| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Targets |
IMM-H007 targets AMP-activated protein kinase (AMPK), a key regulator of cellular energy homeostasis, which it activates. It also acts as an antagonist of transforming growth factor β1 (TGFβ1). Through AMPK activation, it inactivates downstream inflammatory signaling pathways, including NF-κB and JNK/AP1. Furthermore, it inhibits ABCA1 degradation and promotes its cell-surface localization in macrophages.
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| ln Vitro |
In vitro, IMM-H007 significantly inhibits monocyte adhesion to endothelial cells and their subsequent transendothelial migration. Mechanistically, it represses TNFα-induced IκBα degradation and NF-κB nuclear translocation, thereby suppressing NF-κB-mediated inflammatory responses. It also inhibits the JNK/c-Jun inflammatory signaling pathway by reducing its phosphorylation. These actions lead to a negative regulation of endothelial inflammation.
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| ln Vivo |
IMM-H007 concurrently promotes fatty acid oxidation, autophagy, and hepatic lipid export while suppressing fatty acid import into hepatocytes and hepatic lipogenesis [2]. By decreasing ISO-induced Smad2/3 phosphorylation downstream of TGFβ1 via AMPKα2, IMM-H007 (200 mg/kg, oral, once daily, for 10 days) inhibits ISO-induced cardiac fibrosis and diastolic dysfunction independently of AMPKα2 expression [3]. TGFβ1 expression inhibition in cardiac fibrosis is AMPKα2-dependent.
In vivo, IMM-H007 has demonstrated cardioprotective effects. It regulates lipid metabolism and effectively resolves hepatic steatosis in high-fat diet-fed hamsters. It inhibits fatty acid import into hepatocytes and liver lipogenesis while concomitantly stimulating fatty acid oxidation. It also reduces isoprenaline-induced Smad2/3 phosphorylation downstream of TGFβ1 and cardiac fibrosis. |
| Enzyme Assay |
Non-cellular assays for IMM-H007's activity typically involve measuring AMPK activation. This is often done using a cell-free kinase assay where recombinant AMPK is incubated with ATP and a substrate peptide in the presence of the compound. The phosphorylation of the substrate is then quantified using techniques like ELISA or by using radioactive [γ-³²P]-ATP. The compound's ability to directly activate AMPK is determined from the dose-response curve.
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| Cell Assay |
In vitro cellular assays for IMM-H007 commonly use endothelial cells or macrophages. To assess its anti-inflammatory effects, endothelial cells are pre-treated with the compound and then stimulated with TNFα. The extent of monocyte adhesion is measured. For signaling studies, the phosphorylation status of proteins like IκBα, NF-κB, and JNK is analyzed by Western blotting. In macrophages, the effect on ABCA1 protein level and cell-surface localization, as well as cholesterol efflux, is assessed.
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| Animal Protocol |
In vivo animal studies for IMM-H007 have been conducted using hamster models of high-fat diet-induced hepatic steatosis to evaluate its lipid-lowering and liver-protective effects. The compound is typically administered orally. Endpoints include measuring hepatic lipid content, serum lipid profiles, and markers of liver injury. In other models, its effect on cardiac fibrosis and inflammation is assessed, for example, by measuring Smad2/3 phosphorylation in heart tissue.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of IMM-H007 are not extensively detailed in the available literature, but as a small molecule (MW 485.45), it is suitable for oral administration. It is soluble in DMSO. For in vivo use, it can be formulated in vehicles like 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline.
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| Toxicity/Toxicokinetics |
Specific toxicological data for IMM-H007 are not extensively provided. As a research compound, comprehensive toxicity profiles are not typically available in product descriptions. It is intended for research use only and not for human consumption. Standard laboratory safety precautions should be observed when handling this compound.
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| References |
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| Additional Infomation |
IMM-H007 is a research-grade compound for laboratory use only and is not approved for clinical use. Its primary applications are in researching metabolic and inflammatory diseases, including atherosclerosis, NAFLD, and cardiac fibrosis. It is a valuable tool for studying the AMPK and TGFβ1 signaling pathways. Its CAS number is 1221412-23-2, and its molecular formula is C₂₂H₂₃N₅O₈.
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| Molecular Formula |
C22H23N5O8
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| Molecular Weight |
485.45
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| CAS # |
1221412-23-2
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| Related CAS # |
1221412-23-2;
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| Appearance |
White to off-white solid powder
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| Density |
1.54±0.1 g/cm3
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| Boiling Point |
684.6±65.0 °C
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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 (~257.49 mM)
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| 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 | 2.0599 mL | 10.2997 mL | 20.5994 mL | |
| 5 mM | 0.4120 mL | 2.0599 mL | 4.1199 mL | |
| 10 mM | 0.2060 mL | 1.0300 mL | 2.0599 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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