GR 159897

Non-peptide, potent NK2 antagonist CAS# 158848-32-9

GR 159897

Catalog No. BCC7001----Order now to get a substantial discount!

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Chemical structure

GR 159897

3D structure

Chemical Properties of GR 159897

Cas No. 158848-32-9 SDF Download SDF
PubChem ID 3570748 Appearance Powder
Formula C23H27FN2O2S M.Wt 414.54
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 50 mM in DMSO and to 10 mM in ethanol
Chemical Name 3-[2-[4-(benzenesulfinylmethyl)-4-methoxypiperidin-1-yl]ethyl]-5-fluoro-1H-indole
SMILES COC1(CCN(CC1)CCC2=CNC3=C2C=C(C=C3)F)CS(=O)C4=CC=CC=C4
Standard InChIKey BANYJBHWTOJQDU-UHFFFAOYSA-N
Standard InChI InChI=1S/C23H27FN2O2S/c1-28-23(17-29(27)20-5-3-2-4-6-20)10-13-26(14-11-23)12-9-18-16-25-22-8-7-19(24)15-21(18)22/h2-8,15-16,25H,9-14,17H2,1H3
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of GR 159897

DescriptionA potent, selective, non-peptide, orally active neurokinin NK2 receptor antagonist. Competes for binding of [3H]GR100679 to hNK2-transfected CHO cells with a pKi of 9.5. Inhibits NK2 receptor-mediated contraction of guinea pig trachea with a pA2 of 8.7. Anxiolytic in vivo.

GR 159897 Dilution Calculator

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GR 159897 Molarity Calculator

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Preparing Stock Solutions of GR 159897

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.4123 mL 12.0616 mL 24.1231 mL 48.2462 mL 60.3078 mL
5 mM 0.4825 mL 2.4123 mL 4.8246 mL 9.6492 mL 12.0616 mL
10 mM 0.2412 mL 1.2062 mL 2.4123 mL 4.8246 mL 6.0308 mL
50 mM 0.0482 mL 0.2412 mL 0.4825 mL 0.9649 mL 1.2062 mL
100 mM 0.0241 mL 0.1206 mL 0.2412 mL 0.4825 mL 0.6031 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on GR 159897

Synthesis of new C-25 and C-26 steroidal acids as potential ligands of the nuclear receptors DAF-12, LXR and GR.[Pubmed:28300583]

Steroids. 2017 May;121:40-46.

A new methodology to obtain C-25 and C-26 steroidal acids starting from pregnenolone is described. Construction of the side chain was achieved by applying the Mukaiyama aldol reaction with a non-hydrolytic work-up to isolate the trapped silyl enol ether with higher yields. Using this methodology we synthesized three new steroidal acids as potential ligands of DAF-12, Liver X and Glucocorticoid nuclear receptors and studied their activity in reporter gene assays. Our results show that replacement of the 21-CH3 by a 20-keto group in the side chains of the cholestane scaffold of DAF-12 or Liver X receptors ligands causes the loss of the activity.

Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexah ydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methano ne (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist.[Pubmed:28368581]

J Med Chem. 2017 Apr 27;60(8):3405-3421.

The nonselective glucocorticoid receptor (GR) antagonist mifepristone has been approved in the U.S. for the treatment of selected patients with Cushing's syndrome. While this drug is highly effective, lack of selectivity for GR leads to unwanted side effects in some patients. Optimization of the previously described fused azadecalin series of selective GR antagonists led to the identification of CORT125134, which is currently being evaluated in a phase 2 clinical study in patients with Cushing's syndrome.

Recruitment of bone marrow CD11b(+)Gr-1(+) cells by polymeric nanoparticles for antigen cross-presentation.[Pubmed:28317931]

Sci Rep. 2017 Mar 20;7:44691.

The objective of this study was to investigate the function of poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) on the activation of antigen-specific CD8(+) T cell responses via the CD11b(+)Gr(-)1(+) myeloid subpopulations in murine bone marrow (BM). PLGA NPs containing ovalbumin (OVA) were fabricated by the double-emulsion method. The CD11b(+)Gr-1(low)Ly-6C(high) and CD11b(+)Gr-1(high)Ly-6C(low) subsets from mice bone marrow were sorted and treated with the PLGA/OVA NPs, followed by co-culture with the carboxyfluorescein succinimidyl ester (CFSE)-labelled OT-I CD8(+) cells. Co-culture of OT-I CD8(+) T cells with PLGA/OVA NPs-primed CD11b(+)Gr-1(+) subsets upregulated the expression of IL-2, TNF-alpha, INF-gamma, granzyme B, and perforin, resulting in proliferation of CD8(+) T cells and differentiation into effector cytotoxic T lymphocytes (CTLs). In vivo proliferation of CFSE-labelled OT-I CD8(+) cells in response to OVA was also obtained in the animals immunized with PLGA/OVA NPs. The results presented in this study demonstrate the ability of polymeric NPs to recruit two CD11b(+)Gr(-)1(+) myeloid subsets for effective presentation of exogenous antigen to OT-I CD8(+) T cells in the context of major histocompatibility complex (MHC) class I, leading to an induction of antigen-specific cell proliferation and differentiation into effector cells.

Muscle-specific downregulation of GR levels inhibits adipogenesis in porcine intramuscular adipocyte tissue.[Pubmed:28360421]

Sci Rep. 2017 Mar 30;7(1):510.

Intramuscular adipose is conducive to good pork quality, whereas subcutaneous adipose is considered as waste in pig production. So uncovering the regulation differences between these two adiposes is helpful to tissue-specific control of fat deposition. In this study, we found the sensitivity to glucocorticoids (GCs) was lower in intramuscular adipocytes (IMA) compared with subcutaneous adipocytes (SA). Comparison of glucocorticoid receptor (GR) revealed that IMA had lower GR level which contributed to its reduced GCs sensitivity. Higher methylation levels of GR promotor 1-C and 1-H were detected in IMA compared with SA. GR expression decrease was also found in adipocytes when treated with muscle conditioned medium (MCM) in vitro, which resulted in significant inhibition of adipocytes proliferation and differentiation. Since abundant myostatin (MSTN) was detected in MCM by ELISA assay, we further investigated the effect of this myokine on adipocytes. MSTN treatment suppressed adipocytes GR expression, cell proliferation and differentiation, which mimicked the effects of MCM. The methylation levels of GR promotor 1-C and 1-H were also elevated after MSTN treatment. Our study reveals the role of GR in muscle fiber inhibition on intramuscular adipocytes, and identifies myostatin as a muscle-derived modulator for adipose GR level.

GR159897, a potent non-peptide antagonist at tachykinin NK2 receptors.[Pubmed:7713168]

Eur J Pharmacol. 1995 Jan 16;272(2-3):241-8.

GR159897 ((R)-1-[2-(5-fluoro-1H-indol-3-yl)ethyl]-4-methoxy-4- [(phenylsulfinyl)methyl]piperidine) is a novel, highly potent and selective non-peptide antagonist at tachykinin NK2 receptors. GR159897 inhibited binding of the NK2 receptor antagonist radioligand [3H]cyclohexylcarbonyl-Gly-Ala-(D)Trp-Phe-NMe2 ([3H]GR100679) to human ileum NK2 receptors transfected into Chinese hamster ovary cells (pKi 9.5) and to rat colon membranes (pKi 10.0). GR159897 was a competitive antagonist of contractions induced by the NK2 receptor agonist [Lys3,Gly8-R-gamma-lactam-Leu9]neurokinin A-(3-10) (GR64349) in guinea-pig trachea (pA2 8.7), and had negligible activity at human NK1 receptors transfected into Chinese hamster ovary cells (pKi 5.3), NK1 receptors in guinea-pig trachea (pKB < 5) or NK3 receptors in guinea-pig cerebral cortex (pKi < 5). In vivo, in the anaesthetised guinea-pig, GR159897 (0.12 mg.kg-1 i.v.) potently antagonised bronchoconstriction induced by GR64349 (dose-ratio = 28), with a long duration of action (3 h). GR159897 should be a useful tool for studying the physiological and pathophysiological role of tachykinin NK2 receptor activation.

The anxiolytic-like activity of GR159897, a non-peptide NK2 receptor antagonist, in rodent and primate models of anxiety.[Pubmed:8545524]

Psychopharmacology (Berl). 1995 Sep;121(2):186-91.

The non-peptide NK2 receptor antagonist, GR159897, was evaluated in two putative models of anxiety, the mouse light-dark box and the marmoset human intruder response test. Effects were compared to the structurally dissimilar NK2 antagonist, (+/-) SR48968 and the benzodiazepines, diazepam and chlordiazepoxide. GR159897 (0.0005-50 micrograms/kg SC) caused significant and dose-dependent increases in the amount of time mice spent in the more aversive light compartment of the light-dark box, with no effect on locomotor activity. (+/-)SR48968 (0.0005-0.5 microgram/kg SC) and diazepam (1-1.75 mg/kg SC), also increased time spent in the light compartment, without effect on locomotor activity. In the marmoset human intruder response test, GR159897 (0.2-50 micrograms/kg SC) significantly increased the amount of time marmosets spent at the front of the cage during confrontation with a human observer ("threat"). Similar effects were produced by (+/-)SR48968 (10-50 micrograms/kg SC) and chlordiazepoxide (0.3-3.0 mg/kg SC). These results provide further evidence, in both rodent and primate species, for the ability of NK2 antagonists to restore behaviours which have been suppressed by novel aversive environments. Such effects indicate that NK2 antagonists may have anxiolytic activity.

Description

GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects.

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