| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
Magnesium ions (Mg2+).
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|---|---|
| ln Vitro |
KMG-104 is excited at 490 nm and emits fluorescence around 510 nm, making it useful for confocal laser scanning microscopy. The dissociation constant (Kd) for Mg is 3 mM. The fluorescent intensity of KMG-104 increases with an increase in [Mg], and it is unaffected by Na, K, and Ca. The only changes in physiological conditions that KMG-104 can detect are [Mg] changes[2]. Novel Mg indicator KMG-104 and Ca indicator fura-2 are loaded into PC12 cells, and intracellular Mg is investigated in the mitochondria, Mg-ATP, and endoplasmic reticulums (ERs)[2].
In cell-free assays, KMG-104 exhibits a dissociation constant (Kd) of approximately 3 mM for Mg2+, well within the physiological range of intracellular free Mg2+ concentrations. The fluorescence intensity increases proportionally with [Mg2+] and shows no significant response to physiologically relevant concentrations of Na+, K+, or Ca2+. This high selectivity for Mg2+ over other divalent cations is a key feature of the probe. |
| ln Vivo |
PC12 cells have been loaded with KMG-104 to monitor cytoplasmic Mg2+ changes in real-time. It is a cell-impermeable indicator; therefore, cells must be loaded with the acetoxymethyl (AM) ester form of KMG-104 (KMG-104 AM) for live-cell studies. Once inside the cell, the AM group is cleaved by endogenous esterases, trapping the active indicator. After loading, Mg2+ fluxes induced by agonists or changes in extracellular conditions can be observed by measuring changes in fluorescence (Ex/Em = 490/510 nm).
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| Enzyme Assay |
A standard protocol: Prepare a 1 mM stock of KMG-104 in dry DMSO. Dilute stock to working concentration (e.g., 5-20 uM) in a buffer containing various concentrations of MgCl2 (0-10 mM) and fixed background levels of other ions (e.g., 140 mM KCl, 10 mM HEPES, pH 7.2). Incubate for 10 min. Measure fluorescence using a fluorometer or plate reader with Ex=490 nm, Em=510 nm. Plot fluorescence intensity vs. [Mg2+] to determine Kd.
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| Cell Assay |
For AM ester loading: Prepare a 1 mM stock of KMG-104 AM in dry DMSO. Dilute to 2-10 uM in cell culture medium. Remove medium from adherent cells and replace with AM ester-containing medium. Incubate cells at 37degC for 30-60 min. Wash cells three times with HBSS or PBS to remove extracellular dye. Incubate cells for an additional 15-30 min to allow complete de-esterification. For confocal imaging, maintain cells at 37degC and use Ex=488 nm (Argon laser), Em=500-530 nm. Add ionomycin (10 uM) and varying [Mg2+] to calibrate.
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| Animal Protocol |
For in vivo studies, KMG-104 is typically not used due to its hydrophilicity and membrane impermeability. If required, a solution formulation can be prepared: Dissolve KMG-104 in DMSO, then dilute with 40% PEG300 and 5% Tween-80, and finally add saline to reach a final DMSO concentration of 10%. Administer via intravenous or intraperitoneal injection for tissue distribution studies, though it is not typically used for in vivo imaging.
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| ADME/Pharmacokinetics |
KMG-104 has a molecular weight of 435.33 g/mol and is soluble in DMSO at 50 mg/mL. As a hydrophilic anionic probe (cell-impermeable), it is rapidly excreted via renal filtration. The AM ester derivative enhances cell permeability; once inside cells, it becomes trapped due to de-esterification. In vivo, the non-esterified form is expected to have a short plasma half-life (~0.5-1 hour) and low tissue accumulation.
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| Toxicity/Toxicokinetics |
MTT assays have indicated that KMG-104 exhibits low cytotoxicity at concentrations up to 50 uM in various cell lines, making it suitable for long-term Mg2+ monitoring studies. No specific systemic toxicity data in animals is available for this probe, but as an ion indicator, it is expected to have a favorable safety profile for in vitro use.
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| References | |
| Additional Infomation |
KMG-104 is a research-grade chemical probe designed for basic science studies of Mg2+ signaling in cellular physiology, metabolism, and pathology (e.g., cardiac function, neurological disorders). It is not a drug and has not entered clinical trials or been approved for diagnostic or therapeutic use.
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| Molecular Formula |
C23H11F2NO6
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|---|---|
| Molecular Weight |
435.33
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| Exact Mass |
435.055
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| CAS # |
852057-94-4
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| PubChem CID |
101756039
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| Appearance |
Brown to red solid powder
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| LogP |
3.859
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
32
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| Complexity |
1180
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC2=C(C=C(C(=O)N2C=C1)C(=O)O)C3=C4C=C(C(=O)C=C4OC5=CC(=C(C=C53)F)O)F
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| InChi Key |
SKMWGJDXOVFHEN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H11F2NO6/c24-14-6-11-19(8-17(14)27)32-20-9-18(28)15(25)7-12(20)21(11)10-5-13(23(30)31)22(29)26-4-2-1-3-16(10)26/h1-9,27H,(H,30,31)
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| Chemical Name |
1-(2,7-difluoro-3-hydroxy-6-oxoxanthen-9-yl)-4-oxoquinolizine-3-carboxylic acid
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.2971 mL | 11.4855 mL | 22.9711 mL | |
| 5 mM | 0.4594 mL | 2.2971 mL | 4.5942 mL | |
| 10 mM | 0.2297 mL | 1.1486 mL | 2.2971 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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