SR9009

$77.00
In stock
SKU
W1379686-30-2
CAS No. : 1379686-30-2 Purity: 99.58%
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]
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 (Kd=800 nM)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
While the stress of handling and twice-daily injections caused weight loss in vehicle-treated controls, weight loss of SR9009-treated animals is 60% greater. 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight
437.94
Formula
C??H??ClN?O?S
CAS No.
1379686-30-2
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
6 months

-20°C
1 month
Solvent & SolubilityIn Vitro:


DMSO : ≥ 100 mg/mL (228.34 mM)

H2O : < 0.1 mg/mL (insoluble)

*'≥' means soluble, but saturation unknown.


Preparing
Stock Solutions



Concentration Solvent Mass

1 mg

5 mg

10 mg


1 mM2.2834 mL11.4171 mL22.8342 mL
5 mM0.4567 mL2.2834 mL4.5668 mL
10 mM0.2283 mL1.1417 mL2.2834 mL

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

In Vivo:


1.


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


2.


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


3.


Add each solvent one by one: 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.75 mM); Clear solution


4.


Add each solvent one by one: 6% DMSO 10% Cremophor EL 84% ddH2O

Solubility: 6 mg/mL (13.70 mM); Suspended solution; Need ultrasonic


*All of the co-solvents are provided by MCE.
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.
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