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Structure of 125-65-5
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A cell permeable hydroxytricyclic derivative that acts as a specific and reversible inhibitor of transient receptor potential melastatin 4 (TRPM4) (IC50 = 20 M in HEK293 cells). Does not affect TRPM5 and cystic fibrosis transmembrane conductance regulators (CFTR) channels. Decreases the occurrence of early after depolarizations (EAD) and exhibits an anti-arrhythmic effect that is independent of the action of protein kinase A. Shown to abolish NMDA-induced burst firing in dopaminergic neurons. Does not affect K+ currents at ~10 M, but at higher concentration (~100 M) it reversibly reduces K+ currents.
Pleuromutilin serves as a privileged scaffold in medicinal chemistry, offering a rigid tetracyclic core with defined stereochemistry that enables selective functionalization at C14 and C2 positions. Its structural stability and low metabolic liability make it a valuable building block for antibacterial and antiviral lead optimization. The molecule facilitates direct derivatization via nucleophilic substitution or transition-metal-catalyzed coupling, supporting efficient synthesis of complex analogs with enhanced pharmacokinetic profiles.
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GHS Pictogram :
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GHS No : GHS07,GHS09
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Signal Word : Warning
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UN#: 3077
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Class : 9
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Packing Group : Ⅲ
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Hazard Statements : H302-H410
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Precautionary Statements : P264-P270-P273-P330-P391-P501
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Lot numbers can be found on the outside label of a product: