2024年11月3日发(作者：乌鸿朗)

Peptides, Inhibitors, Agonists

Product Data Sheet

Product Name:

Cat. No.:

Chemical Name:

CB−1158 (INCB01158)

GC33106

CHEMICAL PROPERTIES

Cas No.: 2095732-06-0

Molecular Formula:

Molecular Weight:

Storage:

Solubility:

Chemical Structure:

C

11

H

22

BN

3

O

5

287.12

Powder

Soluble in DMSO

Background

CB−1158 is a potent and orally bioavailable inhibitor of arginase, with IC50s of 86 and 296 nM for recombinant human arginase 1 and

2, respectively.

CB−1158 is a potent and orally−bioavailable inhibitor of arginase, with IC50s of 86 and 296 nM for recombinant human arginase 1 and

2, respectively. CB−1158 inhibits native rginase 1 (Arg1) in human granulocyte, erythrocyte, and hepatocyte lysate with IC50s of 178

nM, 116 nM and 158 nM, respectively, and blocks Arg1 in cancer patient plasma (IC50, 122 nM). CB−1158 also exhibits potent

inhibitory activity against arginase in human HepG2, K562 cell lines and primary human hepatocytes with IC50s of 32, 139, 210 μM,

respectively. CB−1158 show no effect on NOS. In addition, CB−1158 is not directly cytotoxic to murine cancer cell lines[1].

CB−1158 (100 mg/kg, p.o., twice per day) increases the number of tumor−infiltrating cytotoxic cells and decreases myeloid cells in

mice. CB−1158 in combination with PD−L1 blockade or gemcitabine inhibits tumor growth in mice bearing CT26 cancer cells[1].

References:

[1]. Steggerda SM, et al. Inhibition of arginase by CB-1158 blocks myeloid cell-mediated immune suppression in the tumor

microenvironment. J Immunother Cancer. 2017 Dec 19;5(1):101.

Research Update

1. Effect of Hydrofluoric Acid Concentration and Etching Time on Bond Strength to Lithium Disilicate Glass Ceramic. Oper Dent. 2017

Nov/Dec;42(6):606-615. doi: 10.2341/16-215-L. Epub 2017 Jul 14. PMID:28708007

Abstract

The aim of this study was to evaluate the influence of different concentrations of hydrofluoric acid (HF) associated with varied etching

times on the microshear bond strength (μSBS) of a resin cement to a lithium disilicate glass ceramic. Two hundred seventy-five

ceramic blocks (IPS Press [EMX], Ivoclar Vivadent), measuring 8 mm × 3 mm thickness, were randomly distributed into five

groups according to the HF concentrations (n=50): 1%, 2.5%, 5%, 7.5%, and 10%.

2. Does acid etching morphologically and chemically affect lithium disilicate glass ceramic surfaces? J Appl Biomater Funct Mater.

2017 Jan 26;15(1):e93-e100. doi: 10.5301/jabfm.5000303. PMID:27647389

Abstract

BACKGROUND: This study evaluated the surface morphology, chemical composition and adhesiveness of lithium disilicate glass

ceramic after acid etching with hydrofluoric acid or phosphoric S: Lithium disilicate glass ceramic specimens polished by

600-grit silicon carbide paper were subjected to one or a combination of these surface treatments: airborne particle abrasion with 50-

μm alumina (AA), etching with 5% hydrofluoric acid (HF) or 36% phosphoric acid (Phos), and application of silane coupling agent (Si).

3. Fatigue failure load of feldspathic ceramic crowns after hydrofluoric acid etching at different concentrations. J Prosthet Dent. 2018

Feb;119(2):278-285. doi: 10.1016/nt.2017.03.021. Epub 2017 May 26. PMID:28552291

Abstract

STATEMENT OF PROBLEM: Hydrofluoric acid etching modifies the cementation surface of ceramic restorations, which is the same

surface where failure is initiated. Information regarding the influence of hydrofluoric acid etching on the cyclic loads to failure of ceramic

crowns is E: The purpose of this in vitro study was to evaluate the influence of different hydrofluoric acid

concentrations on the fatigue failure loads of feldspathic ceramic crowns.

2024年11月3日发(作者：乌鸿朗)

Peptides, Inhibitors, Agonists

Product Data Sheet

Product Name:

Cat. No.:

Chemical Name:

CB−1158 (INCB01158)

GC33106

CHEMICAL PROPERTIES

Cas No.: 2095732-06-0

Molecular Formula:

Molecular Weight:

Storage:

Solubility:

Chemical Structure:

C

11

H

22

BN

3

O

5

287.12

Powder

Soluble in DMSO

Background

CB−1158 is a potent and orally bioavailable inhibitor of arginase, with IC50s of 86 and 296 nM for recombinant human arginase 1 and

2, respectively.

CB−1158 is a potent and orally−bioavailable inhibitor of arginase, with IC50s of 86 and 296 nM for recombinant human arginase 1 and

2, respectively. CB−1158 inhibits native rginase 1 (Arg1) in human granulocyte, erythrocyte, and hepatocyte lysate with IC50s of 178

nM, 116 nM and 158 nM, respectively, and blocks Arg1 in cancer patient plasma (IC50, 122 nM). CB−1158 also exhibits potent

inhibitory activity against arginase in human HepG2, K562 cell lines and primary human hepatocytes with IC50s of 32, 139, 210 μM,

respectively. CB−1158 show no effect on NOS. In addition, CB−1158 is not directly cytotoxic to murine cancer cell lines[1].

CB−1158 (100 mg/kg, p.o., twice per day) increases the number of tumor−infiltrating cytotoxic cells and decreases myeloid cells in

mice. CB−1158 in combination with PD−L1 blockade or gemcitabine inhibits tumor growth in mice bearing CT26 cancer cells[1].

References:

[1]. Steggerda SM, et al. Inhibition of arginase by CB-1158 blocks myeloid cell-mediated immune suppression in the tumor

microenvironment. J Immunother Cancer. 2017 Dec 19;5(1):101.

Research Update

1. Effect of Hydrofluoric Acid Concentration and Etching Time on Bond Strength to Lithium Disilicate Glass Ceramic. Oper Dent. 2017

Nov/Dec;42(6):606-615. doi: 10.2341/16-215-L. Epub 2017 Jul 14. PMID:28708007

Abstract

The aim of this study was to evaluate the influence of different concentrations of hydrofluoric acid (HF) associated with varied etching

times on the microshear bond strength (μSBS) of a resin cement to a lithium disilicate glass ceramic. Two hundred seventy-five

ceramic blocks (IPS Press [EMX], Ivoclar Vivadent), measuring 8 mm × 3 mm thickness, were randomly distributed into five

groups according to the HF concentrations (n=50): 1%, 2.5%, 5%, 7.5%, and 10%.

2. Does acid etching morphologically and chemically affect lithium disilicate glass ceramic surfaces? J Appl Biomater Funct Mater.

2017 Jan 26;15(1):e93-e100. doi: 10.5301/jabfm.5000303. PMID:27647389

Abstract

BACKGROUND: This study evaluated the surface morphology, chemical composition and adhesiveness of lithium disilicate glass

ceramic after acid etching with hydrofluoric acid or phosphoric S: Lithium disilicate glass ceramic specimens polished by

600-grit silicon carbide paper were subjected to one or a combination of these surface treatments: airborne particle abrasion with 50-

μm alumina (AA), etching with 5% hydrofluoric acid (HF) or 36% phosphoric acid (Phos), and application of silane coupling agent (Si).

3. Fatigue failure load of feldspathic ceramic crowns after hydrofluoric acid etching at different concentrations. J Prosthet Dent. 2018

Feb;119(2):278-285. doi: 10.1016/nt.2017.03.021. Epub 2017 May 26. PMID:28552291

Abstract

STATEMENT OF PROBLEM: Hydrofluoric acid etching modifies the cementation surface of ceramic restorations, which is the same

surface where failure is initiated. Information regarding the influence of hydrofluoric acid etching on the cyclic loads to failure of ceramic

crowns is E: The purpose of this in vitro study was to evaluate the influence of different hydrofluoric acid

concentrations on the fatigue failure loads of feldspathic ceramic crowns.