StemRegenin 1 (SR1)

Alias: SetmEegenin 1; SR1
Cat No.:V0951 Purity: ≥98%
StemRegenin 1(abbreviated as SR1; SR-1),a purine derivative, is a potent antagonist of the aryl hydrocarbon receptor(AhR)with important biological activity.
StemRegenin 1 (SR1) Chemical Structure CAS No.: 1227633-49-9
Product category: AhR
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

StemRegenin 1(abbreviated as SR1; SR-1), a purine derivative, is a potent antagonist of the aryl hydrocarbon receptor (AhR) with important biological activity. It inhibits AhR with IC50 of 127 nM in CD34+ cells. SR1 has been found to promote the ex vivo expansion of CD34+ cells. SR1 has also been found to induce the ex vivo differentiation of pDCs, BDCA1+ and BDCA3+ mDCs as well as the generation of high numbers of all these DC subsets.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
The aryl hydrocarbon receptor is antagonistically acted upon by stem regenin 1 (SR1). (AhR). With an EC50 of less than 120 nM, stemregenin 1 boosts the number of CD34+ cells after 5 to 7 days. Based on these findings, it can be concluded that StemRegenin 1-induced CD34+ cell growth is mediated by direct binding and AhR inhibition (IC50=40 nM). StemRegenin 1 also reduces photoaffinity ligand (PAL) binding. StemRegenin 1 (SR1), an antagonist of the aryl hydrocarbon receptor, strongly encourages the ex vivo growth of human CD34+ cells. Treatment with stemgenin 1 reduces VentX expression levels and speeds up CD34+ cell proliferation[2].
ln Vivo
SR1 promotes expansion of CB CD34+ cells that contribute to both early and sustained engraftment NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice.
Animal Protocol
N/A
Mice
References
[1]. Boitano AE, et al. Aryl Hydrocarbon Receptor Antagonists Promote the Expansion of Human Hematopoietic Stem Cells. Science. 2010 Sep 10;329(5997):1345-8.
[2]. Gao H, et al. Suppression of homeobox transcription factor VentX promotes expansion of human hematopoietic stem/multipotent progenitor cells. J Biol Chem. 2012 Aug 24;287(35):29979-87
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H23N5OS
Molecular Weight
429.54
CAS #
1227633-49-9
Related CAS #
1227633-49-9
SMILES
OC1=CC=C(CCNC2=C3N=CN(C(C)C)C3=NC(C4=CSC5=CC=CC=C54)=N2)C=C1
Synonyms
SetmEegenin 1; SR1
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 86 mg/mL (200.2 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.82 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: 2.5 mg/mL (5.82 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (5.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.3281 mL 11.6404 mL 23.2807 mL
5 mM 0.4656 mL 2.3281 mL 4.6561 mL
10 mM 0.2328 mL 1.1640 mL 2.3281 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • StemRegenin 1 (SR1)

  • StemRegenin 1 (SR1)

  • StemRegenin 1 (SR1)

    SR1-induced CD34+ cell expansion acts by binding and antagonizing AhR. Science. 2010 Sep 10;329(5997):1345-8.
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