cis-ACCP

Names

[ Name ]:
cis-ACCP

[Synonym ]:
Phosphonic acid, [[[(1R,2S)-2-aminocyclohexyl]amino]carbonyl]-

Biological Activity

[Description]:

cis-ACCP is an orally active antimetastatic matrix metalloproteinase-2 (MMP-2) selective inhibitor. cis-ACCP can inhibit MMP-2 and MMP-9 with IC50 values of 4 μM and 20 μM, respectively. cis-ACCP can be used for the research of a variety of chronic diseases[1].

[Related Catalog]:

Research Areas >> Cancer

Research Areas >> Cardiovascular Disease

Research Areas >> Infection

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Metabolic Enzyme/Protease >> MMP

[Target]

MMP-2:4 μM (IC50)

MMP-9:20 μM (IC50)

[In Vitro]

cis-ACCP 可以抑制 MMP-2 和 MMP-9，IC50 值分别为 4 μM 和 20 μM[1]。

[In Vivo]

cis-ACCP（i.p.；50、250、500 mg/kg；每天一次，持续两周）没有显示出毒性作用并减少小鼠转移形成[1]。 cis-ACCP（口服，i.v.，i.p.；50、150 mg/kg）仅分布在细胞外液中[1]。 Animal Model: C57BL mice[1] Dosage: 50, 250, 500 mg/kg; 12.5 to 50 mg/kg Administration: Oral, intraperitoneal, daily for two weeks; daily, 21 days Result: Showed no toxic effects and showed 50-85% inhibition of metastasis formation, depending on the dose. Animal Model: Rats[1] Dosage: 50, 150 mg/kg Administration: Oral, intravenous, intraperitoneal Result: Showed 84% of the intravenously administered drug are excreted unchanged.

[References]

[1]. Hoffman, Amnon et al. Carbamoylphosphonate matrix metalloproteinase inhibitors 6: cis-2-aminocyclohexylcarbamoylphosphonic acid, a novel orally active antimetastatic matrix metalloproteinase-2 selective inhibitor--synthesis and pharmacodynamic and pharmacokinetic analysis. Journal of medicinal chemistry vol. 51,5 (2008): 1406-14.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C₇H₁₅N₂O₄P

[ Molecular Weight ]:
222.179

[ Exact Mass ]:
222.076950

[ PSA ]:
122.46000

[ LogP ]:
-2.04

[ Index of Refraction ]:
1.544

Related Compounds

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