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BAY 41-2272
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BAY 41-2272图片
CAS NO:256376-24-6
规格:≥98%
包装与价格:
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

产品介绍
理化性质和储存条件
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
实验参考方法
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.