| Size | Price | Stock | Qty |
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| Targets |
The primary target of JZP-430 is α/β-hydrolase domain 6 (ABHD6), a serine hydrolase that hydrolyzes the endocannabinoid 2-arachidonoylglycerol (2-AG) and other monoacylglycerols. ABHD6 is one of the major enzymes responsible for 2-AG hydrolysis in the brain, along with MAGL. By inhibiting ABHD6, JZP-430 increases 2-AG levels and modulates endocannabinoid signaling. JZP-430 is a highly selective, irreversible inhibitor of ABHD6 with an IC₅₀ of 44 nM. It shows 230-fold selectivity over FAAH and LAL, making it a highly specific tool for studying ABHD6 function.
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| ln Vitro |
In vitro, JZP-430 inhibits ABHD6 with an IC₅₀ of 44 nM. It exhibits approximately 230-fold selectivity over FAAH and LAL. As an irreversible inhibitor, it covalently modifies the active site serine of ABHD6, providing sustained target inhibition. The compound's high potency and selectivity make it a valuable tool for studying ABHD6 function in endocannabinoid metabolism and lipid signaling.
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| ln Vivo |
In vivo, JZP-430 is used to study the role of ABHD6 in endocannabinoid metabolism, lipid signaling, and metabolic disorders. By irreversibly inhibiting ABHD6, the compound would be expected to increase 2-AG levels and modulate endocannabinoid signaling in vivo. However, specific in vivo efficacy data from animal models is not detailed in the available sources. The compound's selectivity for ABHD6 suggests a favorable specificity profile.
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| Enzyme Assay |
For ABHD6 inhibitors, standard cell-free assays involve measuring the hydrolytic activity of recombinant ABHD6 using a fluorogenic substrate (e.g., arachidonoyl-AMC or 4-methylumbelliferyl butyrate). The compound is incubated with the enzyme and substrate, and the release of fluorescent product is measured to determine IC₅₀ values. Selectivity for ABHD6 over FAAH and LAL is assessed using enzyme assays for these targets.
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| Cell Assay |
For ABHD6 inhibitors, standard cellular assays involve treatment of cells (e.g., neuroblastoma cells, primary neurons, or adipocytes) with the test compound for 1-4 hours. 2-AG levels in cell lysates are measured by LC-MS. ABHD6 activity is assessed by measuring the hydrolysis of a fluorogenic substrate in cell lysates. Effects on downstream signaling (e.g., cannabinoid receptor activation, insulin signaling) are also measured.
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| Animal Protocol |
For in vivo evaluation of ABHD6 inhibitors, standard animal models include models of metabolic disorders (obesity, diabetes), pain, and neuroinflammation. The compound is typically administered orally or intraperitoneally, and metabolic, behavioral, and biochemical endpoints are assessed.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for JZP-430 is not extensively provided in the available sources. The compound has a molecular weight of 354.47 and formula C₁₆H₂₆N₄O₃S. It is a solid and can be transported at room temperature. As a small molecule with moderate lipophilicity, it would be expected to have reasonable cell permeability and oral bioavailability. Comprehensive PK studies would be required for therapeutic development.
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| Toxicity/Toxicokinetics |
Detailed toxicology data for JZP-430 is not provided in the available sources. As a research compound targeting ABHD6, standard preclinical toxicology would be required for therapeutic development. The compound's selectivity for ABHD6 over FAAH and LAL suggests a favorable specificity profile. However, irreversible inhibition may have long-term effects that would need to be evaluated. The compound is for research use only and not for therapeutic applications.
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| References | |
| Additional Infomation |
α/β-hydrolase domain 6 (ABHD6) inhibitor; structure can be found in the first article.
JZP-430 is a potent, highly selective, and irreversible inhibitor of ABHD6 with an IC₅₀ of 44 nM. It exhibits approximately 230-fold selectivity over FAAH and LAL. The compound has the molecular formula C₁₆H₂₆N₄O₃S and a molecular weight of 354.47. No regulatory approval has been identified. |
| Molecular Formula |
C16H26N4O3S
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|---|---|
| Molecular Weight |
354.467642307281
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| Exact Mass |
354.172
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| CAS # |
1672691-74-5
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| PubChem CID |
121513897
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| Appearance |
White to light yellow solid powder
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| LogP |
3.4
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
401
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1N=C(C(=N1)N1CCOCC1)OC(N(C)C1CCCCCCC1)=O
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| InChi Key |
WKSHMJCYWFOADB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H26N4O3S/c1-19(13-7-5-3-2-4-6-8-13)16(21)23-15-14(17-24-18-15)20-9-11-22-12-10-20/h13H,2-12H2,1H3
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| Chemical Name |
(4-morpholin-4-yl-1,2,5-thiadiazol-3-yl) N-cyclooctyl-N-methylcarbamate
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| Synonyms |
JZP430; JZP 430; JZP-430
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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 (~282.11 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 | 2.8211 mL | 14.1056 mL | 28.2111 mL | |
| 5 mM | 0.5642 mL | 2.8211 mL | 5.6422 mL | |
| 10 mM | 0.2821 mL | 1.4106 mL | 2.8211 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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