research use only
Cat.No.S5028
| Related Targets | CFTR CRM1 CD markers AChR Calcium Channel Sodium Channel GABA Receptor TRP Channel ATPase GluR |
|---|---|
| Other Potassium Channel Inhibitors | Nicorandil TRAM-34 Hydralazine HCl Nigericin Sophocarpine ML133 HCl Gliquidone PAP-1 E-4031 dihydrochloride Ajmaline |
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In vitro |
DMSO
: 18 mg/mL
(191.26 mM)
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In vivo |
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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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.
| Molecular Weight | 94.11 | Formula | C5H6N2 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 504-24-5 | -- | Storage of Stock Solutions |
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| Synonyms | Fampridine, Dalfampridine | Smiles | C1=CN=CC=C1N | ||
| Targets/IC50/Ki |
Kv1.4
13 μM
Kv3.1
29 μM
Kv3.2
100 μM
Kv1.3
195 μM
Kv1.1
290 μM
Kv1.2
590 μM
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| In vitro |
Working from the intracellular side of the channel, 4-AP inhibits a wide variety of voltage-dependent K+ channels with affinities ranging from the mid-micromolar to the millimolar range.
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References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06333171 | Not yet recruiting | Wounds|Wound of Skin|Wound Heal|Wounds and Injuries |
John Elfar|University of Arizona |
July 2024 | Phase 2 |
| NCT05338450 | Recruiting | Multiple Sclerosis|Internuclear Ophthalmoplegia |
Amsterdam UMC location VUmc |
August 30 2022 | Phase 3 |
| NCT02868567 | Active not recruiting | Motor Neuron Disease Upper |
Hospital for Special Surgery New York |
March 2016 | Phase 1 |
| NCT02422940 | Terminated | Post-ischemic Stroke |
Acorda Therapeutics |
April 2015 | Phase 3 |
| NCT02208882 | Completed | Healthy Adult Volunteers |
Bristol-Myers Squibb |
August 2014 | Phase 1 |
| NCT02208050 | Completed | Secondary Progressive Multiple Sclerosis|Primary Progressive Multiple Sclerosis |
University College Dublin |
February 21 2014 | Phase 4 |
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