MC-100093
Based on 1 Customer Validation
MC-100093 is an orally active, blood-brain barrier-permeable GLT-1 expression upregulator. MC-100093 upregulates the expression of GLT-1 and xCT in rats, and alleviates sedative agent-induced GLT-1 downregulation, IL-6 upregulation and motor hyperactivity. MC-100093 upregulates GLT-1 expression and enhances glutamate uptake in astrocyte-neuron co-culture systems. MC-100093 reduces ethanol consumption and preference, and exerts gender-specific antidepressant-like effects. MC-100093 can be used in studies related to sedative agent overdose, mood disorders and alcohol use disorders.
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- CAS. Nr.: 1639784-02-3
- Formel: C13H23N3O3
- Molecular Weight:269.34
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Speicherung:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
In Vitro
MC-100093 (0.1 μM) enhances glutamate uptake in astrocyte-neuron co-cultures with an IC50 of 0.1 μM, producing a 23.5% increase in uptake[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
In Vivo
MC-100093 (50 mg/kg; i.p.; daily; days 5 to 9) reverses GLT-1 downregulation and IL-6 upregulation in the nucleus accumbens (NAc), attenuates excessive spontaneous activity, and normalizes in vivo levels of Glycine (HY-Y0966) and Arachidonic acid (HY-109590) in sedative agent-treated male BALB/c mice[2].
MC-100093 (25-100 mg/kg, i.p., once daily for 6 consecutive days) exerts gender-specific antidepressant-like effects in female mice[4].
MC-100093 (50 mg/kg; i.p.; once daily; for 6 consecutive days) reduces ethanol preference and increases water intake in female mice with high alcohol consumption, but exerts no effect on ethanol drinking behavior in male mice with high alcohol consumption[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:alcohol-preferring (P) (male/female,, 80-85 days old, chronic ethanol consumption via continuous free-choice access to 15% v/v and 30% v/v ethanol plus water for 5 weeks)[1]
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Dosage:100 mg/kg
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Administration:i.p.; once daily; 5 days
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Result:Reduced ethanol consumption from Day 1-5 of treatment.
Significantly upregulated glutamate transporter 1 (GLT-1) expression in mPFC-infralimbic (IL) subregion relative to ethanol-saline and water-saline groups, reversing ethanol-induced downregulation.
Significantly upregulated cystine/glutamate antiporter (xCT) expression in mPFC-infralimbic (IL) subregion relative to ethanol-saline groups, reversing ethanol-induced downregulation.
Significantly upregulated GLT-1 expression in mPFC-prelimbic (PL) subregion relative to ethanol-saline and water-saline groups, reversing ethanol-induced downregulation.
Significantly upregulated xCT expression in mPFC-prelimbic (PL) subregion relative to ethanol-saline groups, reversing ethanol-induced downregulation.
Significantly upregulated GLT-1 expression in nucleus accumbens (NAc)-shell subregion relative to ethanol-saline and water-saline groups, reversing ethanol-induced downregulation.
Significantly upregulated xCT expression in nucleus accumbens (NAc)-shell subregion relative to ethanol-saline groups, reversing ethanol-induced downregulation.
Significantly upregulated GLT-1 expression in nucleus accumbens (NAc)-core subregion relative to ethanol-saline and water-saline groups.
Significantly upregulated xCT expression in nucleus accumbens (NAc)-core subregion relative to ethanol-saline groups, reversing ethanol-induced downregulation.
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Animal Model:BALB/c (male, 7 weeks old, fentanyl overdose model)[2]
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Dosage:50 mg/kg
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Administration:i.p.; daily; days 5 to 9
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Result:Attenuated fentanyl-induced hyperlocomotion, with treated mice traveling a mean total distance of 2366 cm.
Normalized fentanyl-induced reduction in glycine levels in the NAc, with no significant difference from control group glycine levels.
Prevented fentanyl-induced reduction in arachidonic acid levels in the NAc, with no significant difference from control group arachidonic acid levels.
Significantly upregulated GLT-1 protein expression in the NAc relative to fentanyl-only mice, reversing the fentanyl-induced downregulation of GLT-1.
Significantly reduced fentanyl-induced upregulation of IL-6 protein expression in the NAc, with levels not significantly different from the control group.
Did not significantly alter fentanyl-induced changes in D-glucose, D-turanose, or L-valine levels in the NAc, nor did it restore the overall fentanyl-altered NAc metabolomic profile.
Did not significantly affect Y-maze spontaneous alternation performance relative to fentanyl-only mice.
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Animal Model:C57BL/6J (male and female, 8-10 weeks old)[4]
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Dosage:25 mg/kg; 50 mg/kg; 100 mg/kg
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Administration:i.p.; daily; 6 days
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Result:Had no effect on body weight, distance traveled, or average velocity in the open field test in either sex at 50 mg/kg.
Had no effect on anxiety-like behaviors, including percentage of time spent in the open field center zone, center zone entries, percentage of time spent in elevated plus maze open arms, or open arm entries in either sex at 50 mg/kg.
Reduced immobility time and increased mobility time in female mice during the tail suspension test at 50 mg/kg; no changes were seen in male mice.
Reduced immobility time and increased mobility time in female mice during the forced swim test at 50 mg/kg; male mice showed increased immobility time and decreased mobility time at 50 mg/kg.
Showed a dose-dependent reduction in immobility time in female mice during the tail suspension test, with corresponding increased mobility time at higher dose.
Did not alter GLT1 protein expression relative to GAPDH in the medial prefrontal cortex or hippocampus in either sex at 50 mg/kg.
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Animal Model:C57BL/6J (male and female, 8-10 weeks old, high-drinking selected via 2-bottle choice continuous access paradigm with ethanol concentration escalation from 3% to 10%)[4]
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Dosage:50 mg/kg
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Administration:i.p.; daily; 6 days
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Result:Did not change ethanol intake or total liquid intake in female mice, but reduced ethanol preference and increased water intake at 50 mg/kg.
Had no effect on ethanol intake, ethanol preference, water intake, or total liquid intake in male mice at 50 mg/kg.
Chemical Information
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CAS. Nr. 1639784-02-3
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Appearance Solid
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Molecular Weight 269.34
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Formel C13H23N3O3
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SMILES
O=C(N1CCN(CC1)C)[C@@H]([C@]2([H])[C@@](C(N2)=O)([H])[C@H](O)C)C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 50 mg/mL (185.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Neuron-Astrocyte Co-culture
Neuron-astrocyte co-culture is used to study how astrocytes regulate neuronal survival, synapse formation, dendritic morphology, neuronal activity, and disease-related neurotoxicity. Indirect “sandwich” or insert-based designs physically separate neurons and astrocytes while allowing soluble astrocyte-derived factors to affect neurons, whereas direct co-culture permits cell-contact and network-level readouts.
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Ferroptosis Solutions
Ferroptosis is an iron-dependent, non-apoptotic form of regulated cell death characterized by lethal lipid peroxidation and sensitivity to suppression by iron chelators or lipophilic radical-trapping antioxidants. The core pathway links cystine uptake through system Xc−, glutathione availability, GPX4-dependent detoxification of phospholipid hydroperoxides, iron-dependent oxidative reactions, and polyunsaturated-phospholipid metabolism into a cell-death program that is biochemically and morphologically distinct from apoptosis, necrosis, and autophagy. The ferroptosis pathway is experimentally linked to phenotype through chemical and genetic perturbation. Erastin induces ferroptosis by inhibiting cystine uptake through system Xc− and weakening antioxidant defenses, while GPX4 inhibition or depletion causes lipid peroxide accumulation and ferroptotic cancer-cell death. ACSL4 and oxidizable arachidonoyl- or adrenoyl-containing phosphatidylethanolamines shape ferroptosis sensitivity by con
Reinheit & Dokumentation
Verweise
[1]. Alotaibi A, et al. Effects of MC-100093 on Ethanol Drinking and the Expression of Astrocytic Glutamate Transporters in the Mesocorticolimbic Brain Regions of Male and Female Alcohol-Preferring Rats. Neuroscience. 2024;552:89-99. [Content Brief]
[2]. Alasmari MS, et al. Neuroinflammation and Neurometabolomic Profiling in Fentanyl Overdose Mouse Model Treated with Novel β-Lactam, MC-100093, and Ceftriaxone. Toxics. 2024;12(8):604. Published 2024 Aug 19. [Content Brief]
[3]. Knackstedt LA, et al. MC-100093, a Novel β-Lactam Glutamate Transporter-1 Enhancer Devoid of Antimicrobial Properties, Attenuates Cocaine Relapse in Rats. J Pharmacol Exp Ther. 2021;378(2):51-59. [Content Brief]
[4]. León BE, et al. A novel monobactam lacking antimicrobial activity, MC-100093, reduces sex-specific ethanol preference and depressive-like behaviors in mice. Neuropharmacology. 2023 Jul 1;232:109515. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7128 mL | 18.5639 mL | 37.1278 mL | 92.8195 mL |
| 5 mM | 0.7426 mL | 3.7128 mL | 7.4256 mL | 18.5639 mL | |
| 10 mM | 0.3713 mL | 1.8564 mL | 3.7128 mL | 9.2819 mL | |
| 15 mM | 0.2475 mL | 1.2376 mL | 2.4752 mL | 6.1880 mL | |
| 20 mM | 0.1856 mL | 0.9282 mL | 1.8564 mL | 4.6410 mL | |
| 25 mM | 0.1485 mL | 0.7426 mL | 1.4851 mL | 3.7128 mL | |
| 30 mM | 0.1238 mL | 0.6188 mL | 1.2376 mL | 3.0940 mL | |
| 40 mM | 0.0928 mL | 0.4641 mL | 0.9282 mL | 2.3205 mL | |
| 50 mM | 0.0743 mL | 0.3713 mL | 0.7426 mL | 1.8564 mL | |
| 60 mM | 0.0619 mL | 0.3094 mL | 0.6188 mL | 1.5470 mL | |
| 80 mM | 0.0464 mL | 0.2320 mL | 0.4641 mL | 1.1602 mL | |
| 100 mM | 0.0371 mL | 0.1856 mL | 0.3713 mL | 0.9282 mL |
MC-100093 Related Classifications
HY-182601 Related Classifications
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