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Chemical Structure| 1227633-49-9 Chemical Structure| 1227633-49-9

Structure of StemRegenin 1
CAS No.: 1227633-49-9

Chemical Structure| 1227633-49-9

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StemRegenin 1 is an effective aryl hydrocarbon receptor (AhR) antagonist with an IC50 of 127 nM.

Synonyms: SR1

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Product Details of StemRegenin 1

CAS No. :1227633-49-9
Formula : C24H23N5OS
M.W : 429.54
SMILES Code : OC1=CC=C(CCNC2=C3N=CN(C(C)C)C3=NC(C4=CSC5=CC=CC=C54)=N2)C=C1
Synonyms :
SR1
MDL No. :MFCD16987861
InChI Key :BGFHMYJZJZLMHW-UHFFFAOYSA-N
Pubchem ID :46199207

Safety of StemRegenin 1

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • AhR

    Aryl hydrocarbon receptor (AhR), IC50:127 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
human CD34+ cells 120 nM 5 to 7 days SR1 increases the number of CD34+ cells with an EC50 of 120 nM PMC3033342
human CB CD34+ cells 1 μM 5 weeks SR1 expands CD34+ cells by 17,100-fold, increases TNC by 10-fold, and CD34+ cells by 47-fold PMC3033342
CD34+ hematopoietic stem and progenitor cells 2 µM 21 days Generate highly functional HSPC-NK cells, demonstrating efficient cytolytic activity against ovarian cancer cells PMC5593716
CD34+ HSPCs 0.75 µM 15 days SR1 significantly enhanced the expansion of CD34+ HSPCs and generated large numbers of proT cells in OP9-DL1 cell coculture. PMC6849952
CD34+ CD7+ cells 0.75 µM 14 days SR1-expanded HSPCs generated proT cells in OP9-DL1 cell coculture and showed effective thymus-seeding and peripheral T-cell functional capabilities in vivo. PMC6849952
Human cord blood CD34+ cells 1 µM 9 days To compare the effects of StemRegenin 1 on the ex vivo expansion of cord blood CD34+ cells under different cytokine conditions, results showed that StemRegenin 1 effectively maintained the CD34+/CD133+ stem cell phenotype and had a superior expansion effect compared to other cytokine combinations. PMC4542867
Human HSPCs 1 µM 5 days SR1 enhanced the population of CD34-positive cells, indicating it promoted the expansion of HSPCs PMC10045038
Human HSPCs 1 µM 3 days SR1 enhanced the population of CD34-positive cells post-radiation, indicating it modulated the radioresponse of HSPCs PMC10045038
Bone marrow macrophages (BμMs) 10 μM 48 h and 96 h To evaluate the cytotoxicity of SR1 on BμMs, the results showed that SR1 had no effect on the proliferative activity of BμMs at 10 μM or lower concentrations. PMC11039397
Bone marrow macrophages (BμMs) Various concentrations (3, 6, 8, 10 μM) 4 days To evaluate the effect of SR1 on AhR expression in BμMs, the results showed that SR1 significantly reduced the expression of AhR. PMC11039397
Bone marrow macrophages (BμMs) Various concentrations (3, 6, 8, 10 μM) 7 days To evaluate the effect of SR1 on the differentiation of BμMs into osteoclasts, the results showed that SR1 significantly reduced the number and area of osteoclasts. PMC11039397

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
mice NOD.Cg-Prkdcscid Il2rgtm1Wjl /SzJ (NSG) mice transplantation 1 mg/mouse Once daily for 5 days SR1-expanded CB CD34+ cells showed significant increases in human engraftment in NSG mice PMC3033342
NOD/SCID/IL2Rγnull mice Ovarian cancer model Intraperitoneal injection 0.75 μM 21 days Evaluate the anti-tumor effects of HSPC-NK cells in vivo, showing that HSPC-NK cells significantly inhibited tumor progression and prolonged mouse survival PMC5593716
NSG mice Immunodeficient mouse model Intrahepatic injection 50 mg/kg daily until the end of the experiment SR1-expanded proT cells showed effective thymus-seeding and peripheral T-cell functional capabilities in NSG mice, and generated a polyclonal T-cell receptor repertoire. PMC6849952
NSG mice NSG mouse model transplantation 12 × 10^6 cells/mouse/infusion Two infusions, lasting until day 21 Evaluate the in vivo functional potential of HSCs expanded under different small molecule combinations (UM171, SR1+Ly, and SR1+Ly+UM171) PMC6430062
C57BL/6 mice Total body irradiation model Intraperitoneal injection 20 mg single implantation, sustained for 30 days SR1 significantly increased the survival rate of mice post-irradiation (80% vs 30%) and promoted the recovery of peripheral blood cell counts PMC10045038
C57BL/6 female mice Ovariectomy (OVX)-induced osteoporosis model Injection 10 mg/kg Once daily for 3 days To evaluate the effect of SR1 on bone loss in OVX mice, the results showed that SR1 significantly improved bone loss in mice. PMC11039397

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.33mL

0.47mL

0.23mL

11.64mL

2.33mL

1.16mL

23.28mL

4.66mL

2.33mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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