| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| Other Sizes |
| Targets |
The primary target of FM19G11 is hypoxia-inducible factor (HIF) α-subunit, specifically HIF-1α and HIF-2α. By inhibiting HIF-mediated transcription, FM19G11 suppresses the expression of hypoxia-responsive genes involved in angiogenesis, glycolysis, and survival pathways. When the HIF-1α pathway is inactivated under normoxic conditions, FM19G11 regulates other signaling pathways like mTOR and PI3K/Akt/eNOS. It also inhibits cholesteryl ester transfer protein (CETP).
|
|---|---|
| ln Vitro |
In HeLa cell line, FM19G11 (30-300 nM) suppresses HIFα protein [1]. In hypoxic settings, FM19G11 (500 nM) stimulates oligodendrocyte differentiation [1]. In hypoxia GBM-XD, hypoxic T98G, and normoxic T98G cells, FM19G11 (300 nM; 3 days) dramatically reduces the mRNA levels of O6-methylguanine DNA methyltransferase (MGMT) [2]. While FM19G11 did not directly cause apoptosis, M19G11 (300 nM; 3 days) greatly increased temozolomide's (TMZ) pro-apoptotic impact [2].
In vitro, FM19G11 prevents hypoxia-induced increase in HIF-1α and HIF-2α protein levels in HeLa cultures with an IC50 of 80 nM in HRE-mediated luciferase reporter assays. FM19G11 (500 nM) promotes oligodendrocyte differentiation under hypoxic conditions. FM19G11 (300 nM) significantly enhances the pro-apoptotic effect of temozolomide, whereas FM19G11 does not induce apoptosis by itself. It suppresses hypoxia-induced luciferase activity in HeLa cells. |
| ln Vivo |
In severe spinal cord damage (SCI), FM19G11 (intramedullary injection; 1–8 weeks) improves locomotor performance [3]. The expression of RIP, a marker of myelinating oligodendrocytes at the injury site, and GAP43, an axonal growth marker, are both induced by FM19G11 (intramedullary injection; 8 weeks) [3].
In vivo, FM19G11 has demonstrated potential in research on cancer, neurodegeneration, and stem cell biology, where HIF signaling plays a critical role. It is also used to study metabolic reprogramming and tissue responses to hypoxia. Its specificity makes it a valuable probe for investigating oxygen-sensing mechanisms and therapeutic targeting of HIF pathways. However, specific in vivo efficacy data from animal models are limited in the available literature. |
| Enzyme Assay |
In vitro enzyme or receptor binding assays for FM19G11 involve measuring its inhibition of HIF-mediated transcription. HeLa cells are cultured under hypoxic conditions (1% O₂) in the presence of varying concentrations of FM19G11. HIF Responsive Element (HRE)-mediated luciferase activity is measured to determine the IC50, which is 80 nM. The compound's effects on HIF-1α and HIF-2α protein levels are assessed by Western blotting.
|
| Cell Assay |
Cell viability assay [2]
Cell Types: GBM-XD and T98G Cell Tested Concentrations: 300 nM Incubation Duration: 3 days Experimental Results: No cytotoxicity per se. Enhanced TMZ cytotoxicity in hypoxic GBM-XD cells, hypoxic T98G cells and normoxic T98G cells. Western Blot Analysis[2] Cell Types: GBM-XD and T98G Cell Tested Concentrations: 300 nM Incubation Duration: 3 days Experimental Results: In hypoxic culture, MGMT expression in both cell lines was Dramatically inhibited. The expression of MGMT was Dramatically down-regulated in T98G cells cultured under normoxia. In vitro cell-based assays for FM19G11 are performed using HeLa cells and other cell lines. Cells are cultured under normoxic or hypoxic conditions and treated with FM19G11 at concentrations ranging from 80 nM to 500 nM. HIF-1α and HIF-2α protein levels are measured by Western blotting. HRE-mediated luciferase activity is measured using a reporter assay. Oligodendrocyte differentiation is assessed under hypoxic conditions. |
| Animal Protocol |
In vivo animal experiments for FM19G11 are limited in the available literature. The compound has demonstrated potential in research on cancer, neurodegeneration, and stem cell biology. It is used to study metabolic reprogramming and tissue responses to hypoxia. However, specific animal experimental protocols are not well-documented. The compound is typically administered orally or intraperitoneally in preclinical studies.
|
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of FM19G11 indicate that it is a cell-permeable small molecule. The compound has a molecular weight of 463.40 and a molecular formula of C23H17N3O8. It has a purity of ≥95%. The compound is soluble in DMSO. The IUPAC name is [2-(4-methylphenyl)-2-oxoethyl] 3-[(2,4-dinitrobenzoyl)amino]benzoate. Storage at -20°C is recommended.
|
| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for FM19G11 are characteristic of a research compound. As a HIF inhibitor, its safety profile is an important consideration. The compound is generally well-tolerated at effective doses in cell-based assays. However, its long-term safety profile in vivo requires further evaluation. The compound is for research use only and not for human therapeutic use.
|
| References |
|
| Additional Infomation |
3-[[(2,4-dinitrophenyl)-oxymethyl]amino]benzoic acid [2-(4-methylphenyl)-2-oxyethyl] ester is a member of the benzamide class of compounds.
Other information: FM19G11 is a hypoxia-inducible factor (HIF) α-subunit inhibitor. It is also known as HIF-1α/2α Inhibitor IV. The compound is a cell-permeable benzamido-benzoate small molecule. It has demonstrated potential in research on cancer, neurodegeneration, and stem cell biology. Its CAS number is 329932-55-0. |
| Molecular Formula |
C23H17N3O8
|
|---|---|
| Molecular Weight |
463.402
|
| Exact Mass |
463.102
|
| CAS # |
329932-55-0
|
| PubChem CID |
1730746
|
| Appearance |
White to off-white solid powder
|
| LogP |
5.533
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
34
|
| Complexity |
784
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
XVUOIWIIQVGWAJ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C23H17N3O8/c1-14-5-7-15(8-6-14)21(27)13-34-23(29)16-3-2-4-17(11-16)24-22(28)19-10-9-18(25(30)31)12-20(19)26(32)33/h2-12H,13H2,1H3,(H,24,28)
|
| Chemical Name |
[2-(4-methylphenyl)-2-oxoethyl] 3-[(2,4-dinitrobenzoyl)amino]benzoate
|
| Synonyms |
FM19 G11; FM19-G11; FM19G11
|
| 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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~100 mg/mL (~215.80 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 | 2.1580 mL | 10.7898 mL | 21.5796 mL | |
| 5 mM | 0.4316 mL | 2.1580 mL | 4.3159 mL | |
| 10 mM | 0.2158 mL | 1.0790 mL | 2.1580 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
