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

MC-100093 是一种具有口服活性和血脑屏障透过性的 GLT-1 表达上调剂。MC-100093 可上调大鼠中 GLT-1 和 xCT 的表达，减轻芬太尼诱导的 GLT-1 下调、IL-6 上调以及运动过度活跃。MC-100093 可在星形胶质细胞-神经元共培养体系中上调 GLT-1 表达并增强谷氨酸摄取。MC-100093 能够减少乙醇的消耗量和偏好性，发挥性别特异性的类抗抑郁作用。MC-100093 可用于芬太尼过量、心境障碍以及酒精使用障碍的相关研究。

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MC-100093

MC-100093 Chemical Structure

CAS No. : 1639784-02-3

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MC-100093 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

MC-100093 可增强星形胶质细胞-神经元共培养体系中的谷氨酸摄取能力，其 IC50 为 0.1 μM，可使摄取量提升 23.5%[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

MC-100093 相关抗体:
药代动力学
(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 %
体内研究
(In Vivo)

MC-100093 (100 mg/kg；腹腔注射；每日 1 次；连续 5 天) 可减少嗜酒大鼠的乙醇摄入量，并上调其内侧前额叶皮层 (mPFC) 和伏隔核 (NAc) 亚区中 GLT-1 与 xCT 的表达[1]。
MC-100093 (50 mg/kg；腹腔注射；每日；第 5 至 9 天) 在芬太尼诱导雄性 BALB/c 小鼠中可逆转伏隔核 (NAc) 中 GLT-1 下调与 IL-6 上调，减轻过度自主活动，并使体内 Glycine (HY-Y0966) 与 Arachidonic acid (HY-109590) 水平恢复正常[2]。
MC-100093 (25-100 mg/kg，腹腔注射，每日 1 次，连续 6 天) 在雌性小鼠中发挥性别特异性的类抗抑郁作用[4]。
MC-100093 (50 mg/kg；腹腔注射；每日一次；连续 6 天) 可降低高饮酒雌性小鼠的乙醇偏好性并增加其饮水量，但对高饮酒雄性小鼠的乙醇饮酒行为无影响[4]。

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.
分子量

269.34

Formula

C13H23N3O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

MC-100093 相关分类

  • 摩尔计算器

  • 稀释计算器

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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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