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).

• 別名: BAY 41-2272, 5-Cyclopropyl-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-4-ylamine
• 実験式（ヒル表記法）: C₂₀H₁₇FN₆
• CAS番号: 256376-24-6
• 分子量: 360.39
• MDL番号: MFCD06411391
• UNSPSCコード: 51111800
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: white
• 溶解性: DMSO: 10 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C
• SMILES記法: 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

詳細

詳細

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.

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.

生物化学的／生理学的作用

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

警告

Toxicity: Standard Handling (A)

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

その他情報

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.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable