SR9009, also known as Stenabolic, is a research drug that was developed by professor Thomas Burris of the Scripps Research Institute as an agonist of Rev-ErbA (i.e., increases the constitutive repression of genes regulated by Rev-ErbA) with a half-maximum inhibitory concentration (IC50) = 670 nM for Rev-ErbAα and IC50 = 800 nM for Rev-ErbAβ. In an animal study, some of its effects were found to be independent of REV-ERB with an unknown mechanism of action.
Activation of Rev-ErbA-α buy SR9009 in mice increases exercise capacity by increasing mitochondria counts in skeletal muscle.
Description
SR-9009 is an agonist at nuclear receptor Rev-ErbA. Greatly diminishes VILI-induced lung edema, inflammatory cell infiltration and TNFα production in a rat lung injury model. SR-9009 suppresses atherosclerosis in a mouse model. Specifically lethal to cancer cells and oncogene-induced senescent cells with no effect on the viability of normal cells or tissues. Disrupts pain associated with osteoarthritis by reducing BMAL1 expression in bmal1f/fNav1.8CreERT mice.
Uses SR 9009 is a synthetic REV-ERB agonist that regulates circadian behavior and metabolism; has potential use in the treatment of sleep disorders and metabolic diseases. It is a lead compound for a new class of cancer drugs associated with the body’s circadian clock.
Pharmaceutical Applications SR9009 is a research drug that was developed by professor Thomas Burris of the Scripps Research Institute as an agonist of Rev-ErbA (i.e., increases the constitutive repression of genes regulated by Rev-ErbA) with a half-maximum inhibitory concentration (IC50) = 670 nM for Rev-ErbAα and IC50 = 800 nM for Rev-ErbAβ.
sr9009 Side effects
No side effect caused by SR9009 has been identified. It can then be rightly said that the supplement is very safe to consume. SR9009 does not influence the hormones in any way and so won’t aromatize into the estrogen, and won’t suppress the production of testosterone. Just like other supplements like SARMS, SR9009 does not deposit toxins in the liver, though it is needful for there to be some supplements that will support the liver when using it. 3 to 5 capsules of N2Guard taken every day will serve as good support to the kidney and liver.
in vitro IC50: 670 nM for REV-ERB-α and 800 nM for REV-ERB-β
SR9009, also known as Stenabolic, is a research drug as agonist of REV-ERB.
REV-ERB-α and REV-ERB-β, two nuclear receptors, have a critical role in regulating the expression of core clock proteins driving rhythms in activity and metabolism.
In vitro: Both SR9009 and its analog SR9011 powder could dose-dependently increase the REV-ERB-dependent repressor activity assessed in HEK293 cells expressing a chimaeric Gal4 DNA binding domain: REV-ERB ligand binding domain α or β and a Gal4-responsive luciferase reporter. Also, SR9009 was found to be able to suppress BMAL1 messenger RNA expression in HepG2 cells in a REV-ERB-α/β-dependent manner.
In vivo: Mice were treated with a single dose of SR9009, SR9011 or vehicle at circadian time 6 (CT6 (6h after lights on) after 12 days in D/D conditions showing peak expression of Rev-erb-α. Results showed that vehicle injection caused no disruption in circadian locomotor activity. In contrast, administration of a single dose of either SR9009 or SR9011 led to the loss of locomotor activity during the subject dark phase. In addition, the normal activity returned the next circadian cycle, which was consistent with clearance of the drugs in less than 24h.
Clinical trial: Up to now, SR9009 is still in the preclinical development stage.
storage Store at +4°C
Sarm SR9009 Chemical Properties
Melting point 79-81°C
Boiling point 547.2±45.0 °C(Predicted)
density 1.327±0.06 g/cm3(Predicted)
storage temp. -20°
solubility Soluble in DMSO (greater than 25 mg/ml) or in Ethanol (up to 20 mg/ml).
pka 6.12±0.50(Predicted)
form solid
color Tan
Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.
InChI InChI=1S/C20H24ClN3O4S/c1-2-28-20(25)23-10-9-16(13-23)12-22(11-15-3-5-17(21)6-4-15)14-18-7-8-19(29-18)24(26)27/h3-8,16H,2,9-14H2,1H3
InChIKey MMJJNHOIVCGAAP-UHFFFAOYSA-N
SMILES N1(C(OCC)=O)CCC(CN(CC2=CC=C(Cl)C=C2)CC2SC([N+]([O-])=O)=CC=2)C1
More Introduction:https://en.wikipedia.org/wiki/SR9009
