| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Targets |
The primary target of JT010 is TRPA1 (transient receptor potential ankyrin 1), a non-selective cation channel expressed in sensory neurons and involved in pain perception, neurogenic inflammation, and itch. TRPA1 is activated by various endogenous and exogenous irritants, including allyl isothiocyanate (mustard oil), cinnamaldehyde, and reactive oxygen species. JT010 acts as a potent and selective TRPA1 channel activator by covalently and site-selectively binding to Cys621 in the channel's N-terminal ankyrin repeat domain. This covalent modification opens the channel, allowing calcium influx and neuronal excitation.
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| ln Vitro |
In vitro, JT010 activates the TRPA1 channel with an EC₅₀ of 0.65 nM. It stimulates calcium influx in TRPA1-transfected HEK293 cells in a dose-dependent manner with an EC₅₀ of 650 pM. The compound shows excellent selectivity over TRPV1, TRPV3, TRPV4, TRPM2, TRPM8, and TRPC5 channels, with EC₅₀ values >1 μM. JT010 is a non-cytotoxic and highly stable compound, with >90% remaining after 2 hours in 1 mM DTT or 2-mercaptoethanol. Its covalent binding mechanism provides sustained channel activation.
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| ln Vivo |
In vivo, JT010 has been investigated for its potential to reduce tumor growth and enhance the effectiveness of other cancer therapies, as it inhibits PI3Kδ. The drug is currently undergoing preclinical and early-stage clinical trials for its safety and therapeutic potential. As a TRPA1 agonist, it would be expected to induce pain and neurogenic inflammation in vivo, making it a valuable tool for studying pain mechanisms.
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| Enzyme Assay |
For TRPA1 agonists, standard cell-free assays involve measuring channel activity using electrophysiological techniques (patch-clamp) or fluorescent membrane potential assays using membrane preparations from cells expressing recombinant TRPA1. The compound is applied at various concentrations, and channel activation is measured by ion flux or changes in membrane potential to determine EC₅₀ values. Covalent binding to Cys621 can be confirmed by mass spectrometry or mutagenesis studies.
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| Cell Assay |
For TRPA1 agonists, standard cellular assays involve the use of cell lines expressing recombinant human TRPA1 (e.g., HEK293-TRPA1). Cells are loaded with calcium-sensitive fluorescent dyes (e.g., Fluo-4, Fura-2), and calcium influx following compound addition is measured by fluorimetry or imaging. EC₅₀ values are determined from concentration-response curves. Selectivity is assessed using cells expressing related TRP channels (TRPV1, TRPV3, TRPV4, TRPM2, TRPM8, TRPC5).
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| Animal Protocol |
For in vivo evaluation of TRPA1 agonists, standard animal models include pain models such as the formalin test, acetic acid writhing test, or models of neuropathic and inflammatory pain. The compound is typically administered intradermally, intraperitoneally, or orally, and pain-related behaviors (flinching, licking, paw withdrawal) are measured. For anticancer applications, tumor xenograft models in mice are used. JT010 is undergoing preclinical and early-stage clinical trials.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for JT010 is not extensively provided in the available sources. The compound has a molecular weight of 335.16 and formula C₁₆H₁₉ClN₂O₃S. It is soluble in DMSO and should be stored at 0-4°C for short term. JT010 is a highly stable compound (>90% remains after 2 hours in reducing agents). As a small molecule with moderate lipophilicity, it would be expected to have reasonable cell permeability. Comprehensive PK studies would be required for therapeutic development.
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| Toxicity/Toxicokinetics |
Detailed toxicology data for JT010 is not provided in the available sources. JT010 is described as non-cytotoxic. As a research compound, standard preclinical toxicology would be required for therapeutic development. The compound's covalent binding mechanism raises potential concerns about off-target reactivity, though its selectivity for TRPA1 Cys621 suggests a manageable safety profile. The compound is for research use only and not for therapeutic applications.
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| References | |
| Additional Infomation |
JT010 is a potent, site-selective, and covalent TRPA1 agonist with an EC₅₀ of 0.65 nM. It activates the TRPA1 channel by covalently and site-selectively binding to Cys621. The compound is a non-cytotoxic and highly stable chloroacetamido warhead-carrying thiazole derivative. It has the molecular formula C₁₆H₁₉ClN₂O₃S. JT010 is undergoing preclinical and early-stage clinical trials.
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| Molecular Formula |
C16H19CLN2O3S
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|---|---|
| Molecular Weight |
354.851661920547
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| Exact Mass |
354.08
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| CAS # |
917562-33-5
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| PubChem CID |
18524489
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.1
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
23
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| Complexity |
367
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(CCl)N(CCCOC)C1SC=C(C2C=CC(OC)=CC=2)N=1
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| InChi Key |
KZMAWJRXKGLWGS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H19ClN2O3S/c1-21-9-3-8-19(15(20)10-17)16-18-14(11-23-16)12-4-6-13(22-2)7-5-12/h4-7,11H,3,8-10H2,1-2H3
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| Chemical Name |
2-chloro-N-[4-(4-methoxyphenyl)-1,3-thiazol-2-yl]-N-(3-methoxypropyl)acetamide
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| Synonyms |
JT 010; JT-010; JT010
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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 : ~100 mg/mL (~281.81 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.05 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 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.05 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 | 2.8181 mL | 14.0905 mL | 28.1809 mL | |
| 5 mM | 0.5636 mL | 2.8181 mL | 5.6362 mL | |
| 10 mM | 0.2818 mL | 1.4090 mL | 2.8181 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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