Name: Psora 4
Price: 384.00 USD

- Overview
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    Background
    
    EC50: 3 nM
    Psora 4 is a Kv1.3 blocker.
    The voltage-gated Kv1.3 channel and the Ca2+-activated IKCa1 channel has been reported to promote and sustain Ca2+ signaling in human T cells via providing the driving force for Ca2+ entry through voltage-independent Ca2+ channels. Selective blockade of Kv1.3 and/or IKCa1 leads to membrane depolarization, reduced Ca2+ entry, as well as diminished cytokine proliferation and production.
    In vitro: Psora-4 could block Kv1.3 in a dose-dependent manner. Psora-4 was found to be the most potent small-molecule Kv1.3 blocker known. Psora-4 exhibited 17- to 70-fold selectivity for Kv1.3 over Kv1-family channels including Kv1.1, Kv1.2, Kv1.4, and Kv1.7 and also showed no effect on human ether-a-go-go-related channel, Kv3.1, or the neuronal NaV1.2 channel. In addition, Psora-4 could suppress the proliferation of rat and human myelin-specific effector memory T cells with EC50 values of 60 and 25 nM, respectively, without persistently suppressing the peripheral blood naive and central memory T cells [1].
    In vivo: In a study of in vivo toxicity in rats, Psora-4 was found not to show any signs of acute toxicity following five daily subcutaneous injections at 33 mg/kg body weight [1].
    Clinical trial: N/A
    
    Reference:[1] Vennekamp J,Wulff H,Beeton C,Calabresi PA,Grissmer S,Hnsel W,Chandy KG. Kv1.3-blocking 5-phenylalkoxypsoralens: a new class of immunomodulators. Mol Pharmacol.2004 Jun;65(6):1364-74.
- Properties
  - Categories
    
    Kv1.3 blocker
    
    Alternative Name
    
    4-(4-phenylbutoxy)-7H-furo[3,2-g]chromen-7-one
    
    CAS Number
    
    724709-68-6
    
    Molecular Formula
    
    C21H18O4
    
    Molecular Weight
    
    334.37
    
    Appearance
    
    A solid
    
    Purity
    
    99.53%
    
    Solubility
    
    insoluble in H2O; ≥1.72 mg/mL in EtOH with ultrasonic; ≥15.75 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    O=C1OC2=C(C=C1)C(OCCCCC3=CC=CC=C3)=C4C(OC=C4)=C2
    
    * For Research Use Only
- Reference
  - 1.Admasu TD, Chaithanya Batchu K, et al. "Drug Synergy Slows Aging and Improves Healthspan through IGF and SREBP Lipid Signaling." Dev Cell. 2018 Oct 8;47(1):67-79.e5. PMID:30269951