| CAS NO: | 256376-24-6 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 360.39 |
|---|---|
| Formula | C20H17FN6 |
| 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 info | IUPAC/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 |
| Synonyms | BAY 41-2272; BAY-41-2272; BAY41-2272; BAY412272; BAY-412272; BAY 412272 |
| 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 Vivo | In 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 model | Female spontaneously hypertensive rats |
| Formulation & Dosage | Dissolved 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. |
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