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| | K-7174, 1,4-Bis[5-(3,4,5-triMethoxyphenyl)-4(E)-pentenyl]hexahydro-1H-1,4-diazepine Basic information |
| Product Name: | K-7174, 1,4-Bis[5-(3,4,5-triMethoxyphenyl)-4(E)-pentenyl]hexahydro-1H-1,4-diazepine | | Synonyms: | K-7174, 1,4-Bis[5-(3,4,5-triMethoxyphenyl)-4(E)-pentenyl]hexahydro-1H-1,4-diazepine;K-7174 dihydrochloride;K-7174 2HCl;1,4-Bis((E)-5-(3,4,5-trimethoxyphenyl)pent-4-en-1-yl)-1,4-diazepane;K7174; K 7174; K-7174; K-7174-2HCL; K-7174 DIHYDROCHLORIDE.;1,4-Bis[5-(3,4,5-triMethoxyphenyl)-4(E)-pentenyl]hexahydro-1H-1,4-diazepine;K 7174 dihydrochloride,K7174 dihydrochloride;K-7174 (hydrochloride) | | CAS: | 191089-60-8 | | MF: | C33H48N2O6 | | MW: | 568.76 | | EINECS: | | | Product Categories: | | | Mol File: | 191089-60-8.mol | ![K-7174, 1,4-Bis[5-(3,4,5-triMethoxyphenyl)-4(E)-pentenyl]hexahydro-1H-1,4-diazepine Structure](CAS/GIF/191089-60-8.gif) |
| | K-7174, 1,4-Bis[5-(3,4,5-triMethoxyphenyl)-4(E)-pentenyl]hexahydro-1H-1,4-diazepine Chemical Properties |
| storage temp. | Store at -20°C | | solubility | Water:15.0(Max Conc. mg/mL);23.38(Max Conc. mM) | | form | A crystalline solid | | color | White to yellow | | Water Solubility | H2O: 2mg/mL, clear | | InChIKey | JXXCDAKRSXICGM-AOEKMSOUSA-N | | SMILES | C1CCN(CCC/C=C/C2C=C(OC)C(OC)=C(OC)C=2)CCN1CCC/C=C/C1C=C(OC)C(OC)=C(OC)C=1 |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | K-7174, 1,4-Bis[5-(3,4,5-triMethoxyphenyl)-4(E)-pentenyl]hexahydro-1H-1,4-diazepine Usage And Synthesis |
| Uses | K-7174, a GATA-specific inhibitor, is a putative antiinflammatory agent that attenuates effects of inflammatory cytokines in certain cell types. | | Biological Activity | K-7174 is a homopiperazine with dual GATA and proteasome inhibitory activtiy. K-7174 selective inhibts GATA-mediated gene regulations in cultures (10-30 μM; VCAM-1 expression in HUVECs or Epo suppression in Hep3B cells) and in vivo (30 mg/kg in mice via i.p. against IL-1beta- or TNF-alpha-induced anemia). K-7174 exhibits anti-myeloma activity in vitro (10-25 μM) and in vivo (50 mg/kg/day p.o. in mice) by targeting the active pockets of β1, β2 and β5 subunits of proteasome along hydrophobic grooves in the direction of the β7, β1 and β4 subunits in a manner distinct from th at of bortezomib. | | in vivo | K-7174 dihydrochloride (30 mg/kg; i.p. once daily for 9 days) reverses the decreasing of hemoglobin concentrations and reticulocyte counts by IL-1β or TNF-α[2].
K-7174 dihydrochloride (75 mg/kg; i.p. once daily for 14 days) inhibits the tumor growth in vivo[3].
K-7174 dihydrochloride (50 mg/kg; p.o. once daily for 14 days) inhibits the tumor growth in vivo and shows a better effect than intraperitoneal injection[3]. | Animal Model: | ICR mice with IL-β or TNF-α injection[2] | | Dosage: | 30 mg/kg | | Administration: | Intraperitoneal injection; 30 mg/kg once daily for 9 days | | Result: | Increased erythropoietin (Epo) production, reticulocyte counts, and hemoglobin (Hb) concentrations. |
| Animal Model: | NOD/SCID mice with murine xenograft[3] | | Dosage: | 75 mg/kg | | Administration: | Intraperitoneal injection; once daily for 14 days | | Result: | Significantly decreased tumor volume, but showed a significant body weight reduction after 10 days.
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| Animal Model: | NOD/SCID mice with murine xenograft[3] | | Dosage: | 50 mg/kg | | Administration: | Oral gavage; once daily for 14 days | | Result: | Showed an anti-myeloma activity. Porved oral administration is more effective than intraperitoneal injection.
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| | K-7174, 1,4-Bis[5-(3,4,5-triMethoxyphenyl)-4(E)-pentenyl]hexahydro-1H-1,4-diazepine Preparation Products And Raw materials |
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