PFI-2 hydrochloride (R-PFI-2 hydrochloride)|cas:1627607-87-7|西域试剂

PFI-2 hydrochloride (R-PFI-2 hydrochloride),99.80%

产品编号：Bellancom-18627A| CAS NO：1627607-87-7| 分子式：C₂₃H₂₆ClF₄N₃O₃S| 分子量：535.98

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-18627A		￥1400.00	杭州北京（现货）
Bellancom-18627A		￥4900.00	杭州北京（现货）

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PFI-2 hydrochloride (R-PFI-2 hydrochloride)

产品介绍

PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride 是一种强效的选择性 SETD7 抑制剂。(R)-PFI-2 具有高度抑制活性，其 IC₅₀ 值为 2.0 nM，(S)-PFI-2 的抑制活性 IC₅₀值为 1.0 μM。PFI-2 hydrochloride 可用于研究慢性肾脏疾病和肾纤维化发展过程中的炎症反应。

生物活性

PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride is a potent and selective SET domain containing lysine methyltransferase 7 (SETD7) inhibitor. (R)-PFI-2 shows high inhibiting activity with IC₅₀ value of 2.0 nM and (S)-PFI-2 shows inhibiting activity with IC₅₀ value of 1.0 μM. PFI-2 hydrochloride can be used for the research of chronic kidney disease and inflammation response in the development of renal fibrosis.

体外研究

(R)-PFI-2 shows high inhibiting activity with IC₅₀ value of 2.0 nM and (S)-PFI-2 shows inhibiting activity with IC₅₀ value of 1.0 μM.

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

体内研究

PFI-2 hydrochloride (i.p., 200 μM, twice a week) attenuates the progression of renal fibrosis and preserves renal function in FA nephropathy.
PFI-2 hydrochloride (i.p., 200 μM, twice a week) reduced ECM accumulation and fibroblasts activation after FA injury.
PFI-2 hydrochloride (i.p., 200 μM, twice a week) impeded Th2 cytokine signaling activation and M2 macrophage polarization.
PFI-2 hydrochloride (i.p., 200 μM, twice a week) suppressed M2 macrophages-myofibroblasts transition and myeloid myofibroblasts accumulation in the FA-treated kidneys.
PFI-2 hydrochloride (i.p., 200 μM, twice a week) attenuated macrophages M2 polarization and M2 macrophages-to-myofibroblasts transition in obstructed kidneys.
PFI-2 hydrochloride (i.p., 200 μM, twice a week) suppressed myeloid myofibroblast accumulation and renal fibrosis after UUO injury.
PFI-2 hydrochloride (i.p., 200 μM, twice a week) reduced the infiltration of inflammatory cells, the production of inflammatory molecules, and NF-κB activation in FA nephropathy.

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

Animal Model:	Male C57BL/6 mice (8-10-week old, 20-25 g)
Dosage:	200 μM (PFI-2 is diluted in 100 μL 0.1% (v/v) DMSO to a concentration of 200 μM/100 μL)
Administration:	intraperitoneal injection, twice a week
Result:	Presented less bone marrow-derived myofibroblasts, fewer CD206+/α-smooth muscle actin + cells and developed less renal fibrosis (P<0.01). Reduced the infiltration of inflammatory cells and decreased the production of pro-inflammatory cytokines and chemokines in the kidneys after folic acid treatment (P<0.01). Suppressed the accumulation of NF-κB p65+ cells in folic acid nephropathy (P<0.01).

体内研究

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

Animal Model:	Male C57BL/6 mice (8-10-week old, 20-25 g)
Dosage:	200 μM (PFI-2 is diluted in 100 μL 0.1% (v/v) DMSO to a concentration of 200 μM/100 μL)
Administration:	intraperitoneal injection, twice a week
Result:	Presented less bone marrow-derived myofibroblasts, fewer CD206+/α-smooth muscle actin + cells and developed less renal fibrosis (P<0.01). Reduced the infiltration of inflammatory cells and decreased the production of pro-inflammatory cytokines and chemokines in the kidneys after folic acid treatment (P<0.01). Suppressed the accumulation of NF-κB p65+ cells in folic acid nephropathy (P<0.01).

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 32 mg/mL (59.70 mM)

H₂O : 5.56 mg/mL (10.37 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8657 mL	9.3287 mL	18.6574 mL
5 mM	0.3731 mL	1.8657 mL	3.7315 mL
10 mM	0.1866 mL	0.9329 mL	1.8657 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 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： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.66 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.66 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.66 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.66 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.66 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.66 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
4.

请依序添加每种溶剂： PBS
Solubility: 1 mg/mL (1.87 mM); Clear solution; Need ultrasonic