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Purity: ≥98%
| Targets |
The primary targets of DSP-2230 are the voltage-gated sodium channels Nav1.7 and Nav1.8. These channels are critical for the initiation and propagation of action potentials in neurons. Nav1.7 is predominantly expressed in dorsal root ganglion (DRG) neurons and sympathetic ganglia, where it functions as a threshold channel, amplifying small depolarizations to trigger action potentials. Gain-of-function mutations in Nav1.7 cause inherited pain syndromes like erythromelalgia and paroxysmal extreme pain disorder, while loss-of-function mutations lead to congenital insensitivity to pain, validating it as a key pain target. Nav1.8 is a TTX-resistant channel also expressed in DRG neurons, where it contributes to the upstroke of the action potential. By selectively blocking both channels, DSP-2230 effectively reduces the excitability of pain-sensing neurons.
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| ln Vitro |
DSP-2230 is a potent and selective blocker of Nav1.7 and Nav1.8 channels. Its activity is typically characterized using electrophysiological techniques, such as patch-clamp recording, on cells expressing the recombinant channels. In these assays, the ability of DSP-2230 to inhibit the sodium current through the channels is measured. Its selectivity for Nav1.7 and Nav1.8 over other sodium channel subtypes (Nav1.1, Nav1.2, Nav1.3, Nav1.4, Nav1.5, Nav1.6, Nav1.9) is a key feature, as it would minimize off-target effects on muscle, cardiac, or central nervous system function. This selectivity profile is crucial for the development of a safe and effective pain therapeutic.
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| ln Vivo |
Specific in vivo data for DSP-2230 is not detailed in the provided search results. However, as a selective blocker of Nav1.7 and Nav1.8, it is expected to exhibit potent analgesic effects in animal models of pain. In vivo, blocking these channels would reduce the excitability of nociceptors, leading to a decrease in pain perception. The compound is being developed for the treatment of pain resulting from nerve damage or dysfunction, indicating that it has been evaluated in models of neuropathic pain.
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| Enzyme Assay |
The in vitro assay for DSP-2230 is typically an electrophysiological assay using the patch-clamp technique. Chinese hamster ovary (CHO) or human embryonic kidney (HEK) cells are transfected with cDNA encoding the Nav1.7 or Nav1.8 channel. In the whole-cell patch-clamp configuration, the cell is held at a negative membrane potential (e.g., -100 mV), and a voltage step is applied to activate the sodium channel, eliciting a transient inward current. DSP-2230 is applied to the cell, and its effect on the sodium current amplitude is measured. The percent inhibition of the current is plotted against the compound concentration to determine its potency. This is a highly sensitive and direct method for assessing the activity of sodium channel blockers.
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| Cell Assay |
In vitro cell-based assays for DSP-2230 are the same as the electrophysiological assays described above, as the functional readout is the inhibition of the sodium current. There are no standard cell viability assays for this type of compound, as its activity is defined by its effect on ion channel function. Therefore, the primary cell-based assay for DSP-2230 is patch-clamp recording from cells expressing the target channels.
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| Animal Protocol |
DSP-2230 is a selective Nav1.7/Nav1.8 blocker that is being developed for the treatment of pain. In vivo, DSP-2230 would be administered to animal models of pain, such as the chronic constriction injury (CCI) model of neuropathic pain or the formalin test. In these models, the compound's ability to reduce pain-related behaviors (e.g., mechanical allodynia, thermal hyperalgesia) would be assessed. These studies are crucial for demonstrating its in vivo efficacy and for translating the in vitro findings into a meaningful therapeutic context.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for DSP-2230 is not provided in the search results. Its molecular weight is 419.40. As a small molecule, it is likely to be orally bioavailable, which is a key requirement for a chronic pain therapeutic.
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| Toxicity/Toxicokinetics |
Specific toxicity data for DSP-2230 is not publicly available. As a sodium channel blocker, its selectivity for Nav1.7 and Nav1.8 over other sodium channel isoforms is critical for its safety. Inhibition of Nav1.5, the cardiac sodium channel, could cause cardiac arrhythmias, while inhibition of Nav1.4 could cause muscle weakness. Its development would require extensive toxicology studies. It is classified as a research tool and is not intended for human use.
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| References | |
| Additional Infomation |
DSP-2230 is a research compound being developed as a selective inhibitor of the Nav1.7 and Nav1.8 sodium channels for the treatment of pain. These channels are well-validated targets for analgesia. The compound has not received FDA approval and is currently in the preclinical research stage.
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| Molecular Formula |
C20H20F3N5O2
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|---|---|
| Molecular Weight |
419.400314331055
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| Exact Mass |
419.156
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| CAS # |
1233231-30-5
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| PubChem CID |
129080919
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| Appearance |
White to off-white solid powder
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| LogP |
2.4
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
601
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| Defined Atom Stereocenter Count |
1
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| SMILES |
FC1C(=C(C=C(C=1)OC1C=CC2=C(N=1)N(C(CN[C@H](C(N)=O)C)=N2)C1CCC1)F)F
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| InChi Key |
HHXCJIMPEJSJTG-JTQLQIEISA-N
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| InChi Code |
InChI=1S/C20H20F3N5O2/c1-10(19(24)29)25-9-16-26-15-5-6-17(27-20(15)28(16)11-3-2-4-11)30-12-7-13(21)18(23)14(22)8-12/h5-8,10-11,25H,2-4,9H2,1H3,(H2,24,29)/t10-/m0/s1
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| Chemical Name |
(2S)-2-[[3-cyclobutyl-5-(3,4,5-trifluorophenoxy)imidazo[4,5-b]pyridin-2-yl]methylamino]propanamide
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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 : ~125 mg/mL (~298.04 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.25 mg/mL (5.36 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 22.5 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: ≥ 2.25 mg/mL (5.36 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 22.5 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: ≥ 2.25 mg/mL (5.36 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 | 2.3844 mL | 11.9218 mL | 23.8436 mL | |
| 5 mM | 0.4769 mL | 2.3844 mL | 4.7687 mL | |
| 10 mM | 0.2384 mL | 1.1922 mL | 2.3844 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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