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| 25mg |
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Purity: ≥98%
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. BAY 41-2272 may have a sensitizing effect on NO-sensitive GC in platelets when GSNO at 3 μmol/L (a submaximally effective concentration) is evaluated. Applying NO at this concentration without BAY 41-2272 produced a cGMP response that was merely marginal. A quick rise in cGMP up to 1000 pmol/109 platelets was observed following treatment with GSNO at 3 μmol/L in the presence of BAY 41-2272 at 100 μmol/L.
| Targets |
Guanylate cyclase
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
BAY 41-2272 is an activator of guanylyl cyclase sensitive to nitric oxide (NO-sensitive GC), with EC50 values of 3 μmol/L and 0.3 μmol/L in the presence and absence of 100 nmol/L DEA-NO, respectively.
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| Cell Assay |
BAY 41-2272 may have a sensitizing effect on NO-sensitive GC in platelets when GSNO at 3 μmol/L (a submaximally effective concentration) is evaluated. Applying NO at this concentration without BAY 41-2272 produced a cGMP response that was merely marginal. A quick rise in cGMP up to 1000 pmol/109 platelets was observed following treatment with GSNO at 3 μmol/L in the presence of BAY 41-2272 at 100 μmol/L.
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| Animal Protocol |
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| References | |||
| Additional Infomation |
BAY 41-2272 is a pyrazolopyridine that is 1H-pyrazolo[3,4-b]pyridine which is substituted by a 2-fluorobenzyl group at position 1 and by a 4-amino-5-cyclopropylpyrimidin-2-yl group at position 3. It is an activator of soluble guanylate cyclase. It has a role as a soluble guanylate cyclase activator, a platelet aggregation inhibitor, a vasodilator agent and an antihypertensive agent. It is a pyrazolopyridine, a member of monofluorobenzenes, an aminopyrimidine and a member of cyclopropanes.
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| Molecular Formula |
C20H17FN6
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| Molecular Weight |
360.39
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| Exact Mass |
360.149
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| Elemental Analysis |
C, 66.65; H, 4.75; F, 5.27; N, 23.32
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| CAS # |
256376-24-6
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| Related CAS # |
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| PubChem CID |
9798973
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
496.1±45.0 °C at 760 mmHg
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| Flash Point |
253.8±28.7 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.767
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| LogP |
1.99
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
517
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1=C([H])C([H])=C([H])C([H])=C1C([H])([H])N1C2=C(C([H])=C([H])C([H])=N2)C(C2=NC([H])=C(C(N([H])[H])=N2)C2([H])C([H])([H])C2([H])[H])=N1
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| InChi Key |
ATOAHNRJAXSBOR-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
5-cyclopropyl-2-[1-[(2-fluorophenyl)methyl]pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-4-amine
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.75 mg/mL (4.86 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 17.5 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: ≥ 1.75 mg/mL (4.86 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 17.5 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. View More
Solubility in Formulation 3: ≥ 1.75 mg/mL (4.86 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7748 mL | 13.8739 mL | 27.7477 mL | |
| 5 mM | 0.5550 mL | 2.7748 mL | 5.5495 mL | |
| 10 mM | 0.2775 mL | 1.3874 mL | 2.7748 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.
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.
 sGC/cGMP/PKG signaling pathway in HNSCC cell lines.Cancer Lett. 2016 Jan 28;370(2):279-85. |
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 NO donors, sGC stimulators, and PDE5 inhibitors decrease the viability of HNSCC cells.Cancer Lett. 2016 Jan 28;370(2):279-85. |
 Tadalafil suppressed the growth of CAL27 xenograftsin vivo.Cancer Lett. 2016 Jan 28;370(2):279-85. |
 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. |
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 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. |
 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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