| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
SPS-4251 is a potent KCNA3 (Kv1.3) channel blocker. Kv1.3 is a voltage-gated potassium channel involved in T-cell activation and immune regulation. By blocking Kv1.3 channels, SPS-4251 modulates T-cell function and has potential therapeutic applications in autoimmune diseases such as multiple sclerosis and psoriasis. Its mechanism of action involves inhibition of Kv1.3 channel activity.
|
|---|---|
| ln Vitro |
PAP-1 (2-100 nM; 30 minutes) suppresses CCR7-TEM cell proliferation with an IC50 of 10 nM [1].
In vitro, SPS-4251 is a novel and potent KCNA3 channel blocker. Its activity is characterized by potent inhibition of Kv1.3 voltage-gated potassium channels. SPS-4251 has been studied for its effects on T-cell activation and immune function. It has the potential to be used in the treatment of multiple sclerosis and plaque psoriasis. |
| ln Vivo |
Lewis rats treated intraperitoneally with PAP-1 (0.3–3 mg/kg) three times a day for 48 hours are protected against delayed-type hypersensitivity (DTH) [1].
In vivo, SPS-4251 has been studied in clinical trials for the treatment of plaque psoriasis. It has the potential to be used in the treatment of multiple sclerosis. As a Kv1.3 channel blocker, it modulates T-cell function and immune responses. Its in vivo efficacy is attributed to its ability to inhibit Kv1.3 channels and modulate immune function. SPS-4251 has reached Phase 1 clinical trials for psoriasis. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for SPS-4251 typically involve measuring its inhibition of Kv1.3 potassium channels. The compound is a potent KCNA3 channel blocker. Patch-clamp electrophysiology or flux assays can be used to measure Kv1.3 channel inhibition. These assays confirm its mechanism of action as a Kv1.3 channel blocker.
|
| Cell Assay |
Cell proliferation assay [1]
Cell Types: CCR7-TEM cells (anti-CD3 Ab stimulation) Tested Concentrations: 2, 10, 25, 100 nM Incubation Duration: 30 minutes Experimental Results: Inhibits the proliferation of CCR7-TEM cells, IC50 is 10 nM. In vitro cellular assays for SPS-4251 typically involve treating T-cells with the compound and measuring T-cell activation, proliferation, and cytokine production. As a Kv1.3 channel blocker, SPS-4251 modulates T-cell function. These cell-based studies demonstrate its immunomodulatory effects and its potential for treating autoimmune diseases. |
| Animal Protocol |
Animal/Disease Models: 9 to 11 weeks old female Lewis rats [1] Usage and
Doses: intraperitoneal (ip) injection; 3 times a day for 48 hrs (hrs (hours)). Dosing: 0.3, 1, 3 mg/kg. Experimental Results: Dose-dependent inhibition of DTH response. |
| ADME/Pharmacokinetics |
SPS-4251 has a molecular weight of 350.36 and a molecular formula of C21H18O5. Its CAS number is 870653-45-5. The compound is also known as PAP-1, AS-77, and 5-(4-Phenoxybutoxy)psoralen. It is a psoralen derivative and a potent KCNA3 channel blocker. SPS-4251 has been studied in clinical trials for plaque psoriasis.
|
| Toxicity/Toxicokinetics |
SPS-4251 is a Kv1.3 channel blocker with a well-characterized mechanism of action. As with any ion channel blocker, potential toxicity may include effects on cardiac and neuronal function. The compound's safety profile should be evaluated in preclinical and clinical studies. SPS-4251 is for research use only and is not approved for human therapeutic use. It represents a valuable tool for studying Kv1.3 channel biology and autoimmune diseases.
|
| References |
|
| Additional Infomation |
SPS-4251 (CAS# 870653-45-5), also known as PAP-1 or AS-77, is a novel and potent KCNA3 channel blocker (inhibitor of Kv1.3, voltage-gated K+ channel). It has the potential to be used in the treatment of multiple sclerosis and plaque psoriasis. SPS-4251 has been studied in clinical trials for plaque psoriasis. The compound is for research use only and not for human therapeutic use.
|
| Molecular Formula |
C21H18O5
|
|---|---|
| Molecular Weight |
350.37
|
| Exact Mass |
350.115
|
| CAS # |
870653-45-5
|
| PubChem CID |
11302540
|
| Appearance |
White to yellow solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
555.8±50.0 °C at 760 mmHg
|
| Flash Point |
289.9±30.1 °C
|
| Vapour Pressure |
0.0±1.5 mmHg at 25°C
|
| Index of Refraction |
1.619
|
| LogP |
4.56
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
26
|
| Complexity |
499
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
KINMYBBFQRSVLL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C21H18O5/c22-20-9-8-16-19(26-20)14-18-17(10-13-24-18)21(16)25-12-5-4-11-23-15-6-2-1-3-7-15/h1-3,6-10,13-14H,4-5,11-12H2
|
| Chemical Name |
4-(4-phenoxybutoxy)furo[3,2-g]chromen-7-one
|
| Synonyms |
SPS4251 SPS 4251 SPS-4251PAP-1SPS42515-(4-Phenoxybutoxy)psoralen
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~142.71 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.14 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (7.14 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.14 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8541 mL | 14.2706 mL | 28.5413 mL | |
| 5 mM | 0.5708 mL | 2.8541 mL | 5.7083 mL | |
| 10 mM | 0.2854 mL | 1.4271 mL | 2.8541 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
