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Vofopitant
🥰Excellent
Catalog No. T13329Cas No. 168266-90-8
Alias GR 205171
Vofopitant (GR 205171) is a potent NK1 receptor antagonist with anxiolytic and antiemetic activity for the study of post-traumatic stress disorder (PTSD).
Vofopitant
🥰Excellent
Purity: 97.61%
Catalog No. T13329Alias GR 205171Cas No. 168266-90-8
Vofopitant (GR 205171) is a potent NK1 receptor antagonist with anxiolytic and antiemetic activity for the study of post-traumatic stress disorder (PTSD).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $100 | In Stock | |
| 5 mg | $247 | In Stock | |
| 10 mg | $367 | In Stock | |
| 25 mg | $595 | In Stock | |
| 50 mg | $862 | In Stock | |
| 100 mg | $1,160 | In Stock | |
| 500 mg | $2,320 | In Stock |
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Rolapitant
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Rolapitant (SCH619734) Hydrochloride is the hydrochloride salt form of rolapitant, an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of SP with the NK1-receptor plays a key role in the induction of nausea and vomiting caused by emetogenic cancer chemotherapy. Compared to other NK1-receptor antagonists, rolapitant has both a more rapid onset of action and a much longer half-life.
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Fosaprepitant dimeglumine
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Vofopitant dihydrochloride
Vofopitant 2HCl, GR 205171A
T13329L168266-51-1In house
Vofopitant dihydrochloride (GR 205171A) is an orally available, selective tachykinin NK1 receptor antagonist that inhibits [3H]SP binding to NK1 with pKi values of 9.5 and 10.6, respectively. It is a potential compound for the treatment of pathological vomiting.
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Purity:97.61%
ee:97.524%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | Vofopitant (GR 205171) is a potent NK1 receptor antagonist with anxiolytic and antiemetic activity for the study of post-traumatic stress disorder (PTSD). |
| Targets&IC50 | NK1 receptor (rat):9.5 (pKi), NK1 receptor (ferret):9.8(pKi), NK1 receptor (human):10.6 (pKi) |
| In vitro | Co-administration of paroxetine (4 mg/kg; i.p.) with the NK1 receptor antagonists, Vofopitant/GR205171 (30 mg/kg; i.p.) or L733060 (40 mg/kg; i.p.), potentiated the effects of paroxetine on cortical [5-HT]ext in wild-type mice, whereas GR205171 (30 mg/kg; i.p.) had no effect on paroxetine-induced increase in cortical [5-HT]ext in NK1 receptor knock-out mice. When GR205171 (300 micro mol/L) was perfused by 'reverse microdialysis' into the dorsal raphe nucleus, it potentiated the effects of paroxetine on cortical [5-HT]ext, and inhibited paroxetine-induced increase in [5-HT]ext in the dorsal raphe nucleus[2]. |
| In vivo | In a T-maze experiment, Vofopitant (GR205171, 30 mg/kg, subcutaneously) enhances the selection of a 25-second delayed reward[3]. Furthermore, when administered intraperitoneally at the same dosage, Vofopitant elevates extracellular serotonin (5-HT) levels in the frontal cortex of wild-type mice treated with paroxetine, but not in untreated wild-type or in NK1 receptor knockout mice also treated with paroxetine[2]. |
| Alias | GR 205171 |
| Molecular Weight | 432.44 |
| Formula | C21H23F3N6O |
| Cas No. | 168266-90-8 |
| Smiles | C(F)(F)(F)C=1N(N=NN1)C2=CC(CN[C@@H]3[C@@H](NCCC3)C4=CC=CC=C4)=C(OC)C=C2 |
| Relative Density. | 1.39g/cm3 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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