2. Membrane Transporter/Ion Channel Immunology/Inflammation
  3. EAAT Interleukin Related
  4. MC-100093

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 fentanyl-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 fentanyl overdose, mood disorders and alcohol use disorders.

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MC-100093

MC-100093 Chemical Structure

CAS No. : 1639784-02-3

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MC-100093 Related Antibodies

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Description

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 fentanyl-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 fentanyl overdose, mood disorders and alcohol use disorders[1][2][3][4].

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.

MC-100093 Related Antibodies
Parmacokinetics
Species Dose Route Cmax Tmax T1/2 CL Vz Vss Bioavailability Brain-to-Plasma Ratio
Rat[3] 1 mg/kg i.v. 5.78 mg/mL 0.1 h 0.9 h 0.2 L/h 0.2 L 0.14 L / /
Rat[3] 10 mg/kg p.o. 4.17 mg/mL 1.5 h 1.8 h 1 L/h 3.2 L 4 L 28 % /
Rat[3] 25 mg/kg i.p. 11.5 μg/mL 0.5 h 4.2 h 0.04 L/h 0.26 L 0.1 L / 14 %
In Vivo

MC-100093 (100 mg/kg; i.p.; once daily for 5 consecutive days) reduces ethanol intake in alcohol-preferring rats, and upregulates the expression of GLT-1 and xCT in the medial prefrontal cortex (mPFC) and nucleus accumbens (NAc) subregions[1].
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 fentanyl-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.

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]
Dosage: 100 mg/kg
Administration: i.p.; once daily; 5 days
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.
Animal Model: BALB/c (male, 7 weeks old, fentanyl overdose model)[2]
Dosage: 50 mg/kg
Administration: i.p.; daily; days 5 to 9
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.
Animal Model: C57BL/6J (male and female, 8-10 weeks old)[4]
Dosage: 25 mg/kg; 50 mg/kg; 100 mg/kg
Administration: i.p.; daily; 6 days
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.
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]
Dosage: 50 mg/kg
Administration: i.p.; daily; 6 days
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.
Molecular Weight

269.34

Formula

C13H23N3O3
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MC-100093 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MC-1000931639784-02-3MC100093MC 100093EAATInterleukin RelatedExcitatory amino acid transporter Glutamate transporterILrat mPFCNAcmood disordersGLT-1astrocyte-neuron coculturescocaine use disorderxCTalcohol use disorderfentanylethanol dependenceGLT-1 expression upregulatoralcohol-preferring ratBALB/c miceC57BL/6J miceInhibitorinhibitorinhibit

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