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

Vofopitant 是一種有效的 NK1 receptor 拮抗劑，對(duì)人，大鼠和雪貂的 NK1 receptor 的 pKi 值分別為 10.6，9.5 和 9.8。

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Vofopitant Chemical Structure

Vofopitant Chemical Structure

CAS No. : 168266-90-8

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規(guī)格 價(jià)格 是否有貨
1 mg ￥1300
詢(xún)問(wèn)價(jià)格 & 貨期
5 mg ￥3000
詢(xún)問(wèn)價(jià)格 & 貨期

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Vofopitant 的其他形式現(xiàn)貨產(chǎn)品:

Other Forms of Vofopitant:

查看 Neurokinin Receptor 亞型特異性產(chǎn)品:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

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.

IC50 & Target

pKi: 10.6 (Human NK1 receptor), 9.5 (Rat NK1 receptor), 9.8 (Ferret NK1 receptor)[1]
體外研究
(In Vitro)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

432.44

Formula

C21H23F3N6O
CAS 號(hào)
性狀

固體

顏色

Light yellow to yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
純度 & 產(chǎn)品資料
參考文獻(xiàn)
Kinase Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

The molarity calculator equation

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

質(zhì)量   濃度   體積   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start) × 體積 (start) = 濃度 (final) × 體積 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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.

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Vofopitant
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