71 mM); Suspended solution; Need ultrasonic
Protocol 3

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.71 mM); Suspended solution; Need ultrasonic
Protocol 4

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (4.75 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 5

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (4.75 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 6

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.75 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.61%

Select Batch:

Data Sheet (282 KB) SDS (393 KB)

COA (253 KB) LCMS (113 KB)

Handling Instructions (2659 KB)

References

[1]. Solt LA, et al. Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. Nature. 2012 Mar 29;485(7396):62-68. [Content Brief]

Cell Assay ^[1]	HEK293 cells are grown in 96-well plates (1×10⁶/well) and are transiently transfected using Lipofectamine. Cells are transfected with a total of 200 ng of DNA per well consisting of the pGL4 mIL-17 firefly luciferase reporter construct, the pGL4 mIL-17 + CNS-5 firefly luciferase reporter construct, or the pGL4 mIL-17 2kB RORE mutant (100 ng/well) , an actin promoter Renilla reniformis luciferase reporter (50 ng/well), and either control vector alone or the test DNA (full-length RORα or full-length RORγ at 50 ng/well). All 48 human nuclear receptors are represented in the specificity assay and SR9009 is tested at a concentration of 20 μM. The format of the assay is a cotransfection assay with Gal4 DNA binding domain-nuclear receptor fusions in HEK293 cells^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] For circadian gene expression experiments male C57BL6 mice (8-10 weeks of age) are either maintained on a L:D (12h:12h) cycle or on constant darkness. At circadian time (CT) 0 animals are administered a single dose of 100 mg/kg SR9009 or SR9011 (i.p.) and groups of animals (n=6) are sacrificed at CT0, CT6, CT12 and CT18. Gene expression is determined by real time QPCR. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Solt LA, et al. Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. Nature. 2012 Mar 29;485(7396):62-68. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2834 mL	11.4171 mL	22.8342 mL	57.0854 mL
	5 mM	0.4567 mL	2.2834 mL	4.5668 mL	11.4171 mL
	10 mM	0.2283 mL	1.1417 mL	2.2834 mL	5.7085 mL
	15 mM	0.1522 mL	0.7611 mL	1.5223 mL	3.8057 mL
	20 mM	0.1142 mL	0.5709 mL	1.1417 mL	2.8543 mL
	25 mM	0.0913 mL	0.4567 mL	0.9134 mL	2.2834 mL
	30 mM	0.0761 mL	0.3806 mL	0.7611 mL	1.9028 mL
	40 mM	0.0571 mL	0.2854 mL	0.5709 mL	1.4271 mL
	50 mM	0.0457 mL	0.2283 mL	0.4567 mL	1.1417 mL
	60 mM	0.0381 mL	0.1903 mL	0.3806 mL	0.9514 mL
	80 mM	0.0285 mL	0.1427 mL	0.2854 mL	0.7136 mL
	100 mM	0.0228 mL	0.1142 mL	0.2283 mL	0.5709 mL

SR9009 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.

Keywords:

SR90091379686-30-2SR 9009SR-9009AutophagyInhibitorinhibitorinhibit

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SR9009

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SR9009 Related Antibodies

28 Publications Citing Use of MCE SR9009

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Complete Stock Solution Preparation Table

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