Psora 4
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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 334.37 |
| Cas No. | 724709-68-6 |
| Formula | C21H18O4 |
| Solubility | insoluble in H2O; ≥1.72 mg/mL in EtOH with ultrasonic; ≥15.75 mg/mL in DMSO |
| Chemical Name | 4-(4-phenylbutoxy)-7H-furo[3,2-g]chromen-7-one |
| SDF | Download SDF |
| Canonical SMILES | O=C1OC2=C(C=C1)C(OCCCCC3=CC=CC=C3)=C4C(OC=C4)=C2 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
human and rat TEM cells |
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Preparation method |
The solubility of this compound in DMSO is >15.75mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0-1000 nM; 30 min |
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Applications |
Psora-4 preferentially inhibited the proliferation of human and rat TEM cells with EC50 values of 25 and 60 nM, respectively. |
| Animal experiment [2]: | |
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Animal models |
rats with anti-glomerular basement membrane glomerulonephritis (anti-GBM GN) |
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Dosage form |
0.3 ml; dissolved in a mixture of 25% CremophorEL and 75% PBS to prepare a concentration of 9 mg/ml; from day 0 to day 21; intraperitoneal injection |
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Application |
In rats with anti-glomerular basement membrane glomerulonephritis (anti-GBM GN), Psora 4 significantly reduced urinary protein excretion and the increase in kidney weight was significantly smaller than that in the vehicle group. Psora 4 restored creatinine clearances and reduced the proportion of crescentic glomeruli, and the number of ED-1+ macrophages and CD3+ T cells. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [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. [2]. Hyodo T1, Oda T, Kikuchi Y, et al. Voltage-gated potassium channel Kv1.3 blocker as a potential treatment for rat anti-glomerular basement membrane glomerulonephritis. Am J Physiol Renal Physiol. 2010 Dec;299(6):F1258-69. |
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Quality Control & MSDS
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Chemical structure
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