2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE
- Product Name
- 2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE
- CAS No.
- 182004-65-5
- Chemical Name
- 2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE
- Synonyms
- IN1281;KB-R7943;KB-R7943 MESYLATE;KB-R7943, NCX inhibitor;KB-R7943 mesylate, 10 mM in DMSO;KB-R7943 - CAS 182004-65-5 - Calbiochem;-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE;2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE;S-[4-[(4-Nitrobenzyl)oxy]phenethyl]isothiourea Methanesulfonate;4-((4-Nitrobenzyl)oxy)phenethyl carbaMiMidothioate Methanesulfonate
- CBNumber
- CB6422033
- Molecular Formula
- C17H21N3O6S2
- Formula Weight
- 427.49
- MOL File
- 182004-65-5.mol
2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE Property
- Melting point:
- >214°C (dec.)
- storage temp.
- Inert atmosphere,2-8°C
- solubility
- Soluble in DMSO (up to 50 mg/ml).
- form
- White crystalline solid
- color
- Tan
- Water Solubility
- water: 4mg/mL
DMSO: 40mg/mL - Stability:
- Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
- InChI
- 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
- SMILES
- S(O)(=O)(=O)C.C(C1C=CC(N(=O)=O)=CC=1)OC1C=CC(CCSC(N)=N)=CC=1
Safety
- HS Code
- 2930.90.2900
N-Bromosuccinimide Price
- Product number
- 420336-M
- Product name
- KB-R7943
- Packaging
- 1 unit
- Price
- $154
- Updated
- 2025/07/31
- Product number
- N0966
- Product name
- S-[4-[(4-Nitrobenzyl)oxy]phenethyl]isothiourea Methanesulfonate
- Purity
- >98.0%(HPLC)
- Packaging
- 10mg
- Price
- $119
- Updated
- 2025/07/31
- Product number
- N0966
- Product name
- S-[4-[(4-Nitrobenzyl)oxy]phenethyl]isothiourea Methanesulfonate
- Purity
- >98.0%(HPLC)
- Packaging
- 50mg
- Price
- $413
- Updated
- 2025/07/31
- Product number
- 16352
- Product name
- KB-R7943 (mesylate)
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $49
- Updated
- 2024/03/01
- Product number
- 16352
- Product name
- KB-R7943 (mesylate)
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $77
- Updated
- 2024/03/01
2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE Chemical Properties,Usage,Production
Description
KB-R7943 (182004-65-5) is a potent and selective inhibitor of the reversed Na+/Ca2+ exchanger (NCE or NCX; IC50‘s = 1.2-2.4 μM in cardiomyocytes, smooth muscle cells, NCX1-transfected fibroblasts1; 0.7 μM in cultured rat forebrain2). KB-R7943 has also been shown to inhibit the mitochondrial Ca2+ uniporter (MCU) Ki = 5.5 μM.3 Recently shown to inhibit complex I in the mitochondrial respiratory chain (IC50 = 11.4 μM) and block NMDA receptors (IC50 = 13.4 μM).4
Uses
KB-R7943 Mesylate is a selective inhibitor of the reverse mode of Na+/Ca2+ exchange in cells expressing NCX1.
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).
Biological Activity
Potent, selective inhibitor of the reverse mode of the Na + /Ca 2+ exchanger (IC 50 = 0.7 mM). Does not affect Na + -dependent transport systems, Na + channels or ionotropic glutamate receptors.
Biochem/physiol Actions
Target IC50: 4.3 μM, 4.7 μM, and 1.4 μM for NCX1,NCX2, and NCX3, respectively
storage
Room temperature
References
[1] T IWAMOTO M S T Watano. A novel isothiourea derivative selectively inhibits the reverse mode of Na+/Ca2+ exchange in cells expressing NCX1.[J]. The Journal of Biological Chemistry, 1996, 271 37: 22391-22397. DOI:10.1074/jbc.271.37.22391
[2] K. HOYT. Reverse Na+/Ca2+ exchange contributes to glutamate-induced intracellular Ca2+ concentration increases in cultured rat forebrain neurons.[J]. Molecular Pharmacology, 1998, 53 4 1: 742-749. DOI:10.1124/mol.53.4.742
[3] J SANTO-DOMINGO. The plasma membrane Na+/Ca2+ exchange inhibitor KB-R7943 is also a potent inhibitor of the mitochondrial Ca2+ uniporter[J]. British Journal of Pharmacology, 2009, 151 5: 647-654. DOI:10.1038/sj.bjp.0707260
[4] TATIANA BRUSTOVETSKY. KB-R7943, an inhibitor of the reverse Na+/Ca2+ exchanger, blocks N-methyl-D-aspartate receptor and inhibits mitochondrial complex I[J]. British Journal of Pharmacology, 2010, 162 1: 255-270. DOI:10.1111/j.1476-5381.2010.01054.x
2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE Preparation Products And Raw materials
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View Lastest Price from 2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE manufacturers
- Product
- 2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE 182004-65-5
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 200kgs
- Release date
- 2020-01-29