Psora 4 (Synonyms: 5-(4-Phenylbutoxy)psoralen) |
| Catalog No.GC16502 |
Psora 4는 EC50이 3nM인 Kv1.3(전압 개폐 칼륨 채널)의 강력하고 선택적인 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 724709-68-6
Sample solution is provided at 25 µL, 10mM.
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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.
| 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. |
|
Reacting condition |
0-1000 nM; 30 min |
|
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]: | |
|
Animal models |
rats with anti-glomerular basement membrane glomerulonephritis (anti-GBM GN) |
|
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 |
|
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. |
|
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. |
|
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. | |
| Cas No. | 724709-68-6 | SDF | |
| Synonyms | 5-(4-Phenylbutoxy)psoralen | ||
| Chemical Name | 4-(4-phenylbutoxy)-7H-furo[3,2-g]chromen-7-one | ||
| Canonical SMILES | O=C1OC2=C(C=C1)C(OCCCCC3=CC=CC=C3)=C4C(OC=C4)=C2 | ||
| Formula | C21H18O4 | M.Wt | 334.37 |
| Solubility | ≥ 15.75mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.9907 mL | 14.9535 mL | 29.907 mL |
| 5 mM | 0.5981 mL | 2.9907 mL | 5.9814 mL |
| 10 mM | 0.2991 mL | 1.4953 mL | 2.9907 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)
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