2. GPCR/G Protein Neuronal Signaling
  3. Neurokinin Receptor
  4. Vofopitant

Vofopitant  (Synonyms: GR 205171)

製品番号: HY-12142 純度: 99.82%
COA 取扱説明書 Technical Support

Vofopitant (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting.

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Vofopitant

Vofopitant 構造式

CAS 番号 : 168266-90-8

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 330 在庫あり
Solution
10 mM * 1 mL in DMSO USD 330 在庫あり
Solid
5 mg $300 在庫あり
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Vofopitant 関連抗体

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製品説明

Vofopitant (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting[1][2][3][4][5][6].

IC50 & Target

NK1R

9.02 (pKi)

Cellular Effect
Cell Line Type Value Description References
CHO IC50
0.08 1
Compound: 3
Displacement of [125I]-labeled SP from the human Tachykinin receptor 1 expressed in CHO cells
Displacement of [125I]-labeled SP from the human Tachykinin receptor 1 expressed in CHO cells
[PMID: 9804700]
CHO IC50
0.08 1
Compound: 3
Displacement of [125I]-labeled SP from the human Tachykinin receptor 1 expressed in CHO cells
Displacement of [125I]-labeled SP from the human Tachykinin receptor 1 expressed in CHO cells
[PMID: 9804700]
体外実験

Vofopitant (GR 205171) (10 pM-1 mM; 60 min) potently inhibits [3H]-SP binding to NK1 receptors in mouse cerebral cortex homogenates with a pKi of 9.02[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Vofopitant 関連抗体
体内実験

Vofopitant (GR 205171) (3-30 mg/kg; i.p.; single dose) produces a significant reduction in immobility time at the 30 mg/kg i.p. dose in the mouse forced swim test, with no corresponding change in frontal cortex extracellular monoamine levels[1].
Vofopitant (GR-205171) (50 µg/kg; i.v.; single dose) abolishes fictive retching and emesis-associated antral contractility enhancement, reduces emesis-related hypersalivation and parasympathetic nerve activity, but does not affect gastric corpus relaxation, vagosalivary reflex-mediated salivation, or linguosalivary reflex responses in dogs[2].
Vofopitant (GR 205171) (10 mg/kg; s.c.; single dose) does not alter DRN serotonergic neuron firing or 5-HT1A autoreceptor sensitivity in male C57BL/6J mice[4].
Vofopitant (10 mg/kg/day; s.c.; continuous delivery; 21 days) reduces the potency of Ipsapirone (HY-19686) to inhibit DRN serotonergic neuron firing by ~1.5-fold, indicating functional desensitization of 5-HT1A autoreceptors in male C57BL/6J mice[4].
Vofopitant (10 mg/kg/day; s.c.; continuous delivery; 21 days) reduces the potency and maximal effect of 5-CT to stimulate [35S]GTP-γ-S binding in the DRN, indicating impaired G-protein coupling of desensitized 5-HT1A autoreceptors in male C57BL/6J mice[4].
Vofopitant (10 mg/kg/day; s.c.; continuous delivery; 21 days) significantly increases basal extracellular 5-HT levels in the DRN and potentiates Paroxetine (HY-122272)-induced cortical 5-HT overflow in male C57BL/6J mice[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CD-1 mice (20-26 g)[1]
Dosage: 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: i.p.; single dose
Result: Did not reduce immobility time obviously at 3 mg/kg.
Exerted mild and non-significant reduction at 10 mg/kg.
Reduced immobility time significantly at 30 mg/kg.
Showed no notable changes in cortical monoamine levels at 30 mg/kg within 300 minutes.
Animal Model: C57BL/6J (male, 8-10 weeks old, 20-25 g)[5]
Dosage: 10 mg/kg
Administration: s.c.; single dose
Result: Did not change firing frequency and pattern of DRN serotonergic neurons.
Exhibited comparable inhibitory potency of ipsapirone on neuronal firing between treatment and control groups.
Produced full inhibition at 100 nM ipsapirone in both groups.
Animal Model: C57BL/6J (male, 8-10 weeks old, 20-25 g)[5]
Dosage: 10 mg/kg/day
Administration: s.c.; continuous delivery; 21 days
Result: Did not change basal firing rate of DRN serotonergic neurons.
Decreased ipsapirone’s inhibitory potency on neuronal firing and raised its concentration for full inhibition.
Displayed similar basal [35S]GTP-γ-S labelling in the DRN between groups.
Weakened 5-CT-induced [35S]GTP-γ-S binding with a right-shifted curve and lower maximal response.
Exerted no influence on basal extracellular 5-HT in the frontal cortex but elevated basal 5-HT levels in the DRN.
Enhanced paroxetine-triggered 5-HT elevation in both cortex and DRN of treated mice.
臨床実験
分子量

432.44

分子式

C21H23F3N6O
CAS 番号
Appearance

Solid

Color

Light yellow to yellow

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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (231.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

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In Vivo Dissolution Calculator
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純度とドキュメンテーション

純度: 99.82%

COA (255 KB) HNMR (188 KB) LCMS (118 KB)

取扱説明書 (2659 KB)
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3125 mL 11.5623 mL 23.1246 mL 57.8115 mL
5 mM 0.4625 mL 2.3125 mL 4.6249 mL 11.5623 mL
10 mM 0.2312 mL 1.1562 mL 2.3125 mL 5.7811 mL
15 mM 0.1542 mL 0.7708 mL 1.5416 mL 3.8541 mL
20 mM 0.1156 mL 0.5781 mL 1.1562 mL 2.8906 mL
25 mM 0.0925 mL 0.4625 mL 0.9250 mL 2.3125 mL
30 mM 0.0771 mL 0.3854 mL 0.7708 mL 1.9270 mL
40 mM 0.0578 mL 0.2891 mL 0.5781 mL 1.4453 mL
50 mM 0.0462 mL 0.2312 mL 0.4625 mL 1.1562 mL
60 mM 0.0385 mL 0.1927 mL 0.3854 mL 0.9635 mL
80 mM 0.0289 mL 0.1445 mL 0.2891 mL 0.7226 mL
100 mM 0.0231 mL 0.1156 mL 0.2312 mL 0.5781 mL
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Vofopitant Related Classifications

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Vofopitant168266-90-8GR 205171GR205171GR-205171Neurokinin ReceptorNK receptorTachykinin receptorInhibitorinhibitorinhibit

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