1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Histamine Receptor
  3. Ciproxifan

Ciproxifan (FUB 359) 是一种有效的,选择性的,具有口服活性和竞争性的组胺 H3 受体拮抗剂,IC50 值为 9.2 nM。Ciproxifan 对其他受体亚型的表观亲和力低。Ciproxifan 可用于研究衰老性疾病和阿尔兹海默症。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 Ciproxifan maleate 通常具有更好的水溶性和稳定性。

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Ciproxifan Chemical Structure

Ciproxifan Chemical Structure

CAS No. : 184025-18-1

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Ciproxifan 的其他形式现货产品:

Other Forms of Ciproxifan:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Ciproxifan (FUB 359) is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan displays low apparent affinity at other receptor subtypes. Ciproxifan can be used for the research of aging disorders and Alzheimer's disease[1][3].

IC50 & Target[1]

H3 receptor

9.2 nM (IC50)

体外研究
(In Vitro)

Ciproxifan inhibits [3H]HA release from synaptosomes of rat cerebral cortex, with a Ki of 0.5 nM[1].
Ciproxifan (0.01 nM-1 μM; 60 min) inhibits the binding of [125I]iodoproxyfan with rat striatal membranes, with a Ki of 0.7 nM[1].

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

体内研究
(In Vivo)

Ciproxifan (1 mg/kg; a single p.o.) increases the t-MeHA level in mouse brain, with an ED50 of 0.14 mg/kg[1].
Ciproxifan (3 mg/kg, i.p.) improves the accuracy of responding in the five-choice task in rats only when the stimulus duration was 0.25 sec instead of 0.50 sec[1].
Ciproxifan (0.15-2 mg/kg; p.o.) induces marked signs of neocortical electroencephalogram activation manifested by enhanced fast-rhythms density and an almost total waking state in cats[1].
Ciproxifan (1 mg/kg; a single i.v.) decreases the H3-receptor ligand concentration in serum in mice, with the half-lives (t1/2) of 13 and 87 min for the distribution and elimination phases in mice, respectively[1].
Ciproxifan (1 mg/kg; a single p.o.) exhibits oral bioavailability (F=62%) and maximal concentration (Cmax=420 nM) in mice[1].

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

分子量

270.33

Formula

C16H18N2O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (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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Ciproxifan
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HY-14567
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