| Size | Price | Stock | Qty |
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| Targets |
HN-37 targets KCNQ2 (Kv7.2), a voltage-gated potassium channel that plays a critical role in regulating neuronal excitability. KCNQ2 channels are responsible for the M-current, a slowly activating and non-inactivating potassium current that stabilizes the resting membrane potential and limits repetitive neuronal firing. By activating KCNQ2 channels, HN-37 enhances M-current activity, reducing neuronal hyperexcitability and providing anticonvulsant effects.
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| ln Vitro |
Similar to RTG in terms of isoform selectivity, HN37 is a strong neuronal Kv7 activator [1].
HN-37 is a potent neuronal Kv7 activator with an EC50 of 37 nM for KCNQ2. It exhibits subtype selectivity similar to RTG, a known Kv7 activator. As a potent and chemically stable antiepileptic agent candidate, HN-37 reduces neuronal hyperexcitability by enhancing M-current activity through KCNQ2 activation. The compound's alkyne group enables click chemistry applications for bioconjugation and labeling studies. |
| ln Vivo |
In vivo activity data for HN-37 are not extensively detailed, but the compound is being developed as an antiepileptic agent candidate. As a KCNQ2 activator, it is expected to exhibit anticonvulsant activity in animal models of epilepsy by reducing neuronal hyperexcitability. The compound's potency (EC50 = 37 nM) and chemical stability suggest potential for in vivo efficacy. Specific dosing regimens and efficacy data would be determined from preclinical studies. The compound is intended for research use.
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| Enzyme Assay |
The in vitro electrophysiology assay for HN-37 typically involves measuring its effects on KCNQ2 channel activity using patch-clamp techniques. KCNQ2 channels are expressed in Xenopus oocytes or mammalian cell lines. Varying concentrations of HN-37 (typically 0.001-100 μM) are applied to the cells, and the M-current is measured. The EC50 value is determined by plotting the percentage of current enhancement against compound concentration. The compound is dissolved in DMSO and diluted in recording buffer.
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| Cell Assay |
In vitro cellular assays for HN-37 typically involve treating neuronal cell lines or primary neurons with the compound at concentrations ranging from 0.001 to 10 μM. Neuronal excitability is assessed by measuring action potential firing using patch-clamp or multi-electrode array recordings. Cell viability is assessed using MTT or other standard assays. The compound is dissolved in DMSO as a stock solution and diluted in cell culture medium. The compound's effects on M-current enhancement are assessed by electrophysiological recordings.
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| Animal Protocol |
In vivo animal studies for HN-37 would typically involve administration to mice or rats via oral gavage or intraperitoneal injection at doses determined from preliminary studies. Anticonvulsant activity is assessed using models such as maximal electroshock seizure (MES) or pentylenetetrazol (PTZ)-induced seizure models. The compound's effects on seizure threshold, seizure severity, and mortality are evaluated. Blood and brain tissue samples are collected for pharmacokinetic analysis. The compound is formulated in appropriate vehicles for administration.
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| ADME/Pharmacokinetics |
HN-37 has a molecular weight of 340.39 g/mol and formula C20H21FN2O2. Recommended storage is powder at -20°C for 3 years and at 4°C for 2 years; in solvent at -80°C for 6 months and at -20°C for 1 month. The compound has a purity of ≥99%. Detailed PK parameters such as half-life, Cmax, AUC, and bioavailability would require experimental determination. As a KCNQ2 activator, the compound is expected to penetrate the blood-brain barrier.
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| Toxicity/Toxicokinetics |
Toxicity data for HN-37 are not extensively reported. The compound is intended for research use only and is not approved for human therapeutic applications. Standard preclinical toxicity assessments would include acute toxicity studies in rodents, repeated-dose toxicity studies, and assessment of off-target effects. As a KCNQ2 activator, the compound may affect normal neuronal function at high doses. Appropriate safety precautions should be taken when handling.
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| References | |
| Additional Infomation |
HN-37 (CAS 1821222-10-9) is a potent and chemically stable antiepileptic agent candidate with a molecular weight of 340.39 g/mol and formula C20H21FN2O2. It activates KCNQ2 (Kv7.2) channels with an EC50 of 37 nM. The compound exhibits subtype selectivity similar to RTG and contains an alkyne group for click chemistry applications. HN-37 is being developed as a potential therapeutic for epilepsy. It is also known as HN37 and is not approved for clinical use.
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| Molecular Formula |
C20H21FN2O2
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|---|---|
| Molecular Weight |
340.39
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| Exact Mass |
340.158
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| CAS # |
1821222-10-9
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| PubChem CID |
92045023
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
25
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| Complexity |
469
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=C(C=C(C(NC(OC)=O)=C1C)C)N(CC#C)CC1C=CC(F)=CC=1
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| InChi Key |
HXUBJZRAVCPBRH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H21FN2O2/c1-5-10-23(13-16-6-8-17(21)9-7-16)18-11-14(2)19(15(3)12-18)22-20(24)25-4/h1,6-9,11-12H,10,13H2,2-4H3,(H,22,24)
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| Chemical Name |
methyl N-[4-[(4-fluorophenyl)methyl-prop-2-ynylamino]-2,6-dimethylphenyl]carbamate
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~146.89 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9378 mL | 14.6890 mL | 29.3781 mL | |
| 5 mM | 0.5876 mL | 2.9378 mL | 5.8756 mL | |
| 10 mM | 0.2938 mL | 1.4689 mL | 2.9378 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.
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