FPS-ZM1
Catalog No.: GC15105Purity:>98.00%Synonyms: RAGE Antagonist
مثبط الغضب
المنتجات مخصصة للاستخدام البحثي فقط، وليست للاستخدام البشري. نحن لا نبيع للمرضى.
Cas No.: 945714-67-0
10mM (in 1mL DMSO)In Stock
$44.00
1
5mgIn Stock
$40.00
1
10mgIn Stock
$60.00
1
50mgIn Stock
$192.00
1
100mgIn Stock
$296.00
1
200mgIn Stock
$472.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $44.00 | In Stock | 1 | |
| 5mg | $40.00 | In Stock | 1 | |
| 10mg | $60.00 | In Stock | 1 | |
| 50mg | $192.00 | In Stock | 1 | |
| 100mg | $296.00 | In Stock | 1 | |
| 200mg | $472.00 | In Stock | 1 |
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المراجع (Citations)
5 publicationsمنشورات الباحثين الذين استخدموا هذا المنتجالوصف (Description)
FPS-ZM1 is a RAGE-specific inhibitor, with a Ki value of 25nM[1]. FPS-ZM1 has been widely used in the research for improving the inflammatory response[2].
In vitro, FPS-ZM1 treatment (100nM; 1h) significantly inhibited the overexpression of RAGE induced by advanced glycation end product (AGE), RAGE-dependent microglial activation, nuclear translocation of nuclear factor κB p65 (NF-κB p65), and the expression of downstream inflammatory mediators such as tumor necrosis factor -α (TNF-α) and interleukin-1 β (IL-1β) in rat primary microglia[3]. Pretreated with 20μM FPS-ZM1 for 2 hours inhibited the expression of pro-inflammatory mediators and cytokines induced by lipopolysaccharide (LPS) in BV-2 cells[4].
In vivo, FPS-ZM1 treatment (1 mg/kg/day; i.p.) for 4 consecutive weeks reduced the production of amyloid-β (Aβ)1-40 and Aβ1-42 in Wistar rats and inhibited the increase of AGE-mediated Aβ metabolism-related proteins in the hippocampus[5]. FPS-ZM1 was administered orally at a dose of 2mg/kg/day for 2 months, reduced the levels of serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), glutamate dehydrogenase (GLD), α -glutathione S-transferase (α-GST), alkaline phosphatase (ALP) and γ -glutamyl transpeptidase (GGT) in diabetic mice[6]. Intraperitoneal injection of FPS-ZM1 (3mg/kg/day) for 4 consecutive weeks can reduce lipid deposition in hepatocytes and lower the levels of mature SBP-1C, p-p65 nfκb and p-p38 MAPK in liver tissues in KK-Ay mice[7].
References:
[1]Zhou W, Hu W. Anti-neuroinflammatory agents for the treatment of Alzheimer’s disease[J]. Future Medicinal Chemistry, 2013, 5(13): 1559-1571.
[2] Shen L, Zhang T, Yang Y, et al. FPS-ZM1 alleviates neuroinflammation in focal cerebral ischemia rats via blocking ligand/RAGE/DIAPH1 pathway[J]. ACS chemical neuroscience, 2020, 12(1): 63-78.
[3] Shen C, Ma Y, Zeng Z, et al. RAGE-specific inhibitor FPS-ZM1 attenuates AGEs-induced neuroinflammation and oxidative stress in rat primary microglia[J]. Neurochemical research, 2017, 42: 2902-2911.
[4]Wang L, Zhao D, Wang H, et al. FPS-ZM1 inhibits LPS-induced microglial inflammation by suppressing JAK/STAT signaling pathway[J]. International immunopharmacology, 2021, 100: 108117.
[5] Hong Y, Shen C, Yin Q, et al. Effects of RAGE-specific inhibitor FPS-ZM1 on amyloid-β metabolism and AGEs-induced inflammation and oxidative stress in rat hippocampus[J]. Neurochemical research, 2016, 41: 1192-1199.
[6] Aslani S, Bahrambeigi S, Sanajou D. FPS-ZM1 Alleviates Circulating Indices of Liver Injury in Diet-Induced Type 2 Diabetic Mice[J]. Acta Medica Iranica, 2022: 40-45.
[7] Zhang M, Zhao W, Zhang Z, et al. FPS-ZM1 attenuates the deposition of lipid in the liver of diabetic mice by sterol regulatory element binding protein-1c[J]. BMC Endocrine Disorders, 2024, 24(1): 164.
البروتوكول (Protocol)
| Cell experiment [1]: | |
|
Cell lines |
BV-2 cells |
|
Preparation Method |
BV-2 cells were cultured in Dulbecco’s modified Eagle’s medium with 10% heat-inactivated fetal bovine serum, 100U/mL penicillin and 100μg/mL streptomycin. The culture temperature was 37℃ and the humidity was 5% CO2. BV-2 cells were seeded in 96-well plates at a density of 2×104cells/mL and cultured for 24 hours. Cells were pretreated with FPS-ZM1 (5, 10, and 20μM) for 2 hours and then treated with LPS (100ng/mL) for 24 hours. After treatment, add 10μL of 3-(4, 5-dimethylthiazole-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) solution (5mg/mL) to each well and incubate at 37℃ for 3 hours. The formazan was dissolved in 100μL DMSO, and the absorbance at 490nm was recorded using an microplate reader. Determine the levels of inflammatory cytokines IL-6 and TNF-α in the culture medium in accordance with the manufacturer's instructions. |
|
Reaction Conditions |
5, 10, and 20μM; 2h |
|
Applications |
FPS-ZM1 inhibited the expression of pro-inflammatory mediators and cytokines induced by LPS in a concentration-dependent manner without affecting cell viability. |
| Animal experiment [2]: | |
|
Animal models |
KK-Ay mice |
|
Preparation Method |
Eight KK-Ay mice were fed with the dedicated feed for 8 weeks (15 weeks of age) to establish a mouse model of diabetes mellitus complicated with nonalcoholic fatty liver disease (NAFLD). Eight KK-Ay mice, after being fed a specific diet for 8 weeks, were then fed a specific diet and FPS-ZM1 (3mg/kg/day, i.p.) for 4 weeks. After the experiment was completed, the mice were anesthetized with 50mg/kg pentobarbital sodium. Blood samples are collected through cardiac puncture. All the mice were sacrificed by cervical dislocation. The liver tissues were removed and carefully washed. Subsequently, the tissues were fixed with 4% paraformaldehyde or frozen and stored at -80°C. According to the instructions of the kit, AGEs in plasma were determined by ELISA. Add 50μL of the sample or standard solution to each well of the microplate. Then add 50μL of test reagent A and incubate at 37℃ for 1 hour. After washing three times, add test reagent B and incubate at 37℃ for 30 minutes. After washing 5 times, add 90μL of the substrate. Incubate at 37℃ for 10 minutes and add 50μL of stop solution. Finally, place the microplate into the ELISA reader and read the optical density (OD) value at a wavelength of 450nm. Based on the OD values of standard solution solutions of different concentrations, a standard curve was plotted, and the concentration of AGEs in the sample was calculated through the OD values. |
|
Dosage form |
3mg/kg/day for 4 week; i.p. |
|
Applications |
FPS-ZM1 treatment significantly reduced lipid deposition in hepatocytes and lowered the levels of mature SBP-1C, p-p65 nfκb and p-p38 MAPK in liver tissues of mice. |
|
References: |
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وثائق المنتج (Product Documents)
Purity:>98.00%Appearance:A solid
البيانات البيولوجية (Biological Data)
1 / 1
الخصائص الكيميائية (Chemical Properties)
رقم CAS
945714-67-0
المرادفات
RAGE Antagonist
الاسم الكيميائي
4-chloro-N-cyclohexyl-N-(phenylmethyl)-benzamide
SMILES
ClC1=CC=C(C(N(CC2=CC=CC=C2)C3CCCCC3)=O)C=C1
الصيغة الجزيئية
C20H22ClNO
الوزن الجزيئي
327.9
الذوبانية
≥ 28.6mg/mL in DMSO
التخزين
Store at -20°C
إرشادات عامة
اختر مذيبًا مناسبًا وفقًا لبيانات ذوبانية المنتج. بعد التحضير، قسّم المحلول المخزون إلى أجزاء لتجنب دورات التجميد والذوبان المتكررة.
استخدم المحاليل المخزونة خلال 6 أشهر عند حفظها في -80°C، أو خلال شهر واحد عند حفظها في -20°C.
لتحسين الذوبانية، سخّن الأنبوب إلى 37°C وعرّضه للموجات فوق الصوتية لمدة مناسبة.
استخدم المحاليل المخزونة خلال 6 أشهر عند حفظها في -80°C، أو خلال شهر واحد عند حفظها في -20°C.
لتحسين الذوبانية، سخّن الأنبوب إلى 37°C وعرّضه للموجات فوق الصوتية لمدة مناسبة.
شروط الشحن
تُشحن عينات التقييم مع عبوات تبريد. وتُشحن الأحجام الأخرى المتاحة في درجة حرارة الغرفة، أو مع عبوات تبريد عند الطلب.
الحاسبات (Calculators)المولارية / التخفيف / الوزن الجزيئي / تحويل الوحدات / تركيبة داخل الجسم الحي / الذوبانية
g/mol
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