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Vofopitant (GR 205171) (Synonyms: GR 205171)

Catalog No.GC33747

Vofopitant (GR 205171) is potent tachykinin NK1 receptor antagonist, with pKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK1 receptor, respectively.

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Vofopitant (GR 205171) Chemical Structure

Cas No.: 168266-90-8

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1mg
$143.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Kinase experiment:

Tachykinin NK1 receptor binding assays are carried out in an assay volume of 200 μL, consisting of 50 μL of wash buffer (containing HEPES (50 mM) and MnC12 (3 mM), pH 7.4) or test compound (Vofopitant), 100 μL membrane suspension (3-5 μg of protein) in HEPES assay buffer (composition as above, but containing bacitracin, 80 μg/mL], leupeptin, 8 μg/mL], phosphoramidon, 2 μM and bovine serum albumin, 0.04%) and 50 μL of [3H]substance P (0.7-1.0 nM final concentration). The incubation is carried out at room temperature for 40 min. Non-specific binding is defined by the addition of CP-99,994 (1 μM)[1].

Animal experiment:

Effect of NK1 receptor antagonists administered i.p. on cortical [5-HT]ext of wild-type mice. Following collection of four baseline dialysate samples, freely moving wild-type mice are administered with either the vehicle or various NK1 receptor antagonists, Vofopitant (30 mg/kg; i.p.) or L733060 (40 mg/kg; i.p.). Dialysate samples are collected for a 0-120 min post-treatment period[3].

References:

[1]. Gardner CJ, et al. GR205171: a novel antagonist with high affinity for the tachykinin NK1 receptor, and potent broad-spectrum anti-emetic activity. Regul Pept. 1996 Aug 27;65(1):45-53.
[2]. Loiseau F, et al. Antidepressant-like effects of agomelatine, melatonin and the NK1 receptor antagonist GR205171 in impulsive-related behaviour in rats. Psychopharmacology (Berl). 2005 Oct;182(1):24-32. Epub 2005 Sep 29.
[3]. Guiard BP, et al. Blockade of substance P (neurokinin 1) receptors enhances extracellular serotonin when combined with a selective serotonin reuptake inhibitor: an in vivo microdialysis study in mice. J Neurochem. 2004 Apr;89(1):54-63.

Background

Vofopitant is potent tachykinin NK1 receptor antagonist, with pKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK1 receptor, respectively.

Vofopitant is potent tachykinin NK1 receptor antagonist, with pKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK1 receptor, respectively. Vofopitant less potently inhibits rat 5-HT1A, bovine 5-HT1D, rat 5-HT2A, rat Histamine H1, guinea-pig Histamine H2 and rat Ca2+ channel, with pKis of 6.3, 6.6, 6.5, 6.5, 6.6, and 5.6, respectively. Vofopitant shows negligible affinity at NK2 and NK3, with pIC50 of <5.0[1]. GR205171 (300 µM) potentiates the effects of paroxetine on cortical [5-HT]ext, and inhibits paroxetine-induced increase in [5-HT]ext in the dorsal raphe nucleus[3].

Vofopitant (GR205171, 30 mg/kg, s.c.) increases the number of choices of the 25-s delayed reward in a T-maze[2]. Vofopitant (GR205171, 30 mg/kg, i.p.) increases the extracellular 5-HT levels in the frontal cortex of paroxetine-treated wild-type mice, rather than in wild-type mice and paroxetine-treated NK1 receptor knockout mice[3].

[1]. Gardner CJ, et al. GR205171: a novel antagonist with high affinity for the tachykinin NK1 receptor, and potent broad-spectrum anti-emetic activity. Regul Pept. 1996 Aug 27;65(1):45-53. [2]. Loiseau F, et al. Antidepressant-like effects of agomelatine, melatonin and the NK1 receptor antagonist GR205171 in impulsive-related behaviour in rats. Psychopharmacology (Berl). 2005 Oct;182(1):24-32. Epub 2005 Sep 29. [3]. Guiard BP, et al. Blockade of substance P (neurokinin 1) receptors enhances extracellular serotonin when combined with a selective serotonin reuptake inhibitor: an in vivo microdialysis study in mice. J Neurochem. 2004 Apr;89(1):54-63.

Chemical Properties

Cas No. 168266-90-8 SDF
Synonyms GR 205171
Canonical SMILES COC1=C(CN[C@@H]2[C@H](C3=CC=CC=C3)NCCC2)C=C(N4C(C(F)(F)F)=NN=N4)C=C1
Formula C21H23F3N6O M.Wt 432.44
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.3125 mL 11.5623 mL 23.1246 mL
5 mM 0.4625 mL 2.3125 mL 4.6249 mL
10 mM 0.2312 mL 1.1562 mL 2.3125 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 13 reference(s) in Google Scholar.)

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