1. Immunology/Inflammation GPCR/G Protein
  2. Interleukin Related Adenosine Receptor
  3. FK3453

FK3453 是一种腺苷 A1/2 (adenosine A1/A2) 双重抑制剂和 TSLP 抑制剂。FK3453 也是醛氧化酶 (AO) 的底物。FK3453 可抑制 TSLPIL-33 的产生。FK3453 可用于帕金森病和过敏性疾病的研究。

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FK3453

FK3453 Chemical Structure

CAS No. : 560111-91-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FK3453 is a dual adenosine A1/A2 inhibitor and a TSLP inhibitor. FK3453 is also a substrate of aldehyde oxidase (AO). FK3453 can inhibit the production of TSLP and IL-33. FK3453 is useful for research on Parkinson’s disease and allergic disorders[1][2][3].

体外研究
(In Vitro)

FK3453 (1-10 µM;0-24 h) 以浓度依赖性方式抑制 KCMH-1 小鼠角质形成细胞中组成型 TSLP 的产生,且不降低细胞活力[2]
FK3453 (1-10 µM;4.5 h) 可抑制 TPA (HY-18739) 处理的 PAM212 小鼠角质形成细胞中 TSLP mRNA 的表达[2]
FK3453 (1-10 µM;4.5-24.5 小时) 可抑制 NHEKs 中 T4FP 诱导和 TPA 诱导的 TSLP mRNA 表达,以及 TPA 诱导的 IL-33 mRNA 表达[2]

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

RT-PCR[2]

Cell Line: PA (HY-18739) treated PAM212 cells
Concentration: 1, 3 and 10 μM
Incubation Time: Pretreated with 30 min, then co-incubation for 4 h
Result: Reduced the levels of TSLP mRNA in a ntration-dependent manner.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2β Vdss AUCinf CLt Cmax Tmax F AUC0-∞ T1/2 AUC CL
Rat[1] 3.2 mg/kg i.v. / / / 10.8 mL/min/kg / / / / 0.4 h / /
Rat[1] 3.2 mg/kg p.o. / / / / 544 ng/mL / 34.6 % / / 1789.4 ng·h/mL 29.8 mL/min/kg
Rat[3] 0.1 (male) mg/kg i.v. 0.95 h 0.69 L/kg 111.9 ng·h/mL 14.9 mL/min/kg / / / / / / /
Rat[3] 0.32 (male) mg/kg i.v. 0.50 h 0.91 L/kg 304.1 ng·h/mL 17.6 mL/min/kg / / / / / / /
Rat[3] 3.2 (male) mg/kg i.v. 0.37 h 0.48 L/kg 5170.3 ng·h/mL 10.8 mL/min/kg / / / / / / /
Rat[3] 0.1 (male) mg/kg p.o. / / 34.2 ng·h/mL / 41.0 ng/mL 0.5 h 30.5 % / / / /
Rat[3] 0.32 (male) mg/kg p.o. / / 127.4 ng·h/mL / 36.8 ng/mL 1.5 h 41.9 % / / / /
Rat[3] 3.2 (male) mg/kg p.o. / / / / 544.0 ng/mL 1.0 h 34.6 % 1789.4 ng·h/mL / / /
Rat[3] 0.1 (female) mg/kg i.v. 0.73 h 0.96 L/kg 124.2 ng·h/mL 14.1 mL/min/kg / / / / / / /
Rat[3] 1 (female) mg/kg i.v. 2.77 h 0.77 L/kg 4987.2 ng·h/mL 7.8 mL/min/kg / / / / / / /
Rat[3] 1 (female) mg/kg p.o. / / 3372.4 ng·h/mL / 373.3 ng/mL 1.7 h 67.6 % / / / /
体内研究
(In Vivo)

FK3453 (0.3 mM;气囊局部注射;单剂量) 在 LPS (HY-D1056) 诱导的 ICR 小鼠气囊型炎症模型中抑制 TSLP 的产生,且降低气囊液重量[2]

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

Animal Model: ICR mice (five-week-old male, lipopolysaccharide-induced air pouch-type inflammation model)[2]
Dosage: 0.3 mM
Administration: local injection into air pouch; single dose
Result: Significantly inhibited LPS-induced increases in TSLP protein levels in pouch fluid and TSLP mRNA levels in pouch wall tissues.
Strongly decreased the weight of pouch fluids.
分子量

307.35

Formula

C17H17N5O

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 *
= × ×

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:
FK3453
目录号:
HY-404647
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