TOK 8801 105963-46-0 GlpBio

www.glpbio.com

Product Data Sheet

Product Name: Cat. No.: Chemical Name:

TOK−8801 GC31957

CHEMICAL PROPERTIES Cas No.: 105963-46-0 Molecular Formula: Molecular Weight: Storage: Solubility:

Chemical Structure:

C17H21N3OS 315.43 Powder

Soluble in DMSO

Background

TOK−8801 is a synthesized dihydroimidazothiazole carboxamide and is under development as an immunomodulator.

TOK−8801 is a synthesized dihydroimidazothiazole carboxamide and is under development as an immunomodulator. TOK−8801 augments the in vitro anti−SRBC PFC response of murine splenocytes in a bell−shaped manner. The stimulatory effect of TOK−8801 is observed at concentrations of 2.5×10−7 to 2.5×10−5 M and is diminished at 10−4 M. The cell−viability is not altered during the culture with TOK−8801 at any doses used in this experiment (10−7 to 10−4 M). TOK−8801 enhances the 3H−TdR uptake of these responses in a bell−shaped manner, and effective concentrations of TOK−8801 are 10−7 to 10−5 M[1].

The anti−SRBC PFC response per spleen, which is prominently lowered by restraint−stress (P＜0.05), is significantly restored by the administration of TOK−8801 (0.5 mg/kg, P＜0.05). The number of total splenic lymphocytes in restraint−stress is decreased, but there are no significant changes in the number of total splenic lymphocytes by the treatment with TOK−8801[1]. When TOK−8801 is administered orally at doses of 0.1 to 10 mg/kg, the number of plaque forming cell (PFC) significantly decreases or tends to decrease. Treatment of TOK−8801 at doses of 0.1 to 1 mg/kg causes significant suppression in the delayed−type hypersensitivity (DTH) reaction induced in high responder[2]. References:

[1]. Fujiwara M, et al. Immunomodulatory activity of the newly synthesized compound TOK-8801 (N-(2-phenylethyl)-3,6,6-trimethyl-5,6-dihydroimidazo[2,1-b]thiazole-2- carboxamide). Jpn J Pharmacol. 1989 Dec;51(4):549-54.

[2]. Shibata K, et al. Immunomodulatory effect of a newly synthesized compound, TOK-8801 (N-(2-phenylethyl)-3,6,6-trimethyl-5,6-dihydroimidazo [2,1-b]thiazole-2-carboxamide) on antibody production in vivo and delayed-type hypersensitivity in mice. Int J Immunopharmacol. 1990;12(5):497-502.

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 e.max 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 acid.METHODS: 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/j.prosdent.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 lacking.PURPOSE: 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.