MW 427.5 Da, Purity >98%. Potent, selective inhibitor of the reverse mode of the Na+/Ca2+ exchanger (IC50 = ~0.32 μM in guinea pig ventricular cells). Also potent blocker of TRPC channels (IC50 values are 0.46, 0.71 and 1.38 μM at TRPC3, TRPC6 and TRPC5, respectively).
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- PLoS pathogens 16:e10083072020An activator of G protein-coupled receptor and MEK1/2-ERK1/2 signaling inhibits HIV-1 replication by altering viral RNA processing.Applications:Unspecified applicationReactive species:Unspecified reactive speciesRaymond W Wong et. al.PubMed 32069328
- Scientific reports 8:8502018Cardiac glycoside/aglycones inhibit HIV-1 gene expression by a mechanism requiring MEK1/2-ERK1/2 signaling.Applications:Unspecified applicationReactive species:Unspecified reactive speciesRaymond W Wong et. al.PubMed 29339801
- The European journal of neuroscience 46:2108-21202017Chronic pharmacological blockade of the Na /Ca exchanger modulates the growth and development of the Purkinje cell dendritic arbor in mouse cerebellar slice cultures.Applications:Unspecified applicationReactive species:Unspecified reactive speciesPradeep Sherkhane et. al.PubMed 28715135
- Pflugers Archiv : European journal of physiology 469:1287-12992017Na /Ca exchangers and Orai channels jointly refill endoplasmic reticulum (ER) Ca via ER nanojunctions in vascular endothelial cells.Applications:Unspecified applicationReactive species:Unspecified reactive speciesCristiana M L Di Giuro et. al.PubMed 28497275
Key facts
- CAS number
- 182004-65-5
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 427.5 Da
- Molecular formula
- C17H21N3O6S2
- PubChem identifier
- 9823846
- Nature
- Synthetic
Alternative names
FLJ11098, FLJ14863, FSGS2, Htrp 3, Htrp-5, MGC124333, MTRP6, Mtrp3, Receptor activated cation channel TRP3, Short transient receptor potential channel 3, Short transient receptor potential channel 5, Short transient receptor potential channel 6, TRANSIENT RECEPTOR POTENTIAL DROSOPHILA HOMOLOG OF 3, TRP-5, TRP-6, TRP3, TRPC5_HUMAN, TRPC6_HUMAN, TRRP6, Transient receptor potential cation channel subfamily C member 3, Transient receptor potential cation channel subfamily C member 5, Transient receptor potential cation channel subfamily C member 6, Transient receptor potential channel 3, Transient receptor potential channel 5, Transient receptor protein 3, Transient receptor protein 5, Transient receptor protein 6, Trp related protein 3, Trrp3, bZ1P14.9, si:rp71-1p14.9, transient receptor potential cation channel subfamily C member 3 variant c
Recommended products
MW 427.5 Da, Purity >98%. Potent, selective inhibitor of the reverse mode of the Na+/Ca2+ exchanger (IC50 = ~0.32 μM in guinea pig ventricular cells). Also potent blocker of TRPC channels (IC50 values are 0.46, 0.71 and 1.38 μM at TRPC3, TRPC6 and TRPC5, respectively).
Key facts
- CAS number
- 182004-65-5
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 427.5 Da
- Molecular formula
- C17H21N3O6S2
- PubChem identifier
- 9823846
- Nature
- Synthetic
- Solubility
Soluble in DMSO to 100 mM.
- Biochemical name
- 2-[2-[4-(4-Nitrobenzyloxy)phenyl]ethyl]isothiourea mesylate
- Biological description
Potent, selective inhibitor of the reverse mode of the Na+/Ca2+ exchanger (IC50 = ~0.32 μM in guinea pig ventricular cells). Also potent blocker of TRPC channels (IC50 values are 0.46, 0.71 and 1.38 μM at TRPC3, TRPC6 and TRPC5, respectively).
- Canonical SMILES
- CS(=O)(=O)O.C1=CC(=CC=C1CCSC(=N)N)OCC2=CC=C(C=C2)[N+](=O)[O-]
- 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
- IUPAC name
- methanesulfonic acid;2-[4-[(4-nitrophenyl)methoxy]phenyl]ethyl carbamimidothioate
Storage
- Shipped at conditions
- Ambient - Can Ship with Ice
- Appropriate short-term storage conditions
- Ambient
- Appropriate long-term storage conditions
- Ambient
- Storage information
- The product can be stored for up to 12 months
Supplementary info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
TRPC6 TRPC3 and TRPC5 are members of the transient receptor potential (TRP) channel family. These proteins function as non-selective cation channels allowing the passage of calcium ions and other cations such as sodium. TRPC channels often respond to various chemical and mechanical stimuli. TRPC6 TRPC3 and TRPC5 have molecular masses of approximately 106 kDa 97 kDa and 105 kDa respectively. They express widely in tissues such as the brain heart kidneys and to a lesser degree in the vasculature. Each of these proteins forms homo- or heteromeric complexes which modulate their functional diversity.
- Biological function summary
These channels participate in important cellular processes maintaining ion homeostasis and influencing cellular responses. TRPC6 TRPC3 and TRPC5 contribute to receptor-operated calcium entry (ROCE) playing a significant role in the physiological regulation of calcium levels. They form part of multimeric channel complexes with other TRPC subunits influencing vascular smooth muscle contraction and neuronal signaling. These proteins also interact with other channels and cellular components including the NCX (sodium-calcium exchanger) which further delineates their role in cellular calcium handling.
- Pathways
TRPC6 TRPC3 and TRPC5 integrate into the PIP2 pathway and calcium signaling pathways. These channels interact with phospholipase C to generate inositol trisphosphate and diacylglycerol key second messengers that propagate cellular signals. In the context of these pathways TRPC channels associate closely with proteins such as NCX and PLC modulating intracellular calcium dynamics. This interaction is critical for many cellular processes including smooth muscle contraction and neuronal activity.
- Associated diseases and disorders
TRPC channels particularly TRPC6 and TRPC3 are associated with disorders like focal segmental glomerulosclerosis (FSGS) and cardiac hypertrophy. Mutations or dysregulation of TRPC channels can lead to abnormal calcium signaling contributing to the pathophysiology of these conditions. In these disease states TRPC channels interact with key proteins such as podocin in kidney diseases or calcineurin in cardiac hypertrophy influencing cellular outcomes and tissue pathology. Understanding the detailed mechanisms of these interactions helps in developing targeted therapeutic strategies.
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Chemical Structure - KB-R7943, NCX inhibitor (ab120284)
2D chemical structure image of ab120284, KB-R7943, NCX inhibitor
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