Psora 4
(Synonyms: 5-(4-Phenylbutoxy)psoralen) 目录号 : GC16502
An inhibitor of Kv1.3 channels
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. |
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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. | |
| Cas No. | 724709-68-6 | SDF | |
| 别名 | 5-(4-Phenylbutoxy)psoralen | ||
| 化学名 | 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 | ||
| 分子式 | C21H18O4 | 分子量 | 334.37 |
| 溶解度 | ≥ 15.75mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet