| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
0.50 μM (AIG1) and 0.57 μM (FAHFA) in HEK293T cells [1]
JJH260 selectively targets Androgen-induced Gene 1 (AIG1), also known as ADTRP. AIG1 is a serine hydrolase that regulates the hydrolysis of fatty acid esters of hydroxy fatty acids (FAHFAs) and other endogenous lipids, making it a key regulator of metabolic and inflammatory pathways. |
|---|---|
| ln Vitro |
In HEK293T cells, JJH260 (30 min) inhibits the hydrolytic activity of 9-PAHSA, FP-Rh-labeled hAIG1, and ADTRP with IC50 values of 8.5, 0.5, and 0.57 μM, respectively [1]. FAHFA hydrolysis in LNCaP cells and human T cells is inhibited by JJH260 (5 μM, 4 h) [1].
In HEK293T cells, JJH260 suppresses the fluorophosphonate reactivity and FAHFA hydrolytic activity of AIG1 with IC50 values of 0.50 microM and 0.57 microM, respectively. It also inhibits the hydrolytic activity of 9-PAHSA and ADTRP with IC50 values of 8.5 microM and 0.57 microM. |
| ln Vivo |
JJH260 inhibits FAHFA hydrolysis in LNCaP cells and human T cells at a concentration of 5 microM (incubated for 4 hours). This inhibition modulates the levels of bioactive FAHFAs, which are lipids with anti-diabetic and anti-inflammatory properties, thereby affecting downstream signaling pathways involved in metabolism and inflammation.
|
| Enzyme Assay |
Cell-free inhibition assays for AIG1 are performed using a fluorophosphonate-rhodamine (FP-Rh) probe. The probe reacts with active serine hydrolases in cell lysates or purified enzyme preparations. JJH260 is pre-incubated with the enzyme source for 30 minutes, followed by FP-Rh labeling. The reaction is stopped, and the proteins are separated by SDS-PAGE. The IC50 is determined by quantifying the decrease in fluorescence intensity of the labeled AIG1 band.
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| Cell Assay |
Human embryonic kidney 293T (HEK293T) cells overexpressing AIG1 are lysed and the lysates are pre-incubated with varying concentrations of JJH260 for 30 minutes. Substrate (e.g., 9-PAHSA) is then added to initiate the hydrolysis reaction. After incubation, the reaction is stopped and the remaining substrate or the product (hydroxy fatty acid) is extracted. Quantification is performed using liquid chromatography-tandem mass spectrometry (LC-MS/MS) to calculate the IC50 for inhibition of FAHFA hydrolysis.
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| Animal Protocol |
JJH260 is currently used primarily as an in vitro tool compound. While in vivo animal studies have not been extensively reported, the compound's potent activity in cell lysates and intact cells positions it as a valuable probe for future studies in mouse models of metabolism, inflammation, or cancer, where AIG1 activity may play a role.
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| ADME/Pharmacokinetics |
The pharmacokinetic (PK) profile of JJH260 is under investigation as it transitions from a purely in vitro tool to a potential in vivo probe. Early solubility and stability data suggest it is suitable for formulation. Future studies will focus on determining its bioavailability, half-life, and tissue distribution to enable in vivo pharmacology studies.
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| Toxicity/Toxicokinetics |
JJH260 is a research-grade compound with a favorable in vitro safety profile, showing no significant cytotoxicity at concentrations effectively inhibiting AIG1. As with all chemical probes, standard precautions should be taken during handling. Comprehensive toxicological evaluations are typically not required for compounds intended for in vitro use.
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| References |
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| Additional Infomation |
JJH260 is an advanced chemical probe targeting the poorly characterized enzyme AIG1. It is a key tool for understanding the role of AIG1 in FAHFA metabolism and its broader implications in metabolic diseases (e.g., type 2 diabetes, insulin resistance) and T-cell signaling. It is intended for research use only, not for human consumption.
|
| Molecular Formula |
C29H34CLN5O5
|
|---|---|
| Molecular Weight |
568.06
|
| Exact Mass |
567.224
|
| CAS # |
1831135-30-8
|
| PubChem CID |
71710928
|
| Appearance |
Off-white to light yellow solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
703.9±70.0 °C at 760 mmHg
|
| Flash Point |
379.5±35.7 °C
|
| Vapour Pressure |
0.0±2.2 mmHg at 25°C
|
| Index of Refraction |
1.662
|
| LogP |
2.99
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
40
|
| Complexity |
941
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN(C)C1=CC=C(C=C1)C(=O)N2CCN3C(C2)C(=O)N(C3=O)OC(=O)N4CCC(CC4)CCC5=CC=C(C=C5)Cl
|
| InChi Key |
RISSJZZMOJQTIN-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C29H34ClN5O5/c1-31(2)24-11-7-22(8-12-24)26(36)33-17-18-34-25(19-33)27(37)35(28(34)38)40-29(39)32-15-13-21(14-16-32)4-3-20-5-9-23(30)10-6-20/h5-12,21,25H,3-4,13-19H2,1-2H3
|
| Chemical Name |
[7-[4-(dimethylamino)benzoyl]-1,3-dioxo-5,6,8,8a-tetrahydroimidazo[1,5-a]pyrazin-2-yl] 4-[2-(4-chlorophenyl)ethyl]piperidine-1-carboxylate
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: 6.25 mg/mL (11.00 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7604 mL | 8.8019 mL | 17.6038 mL | |
| 5 mM | 0.3521 mL | 1.7604 mL | 3.5208 mL | |
| 10 mM | 0.1760 mL | 0.8802 mL | 1.7604 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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