WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H522717
CAS#: 945714-67-0
Description: FPS-ZM1 is a high-affinity RAGE-specific blocker that inhibits amyloid-β binding to RAGE, neurological damage and inflammation in the APP(sw/0) transgenic mouse model of AD. FPS-ZM1 is not toxic to mice and can easily cross the blood-brain barrier. AGEs administration induced an-regulation of Abeta production, inflammation, and oxidative stress, and an increased escape latency of rats in the Morris water maze test, all of these are significantly reduced by FPS-ZM1 treatment. FPS-ZM1 might be a novel therapeutic agent to treat AD patients.
Hodoodo Cat#: H522717
Name: FPS-ZM1
CAS#: 945714-67-0
Chemical Formula: C20H22ClNO
Exact Mass: 327.14
Molecular Weight: 327.852
Elemental Analysis: C, 73.27; H, 6.76; Cl, 10.81; N, 4.27; O, 4.88
Synonym: FPS-ZM1; FPS ZM1; FPSZM1; FPS-ZM 1; FPS ZM-1; FPSZM 1;
IUPAC/Chemical Name: N-benzyl-4-chloro-N-cyclohexylbenzamide
InChi Key: XDFKWGIBQMHSOH-UHFFFAOYSA-N
InChi Code: InChI=1S/C20H22ClNO/c21-18-13-11-17(12-14-18)20(23)22(19-9-5-2-6-10-19)15-16-7-3-1-4-8-16/h1,3-4,7-8,11-14,19H,2,5-6,9-10,15H2
SMILES Code: C1CCC(CC1)N(CC2=CC=CC=C2)C(=O)C3=CC=C(C=C3)Cl
Appearance: White Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | FPS-ZM1 is a RAGE inhibitor with a Ki of 25 nM. |
| In vitro activity: | The regulatory effect of FPS‑ZM1 on HG (hyperglycemia) induced inflammation was studied in BMSCs (bone marrow mesenchymal stem cells. Furthermore, the role of the TXNIP/NLRP3 inflammasome signaling pathway in the regulatory effects of FPS‑ZM1 on HG‑induced inflammation was studied. In BMSCs, RAGE expression was stimulated by HG, an effect which was reversed by treatment with FPS‑ZM1. In addition, HG activated inflammatory factors, such as TNF‑α, IL‑1β and IL‑6; however, their levels were suppressed when cells were treated with FPS‑ZM1. Furthermore, FPS‑ZM1 inhibited the mRNA and protein expression levels of TXNIP, caspase‑1, NLRP3 and ASC, and promoted TRX expression. Reference: Mol Med Rep. 2020 Oct;22(4):3255-3262. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7453676/ |
| In vivo activity: | The hypothesis that the RAGE-specific antagonist FPS-ZM1 is neuroprotective against ischemic brain injury was tested. Distal middle cerebral artery occlusion (MCAO) was performed on Sprague-Dawley male rats (n = 60), which were then treated with FPS-ZM1 or vehicle. After 1 week, neurological function was evaluated, and then, brain tissues were collected for 2,3,5-triphenyltetrazolium chloride staining, Nissl staining, TUNEL staining, Western blotting, and immunohistochemical analyses. FPS-ZM1 treatment after MCAO markedly attenuated neurological deficits and reduced the infarct area. More interestingly, FPS-ZM1 inhibited ischemia-induced astrocytic activation and microgliosis and decreased the elevated levels of proinflammatory cytokines. Furthermore, FPS-ZM1 blocked the increase in the level of RAGE and, notably, of DIAPH1, the key cytoplasmic hub for RAGE-ligand-mediated activation of cellular signaling. These findings reveal that FPS-ZM1 treatment reduces neuroinflammation in rats with focal cerebral ischemia and further suggest that the ligand/RAGE/DIAPH1 pathway contributes to this FPS-ZM1-mediated alleviation of neuroinflammation. Reference: ACS Chem Neurosci. 2021 Jan 6;12(1):63-78. https://pubs.acs.org/doi/10.1021/acschemneuro.0c00530 |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 55.7 | 169.89 | |
| Ethanol | 37.6 | 114.66 | |
| DMF | 30.0 | 91.51 | |
| DMF:PBS (pH 7.2) (1:7) | 0.1 | 0.37 |
The following data is based on the product molecular weight 327.85 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Jiang M, Wang X, Wang P, Peng W, Zhang B, Guo L. Inhibitor of RAGE and glucose‑induced inflammation in bone marrow mesenchymal stem cells: Effect and mechanism of action. Mol Med Rep. 2020 Oct;22(4):3255-3262. doi: 10.3892/mmr.2020.11422. Epub 2020 Aug 7. PMID: 32945430; PMCID: PMC7453676. 2. Shen L, Zhang T, Yang Y, Lu D, Xu A, Li K. FPS-ZM1 Alleviates Neuroinflammation in Focal Cerebral Ischemia Rats via Blocking Ligand/RAGE/DIAPH1 Pathway. ACS Chem Neurosci. 2021 Jan 6;12(1):63-78. doi: 10.1021/acschemneuro.0c00530. Epub 2020 Dec 10. PMID: 33300334. 3. Liu Y, Shen W, Chen Q, Cao Q, Di W, Lan R, Chen Z, Bai J, Han Z, Xu W. Inhibition of RAGE by FPS-ZM1 alleviates renal injury in spontaneously hypertensive rats. Eur J Pharmacol. 2020 Sep 5;882:173228. doi: 10.1016/j.ejphar.2020.173228. Epub 2020 Jun 2. PMID: 32502492. |
| In vitro protocol: | 1. Jiang M, Wang X, Wang P, Peng W, Zhang B, Guo L. Inhibitor of RAGE and glucose‑induced inflammation in bone marrow mesenchymal stem cells: Effect and mechanism of action. Mol Med Rep. 2020 Oct;22(4):3255-3262. doi: 10.3892/mmr.2020.11422. Epub 2020 Aug 7. PMID: 32945430; PMCID: PMC7453676. |
| In vivo protocol: | 1. Shen L, Zhang T, Yang Y, Lu D, Xu A, Li K. FPS-ZM1 Alleviates Neuroinflammation in Focal Cerebral Ischemia Rats via Blocking Ligand/RAGE/DIAPH1 Pathway. ACS Chem Neurosci. 2021 Jan 6;12(1):63-78. doi: 10.1021/acschemneuro.0c00530. Epub 2020 Dec 10. PMID: 33300334. 2. Liu Y, Shen W, Chen Q, Cao Q, Di W, Lan R, Chen Z, Bai J, Han Z, Xu W. Inhibition of RAGE by FPS-ZM1 alleviates renal injury in spontaneously hypertensive rats. Eur J Pharmacol. 2020 Sep 5;882:173228. doi: 10.1016/j.ejphar.2020.173228. Epub 2020 Jun 2. PMID: 32502492. |
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(Last updated: 4/20/2016)
