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Merck

196876

BAY 41-2272

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).

동의어(들):

BAY 41-2272, 5-Cyclopropyl-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-4-ylamine

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제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):
C20H17FN6
CAS 번호:
Molecular Weight:
360.39
MDL number:
UNSPSC Code:
51111800
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
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Quality Segment

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

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)


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저장 등급

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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