420336-M

KB-R7943

• Synonyme(s) : KB-R7943, 2-(2-(4-(4-Nitrobenzyloxy)phenyl)ethyl)isothiourea, methane sulfonate, NMDA Antagonist III
• Formule empirique (notation de Hill): C₁₆H₁₇N₃O₃S · xCH₄O₃S
• Numéro CAS: 182004-65-5
• Poids moléculaire : 331.39 (free base basis)
• Code UNSPSC : 12352200

Propriétés

• Pureté: ≥98% (HPLC)
• Niveau de qualité: 100
• Forme: crystalline solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; desiccated (hygroscopic); protect from light
• Couleur: white
• Solubilité: water: 4 mg/mL; DMSO: 40 mg/mL
• Température de stockage: 2-8°C
• InChI: 1S/C16H17N3O3S.CH4O3S/c17-16(18)23-10-9-12-3-7-15(8-4-12)22-11-13-1-5-14(6-2-13)19(20)21;1-5(2,3)4/h1-8H,9-11H2,(H3,17,18);1H3,(H,2,3,4)
• Clé InChI: WGIKEBHIKKWJLG-UHFFFAOYSA-N

Description

Description générale

A cell-permeable inhibitor of the influx/reverse mode of the Na⁺/Ca²⁺ exchanger (NCX) (IC₅₀ = 4.3 µM for NCX1, 4.7 µM for NCX2, and 1.4 µM for NCX3). Directly modulates Na⁺/Mg²⁺ exchange in a Ca²⁺-dependent manner. Reported ot offer neuronal and cardio-protection against ischemic injury. Also inhibits nicotinic acetylcholine receptors and NMDA receptor channels (IC₅₀<10 µM).

A cell-permeable isothiourea derivative that inhibits the influx/reverse mode of Na⁺/Ca²⁺ exchangers (NCX; IC₅₀ = 4.3 µM, 4.7 µM, and 1.4 µM for NCX1,NCX2, and NCX3, respectively) and directly modulates Na⁺/Mg²⁺ exchange in a Ca²⁺-dependent manner. Reported to offer neuronal and cardioprotection. Also inhibits nicotinic acetylcholine receptors and NMDA receptor channels (IC₅₀<10 µM).

Actions biochimiques/physiologiques

Primary Target
Na+/Ca2+ exchangers

Target IC₅₀: 4.3 µM, 4.7 µM, and 1.4 µM for NCX1,NCX2, and NCX3, respectively

Avertissement

Toxicity: Irritant (B)

Reconstitution

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

Autres remarques

Hobai, I.A., and O′Rourke, B. 2004. Expert Opin. Investig. Drugs13, 653.
Uetani, T., et al. 2003. J. Biol. Chem.278, 47491.
Iwamoto, T., et al. 2001. Mol. Pharmacol.59, 524.
Pintado, A.J., et al. 2000. Br. J. Pharmacol.130, 1893.
Sobolevsky, A.I., and Khodorov, B.I. 1999. Neuropharmacology38, 1235.
Iwamoto, T., et al. 1996. J. Biol. Chem.271, 22391.
Watano, T., et al. 1996. Br. J. Pharmacol.119, 555.

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 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable