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Pirfenidone
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Pirfenidone图片
CAS NO:53179-13-8
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
100mg电议
500mg电议
1 g电议
5 g电议
10 g电议
50 g电议

产品名称
吡非尼酮
AMR69
产品介绍
Pirfenidone (AMR69) 是一种抗纤维化剂,可减弱纤维细胞中CCL2CCL12的产生。Pirfenidone 具有抑制细胞生长的作用,并能降低人胶质瘤细胞系中的TGF-β2蛋白水平。Pirfenidone 还具有抗炎活性。
生物活性

Pirfenidone (AMR69) is an antifibrotic agent that attenuatesCCL2andCCL12production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reducesTGF-β2protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities[1][2][3].

IC50& Target

TGF-β2[1]

体外研究
(In Vitro)

Pirfenidone (PFD) reduces the protein levels of the matrix metalloproteinase (MMP)-11, a TGF-β target gene and furin substrate involved in carcinogenesis. These data define PFD or PFD-related agents as promising agents for human cancers associated with enhanced TGF-β activity[1]. In RAW264.7 cells, a murine macrophage-like cell line, Pirfenidone suppresses the proinflammatory cytokine TNF-α by a translational mechanism, which is independent of activation of the MAPK2, p38 MAPK, and JNK. In the murine endotoxin shock model, Pirfenidone potently inhibits the production of the proinflammatory cytokines, TNF-α, interferon-γ, and interleukin-6, but enhances the production of the anti-inflammatory cytokine, interleukin-10[2]. Pirfenidone (PFD) shows its inhibitory effects on the proliferation of HLECs. Cell proliferation is attenuated in the 0.3 mg/mL group after 24 hours compare with the control group (P=0.044). The effect is more apparent in the 0.5 mg/mL group at 24, 48, and 72 hours (P<0.05). The proliferation is almost completely inhibited with 1 mg/mL PFD at all the time-points (P<0.01)[3].

体内研究
(In Vivo)

Administration of Pirfenidone (300 mg/kg/day) for 4 wk. Pirfenidone significantly attenuates the score when administered in Bleomycin (BLM)-treated mice (P<0.0001). Moreover, collagen content is quantified in the lungs to evaluate the anti-fibrotic effects of Pirfenidone. The collagen content in the lungs of BLM-treated mice is significantly increased compared with that in saline- or Pirfenidone-treated mice, and this increase is significantly attenuated by Pirfenidone administration on day 28 after BLM treatment (P=0.0012)[4].

Clinical Trial
分子量

185.22

性状

Solid

Formula

C12H11NO

CAS 号

53179-13-8

中文名称

吡非尼酮;哌非尼酮;吡啡尼酮

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL(539.90 mM)

H2O : 16.67 mg/mL(90.00 mM;Need ultrasonic)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM5.3990 mL26.9949 mL53.9898 mL
5 mM1.0798 mL5.3990 mL10.7980 mL
10 mM0.5399 mL2.6995 mL5.3990 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 0.5%CMC-Na/saline water

    Solubility: 20 mg/mL (107.98 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: PBS

    Solubility: 9.09 mg/mL (49.08 mM); Clear solution; Need ultrasonic and warming and heat to 60℃

  • 3.

    请依序添加每种溶剂: Saline

    Solubility: 6.67 mg/mL (36.01 mM); Clear solution; Need ultrasonic

  • 4.

    请依序添加每种溶剂: 5% DMSO    40%PEG300   5%Tween-80   50% saline

    Solubility: ≥ 2.75 mg/mL (14.85 mM); Clear solution

  • 5.

    请依序添加每种溶剂: 5% DMSO    95% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.75 mg/mL (14.85 mM); Clear solution

  • 6.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.08 mg/mL (11.23 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (11.23 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 7.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.08 mg/mL (11.23 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (11.23 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 8.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.08 mg/mL (11.23 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (11.23 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。