SR9011 hydrochloride

Cat. No.: HY-16988A Purity: 98.07%: FAQs
Data Sheet SDS COA Handling Instructions

SR9011 hydrochloride is a REV-ERBα/β agonist with IC₅₀s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively.

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

SR9011 hydrochloride Chemical Structure

CAS No. : 2070014-94-5

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10 mM * 1 mL in DMSO	USD 272	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL ready for reconstitution	USD 272	In-stock	Estimated Time of Arrival: December 31
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5 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 420	In-stock	Estimated Time of Arrival: December 31
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100 mg	USD 2520	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of SR9011 hydrochloride:

SR9011 In-stock

7 Publications Citing Use of MCE SR9011 hydrochloride

•Br J Pharmacol. 2021 Jan;178(2):328-345. [Abstract]

: SR9011 hydrochloride purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2019 Jan;40(1):26-34. [Abstract]; BV2 cells are pretreated with different doses of SR9011 (0-10 μM) for 4 h and then exposed to LPS (100 ng/mL) for 12 h. Cell lysates are analyzed by Western blot for iNOS, COX-2, and GAPDH. The relative band intensities of iNOS and COX-2 to GAPDH are analyzed

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

SR9011 hydrochloride is a REV-ERBα/β agonist with IC₅₀s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively.

IC₅₀ & Target

IC50: 790 nM (Rev-ErbBα), 560 nM (Rev-ErbBβ)^[1]

In Vitro

SR9011 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 (REV-ERBα IC₅₀=790 nM, REV-ERBβ IC₅₀=560 nM). SR9011 potently and efficaciously suppresses transcription in a cotransfection assay using full-length REV-ERBα along with a luciferase reporter driven by the Bmal1 promoter (SR9011 IC₅₀=620 nM). SR9011 suppresses the expression ofBMAL1 mRNA in HepG2 cells in a REV-ERBα/β-dependent manner^[1] SR9011 suppresses proliferation of the breast cancer cell lines regardless of their ER or HER2 status. SR9011 appears to pause the cell cycle of the breast cancer cells prior to M phase. Cyclin A (CCNA2) is identified as a direct target gene of REV-ERB suggesting that suppression of expression of this cyclin by SR9011 may mediate the cell cycle arrest. Treatment with SR9011 results in an increase in cells in the G₀/G₁ phase and a decrease of cells in S and G₂/M phase suggesting that activation of REV-ERB may be resulting in decreased transition from G₁ to S phase and/or from S to G₂/M phase^[2].

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

In Vivo

SR9011 displays reasonable plasma exposure, thus, the expression of REV-ERB responsive genes is examined in the liver of mice treated with various doses of SR9011 for 6-days. The plasminogen activator inhibitor type 1 gene (Serpine1) is a REV-ERB target gene and displays dose-dependent suppression of expression in response to SR9011. The cholesterol 7α-hydroxylase (Cyp7a1) and sterol response element binding protein (Srepf1) genes have also been shown to be responsive to REV-ERB and are dose-dependently suppressed with increasing amounts of SR9011. After 12 days in D:D conditions mice are injected with a single dose of SR9011 or vehicle at CT6 (peak expression of Rev-erbα). Vehicle injection causes no disruption in circadian locomotor activity. However, administration of a single dose of SR9011 results in loss of locomotor activity during the subject dark phase. Normal activity returns the next circadian cycle, consistent with clearance of the drugs in less than 24h. The SR9011-dependent decrease in wheel running behavior in the mice under constant darkness conditions is dose-dependent and that the potency (ED₅₀=56 mg/kg) is similar to the potency of SR9011-mediated suppression of a REV-ERB responsive gene, Srebf1 , in vivo (ED₅₀=67mg/kg)^[1].

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

Molecular Weight

515.50

Appearance

Solid

Formula

C₂₃H₃₂Cl₂N₄O₃S

CAS No.

2070014-94-5

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 32 mg/mL (62.08 mM)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9399 mL	9.6993 mL	19.3986 mL
5 mM	0.3880 mL	1.9399 mL	3.8797 mL
10 mM	0.1940 mL	0.9699 mL	1.9399 mL

*Please refer to the solubility information to select the appropriate solvent.

Purity & Documentation

Purity: 98.07%

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Data Sheet (281 KB) SDS (251 KB)

COA (251 KB) HNMR (211 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):62-8. [Content Brief]

[2]. Wang Y, et al. Anti-proliferative actions of a synthetic REV-ERBα/β agonist in breast cancer cells. Biochem Pharmacol. 2015 Aug 15;96(4):315-22. [Content Brief]

Cell Assay ^[2]	MCF10A, MDA-MB-231, MCF-7, MDA-MB-361, SKBR3, BT474 cells are plated in 6-well plates one day before treatment. The MTT cell proliferation assays are performed. Briefly, 3×10³ to 5 × 10³ cells per well are plated in 96-well plates. Twenty-four hours later, cells are treated with SR9011 (0, 2, 4, 6, 8 and 10 μM) or DMSO. Seventy-two hours after treatment, the cells are labeled with 1.2 mM MTT and incubated for 4 hours. DMSO is then added and readings are taken on a plate reader at 540 nm^[2]. 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 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):62-8. [Content Brief] [2]. Wang Y, et al. Anti-proliferative actions of a synthetic REV-ERBα/β agonist in breast cancer cells. Biochem Pharmacol. 2015 Aug 15;96(4):315-22. [Content Brief]