1. GPCR/G Protein Neuronal Signaling
  2. mGluR
  3. FTIDC

FTIDC 是一种口服,非竞争性,选择性的变构代谢型谷氨酸受体 1 (mGluR 1) 拮抗剂,对人 mGluR1a 的 IC50 为 5.8 nM。FTIDC 对人,小鼠和大鼠的重组 mGluR1 的拮抗活性没有物种差异。

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FTIDC

FTIDC Chemical Structure

CAS No. : 873551-53-2

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5 mg ¥2900
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10 mg ¥4600
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FTIDC is an orally active, noncompetitive, selective allosteric metabotropic glutamate receptor (mGluR) 1 antagonist with an IC50 of 5.8 nM for human mGluR1a. FTIDC has no species differences in its antagonistic activity on recombinant human, mouse, and rat mGluR1[1].

IC50 & Target[1]

mGluR1a

5.8 nM (IC50)

mGlu5

6200 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
> 10000 nM
Compound: 1
Antagonist activity at human mGluR5 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
Antagonist activity at human mGluR5 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
[PMID: 19692242]
CHO IC50
3.1 nM
Compound: 1
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
[PMID: 18849168]
CHO IC50
5.6 nM
Compound: 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
[PMID: 19692242]
CHO IC50
5.8 nM
Compound: 1
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
[PMID: 18849168]
CHO IC50
6200 nM
Compound: 1
Antagonist activity at human mGluR5 expressed in CHO cells assessed as calcium flux by FLIPR assay
Antagonist activity at human mGluR5 expressed in CHO cells assessed as calcium flux by FLIPR assay
[PMID: 18849168]
体外研究
(In Vitro)

FTIDC inhibits L-glutamate-induced increases in intracellular Ca2+ concentrations, with IC50 values of 5.8 nM , 5.8 nM , 3.1 nM , 7.7 nM for human mGluR1a, rat mGluR1a, mouse mGluR1a, human mGluR1b in CHO cells, respectively[1].

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

体内研究
(In Vivo)

FTIDC (i.p. or p.o.; 1-30 mg/kg) reduces the duration of face-washing behavior elicited in a dosedependent manner and the inhibitory effect is statistically significant at 10 and 30 mg/kg with i.p. and 30 mg/kg with p.o.[1].

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

Animal Model: Male CD1 (ICR) mice of 6-weeks-old[1]
Dosage: 1, 3, 10, and 30 mg/kg
Administration: I.p. or p.o.
Result: Reduced the duration of face-washing behavior elicited in a dosedependent manner and was statistically significant at 10 and 30 mg/kg with i.p. and 30 mg/kg with p.o..
分子量

358.41

Formula

C18H23FN6O

CAS 号
性状

固体

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料

纯度: ≥97.0%

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 *
= × ×

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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产品名称:
FTIDC
目录号:
HY-100405
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