 |
- Technische Daten
- Im Angebot als 5 mg (sc-253325)
- CAS Nummer: 724709-68-6
- Molekulargewicht: 334.37
- Summenformel: C21H18O4
- Reinheit: ≥98%
- Produktform: Solid
- Physisches Aussehen: off-white solid
- Löslichkeit: Soluble in DMSO: ~16 mg/mL: water: insoluble
- SMILES: C1=CC=C(C=C1)CCCCOC2=C3C=CC(=O)OC3=CC4=C2C=CO4
- Beschreibung
- The lymphocyte potassium channel Kv1.3 is a new target for immunosuppression. This is the most potent small-molecule Kv1.3 blocker known. It blocked Kv1.3 in a use-dependent manner, with a Hill coefficient of 2 and an EC50value of 3 nM, by preferentially binding to the C-type inactivated state of the channel. It exhibited 17- to 70-fold selectivity for Kv1.3 over closely related Kv1-family channels (Kv1.1, Kv1.2, Kv1.4, and Kv1.7) with the exception of Kv1.5 (EC50, 7.7 nM) and showed no effect on human ether-a-go-go-related channel, Kv3.1, the calcium-activated K+ channels (IKCa1, SK1-SK3, and BKCa), or the neuronal NaV1.2 channel. In a test of in vivo toxicity in rats, Psora-4 did not display any signs of acute toxicity after five daily subcutaneous injections at 33 mg/kg body weight. Psora-4 selectively suppressed the proliferation of human and rat myelin-specific effector memory T cells with EC50 values of 25 and 60 nM, respectively, without persistently suppressing peripheral blood naive and central memory T cells. Because autoantigen-specific effector memory T cells contribute to the pathogenesis of T cell-mediated autoimmune diseases such as multiple sclerosis, Psora-4 and other Kv1.3 blockers may be useful as immunomodulators for the therapy of autoimmune disorder.
- LAGERUNG:
- Ausschließlich für Forschungszwecke (in-vitro, laboratory research use only)
- Weitere Referenznummern
- Literaturhinweise
- Vennekamp, J., et al., Kv1.3-blocking 5-Phenylalkoxypsoralens: a new class of immunomodulators. Mol. Pharmacol. 65, 1364-1374, (2004)
Chandy, K.G., et al., K+ channels as targets for specific immunomodulation. Trends Pharmacol. Sci. 25, 280-289, (2004)
|
|
| |
|
|
|
Psora-4
Klicken Sie auf das Bild um es zu vergrößern.
|
|
|
Download
|
|
