TRIM - CAS 25371-96-4
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C10H7F3N2
Molecular Weight:
212.17
COA:
Inquire
Targets:
Nitric oxide synthase (NOS)
Description:
TRIM is a potent inhibitor of neuronal and inducible NO synthases (nNOS and iNOS), but exhibits lower affinity for the endothelial isoform (IC50 = 28.2, 27.0 and 1057.5 μM, respectively).
Brife Description:
nNOS and iNOS inhibitor
Purity:
≥99% by HPLC
Synonyms:
1-(2-Trifluoromethylphenyl)imidazole; 1-[2-(Trifluoromethyl)phenyl]imidazole
MSDS:
Inquire
InChIKey:
WZBWBNCQUTXYEL-UHFFFAOYSA-N
InChI:
InChI=1S/C10H7F3N2/c11-10(12,13)8-3-1-2-4-9(8)15-6-5-14-7-15/h1-7H
Canonical SMILES:
C1=CC=C(C(=C1)C(F)(F)F)N2C=CN=C2
1.The TLR4-NOS1-AP1 signaling axis regulates macrophage polarization.
Srivastava M;Saqib U;Naim A;Roy A;Liu D;Bhatnagar D;Ravinder R;Baig MS Inflamm Res. 2017 Apr;66(4):323-334. doi: 10.1007/s00011-016-1017-z. Epub 2016 Dec 24.
OBJECTIVE: ;Macrophages polarize to proinflammatory M1 or anti-inflammatory M2 states with distinct physiological functions. This transition within the M1-M2 phenotypes decides the nature, duration and severity of an inflammatory response. Although there is a substantial understanding of the fate of these phenotypes, the underlying molecular mechanism of transition within the M1-M2 phenotypes is not well understood. We have investigated the role of neuronal nitric oxide synthase (NOS1)-mediated regulation of activator protein 1 (AP-1) transcription factor in macrophages as a critical effector of macrophage phenotypic change.;MATERIALS AND METHODS: ;Raw 264.7 and THP1 macrophages were stimulated with LPS (250 ng/ml) to activate the inflammatory signaling pathway. We analyzed the effect of pharmacological NOS1 inhibitor: TRIM (1-(2- Trifluoromethylphenyl) imidazole) on LPS-induced inflammatory response in macrophages.;RESULTS: ;We determined that NOS1-derived nitric oxide (NO) facilitate Fos and Jun interaction which induces IL-12 & IL-23 expression. Pharmacological inhibition of NOS1 inhibits ATF2 and Jun dimer. Switching of Fos and Jun dimer to ATF2 and Jun dimerization controls phenotype transition from IL-12;high; IL-23;high; IL-10;low; to IL-12;low; IL-23;low;IL-10;high; phenotype, respectively.
2.Inhibition of nitric oxide synthase by 1-(2-trifluoromethylphenyl) imidazole (TRIM) in vitro: antinociceptive and cardiovascular effects.
Handy RL;Harb HL;Wallace P;Gaffen Z;Whitehead KJ;Moore PK Br J Pharmacol. 1996 Sep;119(2):423-31.
1. The ability of a range of substituted imidazole compounds to inhibit mouse cerebellar neuronal nitric oxide synthase (nNOS), bovine aortic endothelial NOS (eNOS) and inducible NOS (iNOS) from lungs of endotoxin-pretreated rats was investigated. In each case the substrate (L-arginine) concentration employed was 120 nM. 2. 1-(2-Trifluoromethylphenyl) imidazole (TRIM) was a relatively potent inhibitor of nNOS and iNOS (IC50S of 28.2 microM and 27.0 microM respectively) but was a relatively weak inhibitor of eNOS (IC50, 1057.5 microM). The parent compound, imidazole, was a weak inhibitor of all three NOS isoforms (IC50S: nNOS, 290.6 microM; eNOS, 101.3 microM; iNOS, 616.0 microM). Substitution of imidazole with a phenyl group to yield I-phenylimidazole (PI) resulted in an isoform non-selective increase in inhibitory potency (IC50S: nNOS, 72.1 microM; eNOS, 86.9 microM; iNOS, 53.9 microM). Further substitution of the attached phenyl group resulted in an increase in nNOS and a decrease in eNOS inhibitory potency as in TRIM, 1-chlorophenylimidazole (CPI; IC50S: nNOS, 43.4 microM; eNOS, 392.3 microM; iNOS, 786.5 microM) and 1-(2,3,5,6-tetrafluorophenyl) imidazole (TETRA-FPI; IC50S; nNOS, 56.
3.Positive N-methyl-D-aspartate receptor modulation by selective glycine transporter-1 inhibition in the rat dorsal spinal cord in vivo.
Whitehead KJ;Pearce SM;Walker G;Sundaram H;Hill D;Bowery NG Neuroscience. 2004;126(2):381-90.
In this study we have employed the selective glycine transporter-1 (GlyT-1) and GlyT-2 transporter inhibitors R-(-)-N-methyl-N-[3-[(4-trifluoromethyl)phenoxy]-3-phenyl-propyl]glycine (1:1) lithium salt (Org 24598) and 4-benzyloxy-3,5-dimethoxy-N-[1-(dimethylaminocyclopently)methyl]benzamide (Org 25543), respectively, and microdialysis perfusion to determine the effect of GlyT transporter inhibition on extracellular amino acid concentrations in the lumbar dorsal spinal cord of the halothane-anaesthetised rat. Reverse dialysis of Org 24598 (0.1-10 microM) induced a concentration-related increase in extracellular glycine accompanied by a progressive increase in citrulline, but not aspartate, glutamate or GABA, efflux. Org 25543 (10 microM) by the same route induced a similar increase in glycine levels without affecting the efflux of other amino acids quantified. To test the hypothesis that the increase in citrulline efflux resulted from activation of the N-methyl-D-aspartate receptor (NMDA-R)/nitric oxide synthase (NOS) signalling cascade, the sensitivity was determined of GlyT-1 inhibition-induced effects to NMDA-R antagonism or NOS inhibition. Co-administration by reverse dialysis of the selective NMDA-R channel blocker MK-801 (0.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Nitric oxide synthase (NOS) Products


CAS 150403-89-7 L-NIL hydrochloride

L-NIL hydrochloride
(CAS: 150403-89-7)

L-NIL hydrochloride is a nitric oxide synthase inhibitor with IC50 value of 3.3 μM.

FK-330
(CAS: 442198-67-6)

FK-330 is a novel inducible nitric oxide synthase inhibitor for preventing ischemia and reperfusion injury in rat liver transplantation.

CAS 1937-19-5 Aminoguanidine hydrochloride

Aminoguanidine hydrochloride
(CAS: 1937-19-5)

Aminoguanidine hydrochloride is the hydrochloride salt form of Aminoguanidine. Aminoguanidine is an inhibitor that has an irreversible function on iNOS with sel...

CAS 157254-60-9 1,4-PB-ITU dihydrobromide

1,4-PB-ITU dihydrobromide
(CAS: 157254-60-9)

The dihydrobromide salt form of 1,4-PB-ITU, a carbamimidoylsulfanyl derivative, has been found to be an iNOS and nNOS inhibitor that has poor membrane permeabil...

CAS 1216722-25-6 BYK 191023 dihydrochloride

BYK 191023 dihydrochloride
(CAS: 1216722-25-6)

BYK 191023 dihydrochloride is a potent and selective inhibitor of inducible nitric oxide synthase (iNOS) (IC50 = 86, 17000, 162000 nM for iNOS, nNOS and eNOS, r...

CAS 137361-05-8 Nω-Propyl-L-arginine hydrochloride

Nω-Propyl-L-arginine hydrochloride
(CAS: 137361-05-8)

Nω-Propyl-L-arginine hydrochloride is a neuronal selective nitric oxide synthase inhibitor and a potent and selective inhibitor of NOS1 (nNOS) (Ki = 57 nM) with...

CAS 4269-97-0 S-Isopropylisothiourea hydrobromide

S-Isopropylisothiourea hydrobromide
(CAS: 4269-97-0)

S-Isopropylisothiourea hydrobromide is the hydrobromide form of S-Isopropylisothiourea, which is a potent non-selective nitric oxide synthase (NOS) inhibitor. I...

CAS 2942-42-9 7-Nitroindazole

7-Nitroindazole
(CAS: 2942-42-9)

7-Nitroindazole is a nitric oxide synthase inhibitor.

Chemical Structure

CAS 25371-96-4 TRIM

Quick Inquiry

Verification code

Featured Items