420336-M

KB-R7943

• 別名: KB-R7943, 2-(2-(4-(4-Nitrobenzyloxy)phenyl)ethyl)isothiourea, methane sulfonate, NMDA Antagonist III
• 実験式（ヒル表記法）: C₁₆H₁₇N₃O₃S · xCH₄O₃S
• CAS番号: 182004-65-5
• 分子量: 331.39 (free base basis)
• MDL番号: MFCD00952138
• UNSPSCコード: 12352200

特性

• アッセイ: ≥98% (HPLC)
• 品質水準: 100
• フォーム: crystalline solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; desiccated (hygroscopic); protect from light
• 色: white
• 溶解性: water: 4 mg/mL; DMSO: 40 mg/mL
• 保管温度: 2-8°C
• SMILES記法: [S](=O)(=O)(O)C.S(CCc1ccc(cc1)OCc2ccc(cc2)[N+](=O)[O-])\C(=N\[H])\N
• 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

詳細

詳細

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).

生物化学的／生理学的作用

Primary Target
Na+/Ca2+ exchangers

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

警告

Toxicity: Irritant (B)

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

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.

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