420336-M

KB-R7943

• Synonym(s): KB-R7943, 2-(2-(4-(4-Nitrobenzyloxy)phenyl)ethyl)isothiourea, methane sulfonate, NMDA Antagonist III
• Empirical Formula (Hill Notation): C₁₆H₁₇N₃O₃S · xCH₄O₃S
• CAS Number: 182004-65-5
• Molecular Weight: 331.39 (free base basis)
• UNSPSC Code: 12352200

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• form: crystalline solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• color: white
• solubility: water: 4 mg/mL; DMSO: 40 mg/mL
• storage temp.: 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)
• InChI key: WGIKEBHIKKWJLG-UHFFFAOYSA-N

Description

General description

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 Actions

Primary Target
Na+/Ca2+ exchangers

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

Warning

Toxicity: Irritant (B)

Reconstitution

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

Other Notes

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.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable