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    BAY 41-2272
    BAY 41-2272

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1869
    CAS #: 256376-24-6Purity ≥98%

    Description: BAY 41-2272 is a novel and potent activator of nitric oxide-sensitive guanylyl cyclase (NO-sensitive GC) with EC50 values of 0.3 μmol/L and 3 μmol/L in the presence and absence of 100 nmol/L DEA-NO, respectively. In platelets, GSNO at 3 μmol/L (a submaximally effective concentration) was used to assess a possible sensitizing effect of BAY 41-2272 on NO-sensitive GC. The cGMP response resulted from the application of NO at this concentration in the absence of BAY 41-2272 was only marginal. In the presence of BAY 41-2272 at 100 μmol/L, treatment with GSNO at 3 μmol/L resulted in a rapid increase in cGMP up to 1000 pmol/109 platelets.

    References: Circulation. 2004 Apr 13;109(14):1711-3; Nature. 2001 Mar 8;410(6825):212-5; J Urol. 2003 Feb;169(2):761-6.

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    Molecular Weight (MW)360.39 
    FormulaC20H17FN6 
    CAS No.256376-24-6 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 35 mg/mL (97.1 mM) 
    Water: <1 mg/mL
    Ethanol: 4 mg/mL (11.09 mM)
    Other infoIUPAC/Chemical Name: 5-cyclopropyl-2-[1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-pyrimidinamine
    InChi Key: ATOAHNRJAXSBOR-UHFFFAOYSA-N
    InChi Code: InChI=1S/C20H17FN6/c21-16-6-2-1-4-13(16)11-27-20-14(5-3-9-23-20)17(26-27)19-24-10-15(12-7-8-12)18(22)25-19/h1-6,9-10,12H,7-8,11H2,(H2,22,24,25)
    SMILES Code: NC1=NC(C2=NN(CC3=CC=CC=C3F)C4=NC=CC=C42)=NC=C1C5CC5
    SynonymsBAY 41-2272; BAY-41-2272; BAY41-2272; BAY412272; BAY-412272; BAY 412272


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    In Vitro

    In vitro activity: In vitro, BAY 41-2272 results in concentration dependent relaxation of human and rabbit cavernosum with EC50 of 489.1 nM and 406.3 nM, respectively.


    Kinase Assay: BAY 41-2272 is an activator of nitric oxide-sensitive guanylyl cyclase (NO-sensitive GC) with EC50 values of 0.3 μmol/L and 3 μmol/L in the presence and absence of 100 nmol/L DEA-NO, respectively.


    Cell Assay: In platelets, GSNO at 3 μmol/L (a submaximally effective concentration) was used to assess a possible sensitizing effect of BAY 41-2272 on NO-sensitive GC. The cGMP response resulted from the application of NO at this concentration in the absence of BAY 41-2272 was only marginal. In the presence of BAY 41-2272 at 100 μmol/L, treatment with GSNO at 3 μmol/L resulted in a rapid increase in cGMP up to 1000 pmol/109 platelets.

    In VivoIn female spontaneously hypertensive rats, BAY 41-2272 (10 mg/kg, p.o.) shows antiplatelet effect, strongly decreases blood pressure and increases survival. In C. albicans-infected mice, BAY 41-2272 (10 mg/kg, i.p.) markedly increases macrophage-dependent cell influx to the peritoneum in addition to macrophage functions, and reduces the death rate. In db/db-/- type II diabetic and obese mice, BAY 41-2272 improves impaired corpus cavernosum (CC) relaxation. 
    Animal modelFemale spontaneously hypertensive rats 
    Formulation & DosageDissolved in 10/20/70 (v/v/v) Transcutol/Cremophor EL/water; 1 mg/kg; p.o. 
    References

    Circulation. 2004 Apr 13;109(14):1711-3; Nature. 2001 Mar 8;410(6825):212-5; J Urol. 2003 Feb;169(2):761-6. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    BAY 41-2272


    sGC/cGMP/PKG signaling pathway in HNSCC cell lines. Cancer Lett. 2016 Jan 28;370(2):279-85.

     BAY 41-2272


    NO donors, sGC stimulators, and PDE5 inhibitors decrease the viability of HNSCC cells.  Cancer Lett. 2016 Jan 28;370(2):279-85.

     BAY 41-2272


    Tadalafil suppressed the growth of CAL27 xenografts in vivo. Cancer Lett. 2016 Jan 28;370(2):279-85.

     BAY 41-2272


    BAY 41-2272 (BAY) and Tadalafil (Tad) decrease cell proliferation and induce apoptosis in HNSCC cells. Cancer Lett. 2016 Jan 28;370(2):279-85.

     BAY 41-2272


    BAY 41-2272 (BAY) and Tadalafil (Tad) decrease clonogenic survival of HNSCC cells. CAL27 (A), UM6 (B) and UM47 (C) cells were plated at 150 cells/well in 6 well plates and treated before first doubling. After 72 h, treatments were replaced with growth media and colonies were allowed to form for 2 weeks. Colonies were stained with crystal violet and counted. Cancer Lett. 2016 Jan 28;370(2):279-85.

     BAY 41-2272


    Effect of sGC or PKG inhibitors on apoptosis induced by BAY or Tadalafil. Cancer Lett. 2016 Jan 28;370(2):279-85.


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