420336-M

KB-R7943

• Synonym(e): KB-R7943, 2-(2-(4-(4-Nitrobenzyloxy)phenyl)ethyl)isothiourea, methane sulfonate, NMDA Antagonist III
• Empirische Formel (Hill-System): C₁₆H₁₇N₃O₃S · xCH₄O₃S
• CAS-Nummer: 182004-65-5
• Molekulargewicht: 331.39 (free base basis)
• UNSPSC-Code: 12352200

Eigenschaften

• Assay: ≥98% (HPLC)
• Qualitätsniveau: 100
• Form: crystalline solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; desiccated (hygroscopic); protect from light
• Farbe: white
• Löslichkeit: water: 4 mg/mL; DMSO: 40 mg/mL
• Lagertemp.: 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)
• InChIKey: WGIKEBHIKKWJLG-UHFFFAOYSA-N

Beschreibung

Allgemeine Beschreibung

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).

Biochem./physiol. Wirkung

Primary Target
Na+/Ca2+ exchangers

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

Warnhinweis

Toxicity: Irritant (B)

Rekonstituierung

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

Sonstige Hinweise

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.

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable