370679

Guanosine 3′,5′-cyclic Monophosphorothioate, β-Phenyl-1,N²-etheno-8-bromo-, Rp-Isomer, Sodium Salt

A metabolically-stable, competitive inhibitor of protein kinase G types 1α and 1β (K_i = 30 nM).

• Synonyme(s) : Guanosine 3′,5′-cyclic Monophosphorothioate, β-Phenyl-1,N²-etheno-8-bromo-, Rp-Isomer, Sodium Salt, Rp-8-Br-PET-cGMPS, Na, PKG Inhibitor VI
• Formule empirique (notation de Hill): C₁₈H₁₄BrN₅O₆PS · Na
• Numéro CAS: 172806-20-1
• Poids moléculaire : 562.27
• Code UNSPSC : 41106305
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: lyophilized
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; desiccated (hygroscopic)
• Solubilité: water: 5 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −20°C
• InChI: 1S/C18H15BrN5O6PS.Na/c19-17-21-11-14(24(17)16-12(25)13-10(29-16)7-28-31(27,32)30-13)22-18-20-9(6-23(18)15(11)26)8-4-2-1-3-5-8;/h1-6,10,12-13,16,25H,7H2,(H,20,22)(H,27,32);/q;+1/p-1/t10-,12-,13-,16-,31?;/m1./s1
• Clé InChI: SVMPQLHYWRTQCX-WKKXCKAJSA-M

Description

Description générale

A metabolically-stable, competitive inhibitor of protein kinase G type Iα and Iβ (K_i = 30 nM) that also blocks cGMP-gated retinal type ion channels (IC₅₀ = 25 µM). Also reported to block the activation of purified PKA type II (K_i = 10 µM). More lipophilic and cell-permeable than Rp-8-pCPT-cGMPS (Cat. No. 370677). Note: 5 µmol = 2.81 mg.

A metabolically-stable, competitive inhibitor of protein kinase G types 1α and 1β (K_i = 30 nM). Blocks cGMP-gated retinal type ion channels (IC₅₀ = 25 µM) and the activation of purified PKA type II (K_i = 10 µM). More lipophilic and cell-permeable than Rp-8-pCPT-cGMPS (Cat. No. 370677). Note: 1 µmol = 0.56 mg.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
PKG1α & 1β

Product does not compete with ATP.

Reversible: no

Target K_i: 30 nM against PKG1α & 1β

Avertissement

Toxicity: Standard Handling (A)

Autres remarques

Wei, J.Y., et al. 1996. Biochemistry35, 16815.
Butt, E., et al. 1995. Br. J. Pharmacol. 116, 3110.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 2
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable