128837-71-8

Basic information

• Product Name: PKSI 527
• Synonyms: Benzeneaceticacid,4-[[2-[[[4-(aminomethyl)cyclohexyl]carbonyl]amino]-1-oxo-3-phenylpropyl]amino]-,monohydrochloride, [1(S)-trans]-; PKSI 527
• CAS NO: 128837-71-8
• Molecular Formula: C25H31N3O4.ClH
• Molecular Weight: 473.998
• Mol File: 128837-71-8.mol
• Article Data: 0

Chemical Properties

• Boiling Point: 763.1°Cat760mmHg
• Flash Point: 415.3°C
• Appearance: /
• Density: g/cm³
• Vapor Pressure: 1.74E-24mmHg at 25°C
• Storage Temp.: -20°C
• Solubility: Soluble in Water (5 mg/ml)
• Stability: Stable for 1 year from date of purchase as supplied. Solutions in water may be stored at -20°C for up to 3 months.
• CAS DataBase Reference: PKSI 527(CAS DataBase Reference)
• NIST Chemistry Reference: PKSI 527(128837-71-8)
• EPA Substance Registry System: PKSI 527(128837-71-8)

Safety Data

• Hazardous Substances Data: 128837-71-8(Hazardous Substances Data)

Usage

Description

PKSI 527 is a selective plasma kallikrein inhibitor with a Ki value of 0.81 μM, which can be used for affinity purification of kallikrein. It has the potential to produce antithrombotic effects when synergized with NO donors and has been shown to suppress collagen-induced arthritis in mouse models.

Uses

Used in Pharmaceutical Industry:
PKSI 527 is used as a plasma kallikrein inhibitor for its potential therapeutic applications in treating conditions related to abnormal blood clotting and inflammation.
Used in Research Applications:
PKSI 527 is used as a research tool for affinity purification of kallikrein, enabling scientists to study the function and regulation of this enzyme in various biological processes.
Used in Ex-vivo Antithrombotic Testing:
PKSI 527 is used in combination with NO donors to evaluate its antithrombotic effects in ex-vivo models, providing valuable insights into its potential use in the development of new antithrombotic therapies.
Used in Arthritis Treatment Research:
PKSI 527 is used in mouse models of collagen-induced arthritis to study its potential as a therapeutic agent for the treatment of arthritis and related inflammatory conditions.

References

Wanaka et al. (1992), Synthesis of trans-4-aminomethylcyclohexanecarbonyl-L- and –D-phenylalanine-4-carboxymethylanilide and examination of their inhibitory activity against plasma kallikrein;? ?Chem. Pharm. Bull., 40 1814 Tada et al. (2001), Isolation of plasma kallikrein by high efficiency affinity chromatography and its characterization; Chem. Pharm. Bull., 24 520 Ikarugi et al. (2005), Synergistic antithrombotic effect of a combination of NO donor and plasma kallikrein inhibitor; Thromb. Res., 116 403 Fujimori et al. (1993), Effects of a highly selective plasma kallikrein inhibitor on collagen-induced arthritis in mice; Agents Actions, 39 42

InChI:InChI=1/C25H31N3O4.ClH/c26-16-19-6-10-20(11-7-19)24(31)28-22(14-17-4-2-1-3-5-17)25(32)27-21-12-8-18(9-13-21)15-23(29)30;/h1-5,8-9,12-13,19-20,22H,6-7,10-11,14-16,26H2,(H,27,32)(H,28,31)(H,29,30);1H/t19?,20?,22-;/m0./s1