- 商品介绍
- 规格参数
- 包装参数
General description
A cell-permeable pyrazolopyridinylpyrimidine compound that acts as a selective and potent stimulator of soluble guanylate cyclase (effective dose ~ 0.1 nM to 100 µM using recombinant soluble guanylate cyclase). The mode of activation is NO-independent and appears to be mediated through direct binding to the α1 and α2 subunits. Shown to be effective in treating numerous cardiovascular conditions in animal models. Inhibits phenylephrine-induced constriction of rabbit aortic rings (IC50 = 304 nM) and blocks collagen-induced aggregation of human platelets (IC50 = 36 nM). Does not inhibit phosphodiesterases.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Soluble guanylate cyclase
Product does not compete with ATP.
Reversible: no
Target IC50: 304 nM inhibiting phenylephrine-induced constriction of rabbit aortic rings; 36 nM in blocking collagen-induced aggregation of human platelets
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Boerrigter, G., et al. 2003. Circulation107, 686.
Kalsi, J.S., et al. 2003. J Urol.169, 761.
Koglin, M., et al. 2002. Biochem. Biophys. Res. Commun.292, 1057.
Becker, E.M., et al. 2001. BMC Pharmacol.1, 13.
Stasch, J.P., et al. 2001. Nature410, 212.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | white |
| solubility | DMSO: 10 mg/mL |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | Fc1c(cccc1)C[n]2nc(c5c2nccc5)c3nc(c(cn3)C4CC4)N |
| 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) |
| InChI key | ATOAHNRJAXSBOR-UHFFFAOYSA-N |
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