StemRegenin 1 (SR1)

Catalog No.S2858

StemRegenin 1 is an aryl hydrocarbon receptor (AhR) inhibitor with IC50 of 127 nM in a cell-free assay.

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StemRegenin 1 (SR1) Chemical Structure

StemRegenin 1 (SR1) Chemical Structure
Molecular Weight: 429.54

Validation & Quality Control

Quality Control & MSDS

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StemRegenin 1 (SR1) is available in the following compound libraries:

Product Information

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Product Description

Biological Activity

Description StemRegenin 1 is an aryl hydrocarbon receptor (AhR) inhibitor with IC50 of 127 nM in a cell-free assay.
Targets Aryl hydrocarbon receptor (AhR) [1]
()
IC50 127 nM
In vitro StemRegenin 1 increases the number of CD34+ cells after 5 to 7 days with an EC50 of 120 nM. Culture of mPB CD34+ cells with cytokines plus SR1 (1 μM) for 7 days increases the number of CD34+, CD133+, and CD90+ hematopoietic stem and progenitor cell populations 2.6-, 2.3-, and 10-fold, respectively compared to control cells. Continued culture with SR1 (1 μM) for 3 weeks leads to an 11-fold increase in total nucleated cells (TNC), a 73-fold increase in CD34+ cells as compared to control cultures, and a 1118-fold increase in CD34+ cells relative to input cells. Culture of 1×103 cord blood CD34+ cells for 5 weeks with SR1 (1 μM) results in the production of 1.69×106 colony forming cells. SR1-induces CD34+ cell expansion acts by binding and antagonizing AhR as evident by decreased CYP1B1 and AHRR mRNA levels. [1] SR1 (1 μM) treatment accelerates the proliferation of CD34+ cells and decreased the expression levels of VentX in human CD34+ cells. Ectopic expression of VentX prevents SR1-induced expansion of CD34+ cells. [2] Sequential coculture with bone morphogenetic protein 4 (20 ng/mL), PGE2 (2 μM), and SR1 (0.75 μM) lead to robust Macaca nemestrina iPSC hematopoietic progenitor cell formation. CD34(+)CD38(-)Thy1(+)CD45RA(-)CD49f(+) cells isolated on the basis of CD34 expression and cultured in SR1 (0.75 μM) expands 3-fold and maintained this long-term repopulating HSC phenotype. [3]
In vivo SR1 promotes expansion of CB CD34+ cells that contribute to both early and sustained engraftment NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice. [1]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

AhR ligand binding assay Mouse livers are homogenized in buffer (25 mM MOPS, 2 mM EDTA, 0.02% NaN3, and 10% glycerol, pH 7.4) containing 20 mM sodium molybdate and protease inhibitors and centrifuged at 100,000g for 1 h. ligand-treated lysates are incubated at room temperature for 20 min and then photolyzes at 8 cm with 402 nm UV light. Dextran-coated charcoal (1%) is added to the photolyzed samples, which are then centrifuged at 3000g for 10 min to remove free ligand. Labeled samples are resolved using 8% acrylamide-tricine-SDS-PAGE, transferred to PVDF membrane, and visualized using autoradiography. Labeled AHR bands are excised and counted using a γ counter.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Boitano AE, et al. Science, 2010, 329(5997), 1345-1348.

[2] Gao H, et al. J Biol Chem, 2012, 287(35), 29979-29987.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02827513 Terminated Adult Attention-deficit Hyperactivity Disorder (ADHD) Neurovance, Inc.|Euthymics BioScience, Inc. December 2015 Phase 1
NCT01744808 Completed Normal, Healthy Volunteers Neurovance, Inc.|Euthymics BioScience, Inc. February 2013 Phase 1
NCT00557973 Completed Muscle Spasticity Indivior Inc. December 2007 Phase 2

Chemical Information

Download StemRegenin 1 (SR1) SDF
Molecular Weight (MW) 429.54
Formula

C24H23N5OS

CAS No. 1227633-49-9
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 86 mg/mL (200.21 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Phenol, 4-[2-[[2-benzo[b]thien-3-yl-9-(1-methylethyl)-9H-purin-6-yl]amino]ethyl]-

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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