| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
AMPK; OXPHOS/oxidative phosphorylation
|
|---|---|
| ln Vitro |
In NIH3T3 murine fibroblasts, lixumistat hydrochloride (0.31–10 μM) phosphorylates AMPKα1 Thr172 in a dose- and time-dependent manner[1]. Important components of glucose homeostasis, such as phosphoenolpyruvate carboxykinase 1 (Pck1) and glucose-6 phosphatase (G6pase), are not affected by riminostat hydrochloride [1].
|
| ln Vivo |
Lixumistat (hydrochloride) did not impact metabolic regulation as determined by body weight, blood glucose, insulin levels, and lipid metabolic content in mice with diet-induced obesity [1]. Lixumistat (HCl) (50 mg/kg; for 2 months) does not influence body weight, general mobility, or anxiety [2]. Lixumistat (hydrochloride) can greatly prevent the aging-induced deterioration in new object recognition memory and spatial working memory [2]. Lixumistat (hydrochloride) dramatically boosts AMPK activation in the hippocampus of elderly mice [2].
|
| Cell Assay |
Western Blot analysis [1]
Cell Types: NIH3T3 cells Tested Concentrations: 0.31 μM, 0.62 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM Incubation Duration: 4 hrs (hours) Experimental Results: AMPK phosphorylation rate was Dramatically increased. |
| Animal Protocol |
Animal/Disease Models: C57BL/6J mice (young group/12-16 weeks, old group/20-22 months) [2]
Doses: 50 mg/kg Route of Administration: Orally (drinking water), lasting 2 months Experimental Results: Age-related cognitive decline. |
| References |
|
| Additional Infomation |
Lixumistat is an orally bioavailable biguanide compound and mitochondrial oxidative phosphorylation (OxPhos) inhibitor, with potential antineoplastic activity. Upon administration, lixumistat inhibits oxidative phosphorylation, decreases mitochondrial function, prevents tumor cell metabolism and deprives tumor cells of energy, thereby preventing tumor cell proliferation. Mitochondrial OxPhos is overactivated in cancer cells and plays a key role in tumor cell proliferation. Drug resistant tumor cells are very susceptible to decreased mitochondrial OxPhos as they cannot easily compensate for the decrease in mitochondrial function by increasing glycolysis.
|
| Molecular Formula |
C13H17CLF3N5O
|
|---|---|
| Molecular Weight |
351.76
|
| Exact Mass |
351.107
|
| CAS # |
1422365-52-3
|
| Related CAS # |
Lixumistat acetate;1422365-94-3;Lixumistat;1422365-93-2
|
| PubChem CID |
71512108
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
22
|
| Complexity |
424
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1CCN(C1)/C(=N/C(=NC2=CC=C(C=C2)OC(F)(F)F)N)/N.Cl
|
| InChi Key |
FSEAYPJRYNBFTN-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C13H16F3N5O.ClH/c14-13(15,16)22-10-5-3-9(4-6-10)19-11(17)20-12(18)21-7-1-2-8-21;/h3-6H,1-2,7-8H2,(H4,17,18,19,20);1H
|
| Chemical Name |
N'-[N'-[4-(trifluoromethoxy)phenyl]carbamimidoyl]pyrrolidine-1-carboximidamide;hydrochloride
|
| Synonyms |
HL271; HL-271
|
| 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) |
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
|
|---|---|
| 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 | 2.8428 mL | 14.2142 mL | 28.4285 mL | |
| 5 mM | 0.5686 mL | 2.8428 mL | 5.6857 mL | |
| 10 mM | 0.2843 mL | 1.4214 mL | 2.8428 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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