Mirodenafil dihydrochloride SK-3530 dihydrochloride|cas:862189-96-6|西域试剂

Mirodenafil dihydrochloride SK-3530 dihydrochloride,99.79%

产品编号：Bellancom-14930A| CAS NO：862189-96-6| 分子式：C₂₆H₃₉Cl₂N₅O₅S| 分子量：604.59

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-14930A	￥3255.00	杭州北京（现货）
Bellancom-14930A	￥4650.00	杭州北京（现货）
Bellancom-14930A	￥13950.00	杭州北京（现货）
Bellancom-14930A	￥0.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

Mirodenafil dihydrochloride SK-3530 dihydrochloride

产品介绍

Mirodenafil (SK3530) dihydrochloride 是一种口服有效、可逆的、选择性的磷酸二酯酶 5 (PDE5) 的抑制剂。Mirodenafil dihydrochloride 是一种糖皮质激素受体 (GR) 的调节剂。Mirodenafil dihydrochloride 通过下调 Dkk1 的表达，激活 Wnt/β-catenin 信号通路。Mirodenafil dihydrochloride 可用于研究勃起功能障碍 (ED)、阿尔茨海默病 (AD) 和系统性硬化症 (SSc)。

生物活性

Mirodenafil (SK3530) dihydrochloride is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil dihydrochloride is a glucocorticoid receptor (GR) modulator Mirodenafil dihydrochloride activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil dihydrochloride can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc).

体外研究

Mirodenafil dihydrochloride (0-40 μM, 24 h) exerts neuroprotective functions via activating the cGMP/PKG/CREB signaling pathway.
Mirodenafil dihydrochloride (0-40 μM, 24 h) enhances neuronal survival by protecting the mitochondrial membrane potential and inhibiting apoptosis.
Mirodenafil dihydrochloride (0-40 μM) inhibits GSK-3β signaling, resulting in reduced tau phosphorylation, decreased Aβ production by inhibiting amyloidogenesis and activating the autophagosomal pathway.
Mirodenafil dihydrochloride inhibits the transcriptional activity of the glucocorticoid receptor (GR), and inhibits homodimerization of GR in HT-22 cells.
Mirodenafil dihydrochloride (0-100 μM, 24 h) inhibits TGF-β-induced phosphorylation of Smad2/3 and mRNA expression of the fibrosis marker in fibroblasts.

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

Western Blot Analysis

Cell Line:	SH-SY5Y human neuroblastoma cells
Concentration:	0, 10, 20, 40 μM
Incubation Time:	24 h
Result:	Significantly increased cGMP levels by about 200% in a dose-dependent manner. Reversed the Aβ-induced decrease in phosphorylated CREB in a dose-dependent manner. Aβ₄₂ alone increased the levels of cleaved caspase-3 and cleaved PARP, whereas the combined treatment with mirodenafil markedly reduced the expression levels of both apoptotic markers.

RT-PCR

Cell Line:	NIH3T3 mouse embryonic fibroblasts
Concentration:	0, 10, 100 μM
Incubation Time:	24 h
Result:	The mRNA expression of COL1A1, α-SMA, and CTGF were induced by treatment with TGF-β1, and Mirodenafil significantly reduced the expression of these profibrotic genes.

体内研究
(In Vivo)

Mirodenafil dihydrochloride (4 mg/kg, IP, daily for 4 weeks) enhances the cognitive-behavioral performance in transgenic AD mice.
Mirodenafil dihydrochloride (0-10 mg/kg, Orally, daily for 3 weeks) ameliorates dermal fibrosis in a BLM-induced SSc mouse model by inhibiting the TGF-β signaling pathway, thereby suppressing the expression of collagen and profibrotic genes.

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

Animal Model:	APP-C105 transgenic mice (13-month-old, male, n=6)
Dosage:	4 mg/kg
Administration:	IP, daily for 4 weeks
Result:	Improved cognitive function in the APP-C105 AD mice.

Animal Model:	Male BALB/c mice (8 weeks old, four groups, n=10/group)
Dosage:	0, 5 or 10 mg/kg
Administration:	Orally, daily for 3 weeks
Result:	Ameliorated dermal fibrosis and downregulated the protein levels of fibrosis markers including COL1A1 and α-SMA in the BLM-induced SSc mouse model. Significantly decreased dermal thickness and collagen content.

体内研究

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

Animal Model:	APP-C105 transgenic mice (13-month-old, male, n=6)
Dosage:	4 mg/kg
Administration:	IP, daily for 4 weeks
Result:	Improved cognitive function in the APP-C105 AD mice.

Animal Model:	Male BALB/c mice (8 weeks old, four groups, n=10/group)
Dosage:	0, 5 or 10 mg/kg
Administration:	Orally, daily for 3 weeks
Result:	Ameliorated dermal fibrosis and downregulated the protein levels of fibrosis markers including COL1A1 and α-SMA in the BLM-induced SSc mouse model. Significantly decreased dermal thickness and collagen content.

体内研究

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

Animal Model:	APP-C105 transgenic mice (13-month-old, male, n=6)
Dosage:	4 mg/kg
Administration:	IP, daily for 4 weeks
Result:	Improved cognitive function in the APP-C105 AD mice.

Animal Model:	Male BALB/c mice (8 weeks old, four groups, n=10/group)
Dosage:	0, 5 or 10 mg/kg
Administration:	Orally, daily for 3 weeks
Result:	Ameliorated dermal fibrosis and downregulated the protein levels of fibrosis markers including COL1A1 and α-SMA in the BLM-induced SSc mouse model. Significantly decreased dermal thickness and collagen content.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (165.40 mM)

H₂O : 5 mg/mL (8.27 mM; ultrasonic and warming and heat to 60°C)

* "≥" 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	1.6540 mL	8.2701 mL	16.5401 mL
5 mM	0.3308 mL	1.6540 mL	3.3080 mL
10 mM	0.1654 mL	0.8270 mL	1.6540 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 (stored under nitrogen)。-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 (4.14 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.14 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 (4.14 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.14 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 (4.14 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.14 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。