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Cilostamide

Name: Cilostamide
Brand: TargetMol
SKU: T7642
Price: 278 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 98.87%

货号 T7642Cas号 68550-75-4

别名 西洛酰胺, OPC3689

Cilostamide (OPC3689) 是选择性 PDE3抑制剂，能够抑制 PDE3A (IC50:27 nM) 和 PDE3B (IC50:50 nM)，具有抗血栓和膜内增生的活性。

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Cilostamide

一键复制产品信息

很棒

纯度: 98.87%

货号 T7642 别名 西洛酰胺, OPC3689Cas号 68550-75-4

Cilostamide (OPC3689) 是选择性 PDE3抑制剂，能够抑制 PDE3A (IC50:27 nM) 和 PDE3B (IC50:50 nM)，具有抗血栓和膜内增生的活性。

规格	价格	库存
1 mg	¥ 278	现货
5 mg	¥ 579	现货
10 mg	¥ 928	现货
25 mg	¥ 1,850	现货
50 mg	¥ 2,780	现货
100 mg	¥ 4,180	现货
200 mg	¥ 5,930	现货
1 mL x 10 mM (in DMSO)	¥ 435	现货

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产品介绍

Cilostamide AI Summary

Cilostamide is a multifunctional bioactive compound that exhibits significant pharmacological activities across various biological pathways. It is a potent inhibitor of blood platelet aggregation, demonstrating in vitro inhibition of both collagen-induced and ADP-induced platelet aggregation in rabbits, with IC50 values of 2200.0 nM and 2400.0 nM, respectively. In vivo, it reduces systolic blood pressure and impacts heart rate in rats following oral administration. The compound also shows efficacy in anti-thrombotic activity in mice, inhibiting pulmonary thromboembolism by 84% at a dose of 30 mg/kg, and displays anti-hyperplastic activity in a rat balloon injury model with a 42% inhibition at the same dosage. Cilostamide is an effective phosphodiesterase (PDE) inhibitor. It inhibits PDE3B and PDE3A with IC50 values of 69.07 nM and 18.1 nM, respectively, and shows significant potency against PDE3 from human platelets, with an IC50 of 10.0 nM. It also inhibits PDE5 with an IC50 of 7150.0 nM. Additionally, it binds to Ca(2+)/calmodulin-dependent phosphodiesterase PDE1 in the human brain, exhibiting a Ki of 22000.0 nM, and to PDE3 in human platelets with a Ki of 5.0 nM and 20.0 nM. In terms of antimalarial activity, Cilostamide shows inhibitory effects on the growth of Plasmodium falciparum with IC50 values ranging from approximately 2511.89 nM to 12589.25 nM. The compound also demonstrates antiviral properties by inhibiting SARS-CoV-2 induced cytotoxicity in Caco-2 and VERO-6 cells at a concentration of 10 µM, though it requires higher concentrations for more significant effects. Other notable activities include inhibitory effects on human HDAC6, induction of lipolysis in mouse and human adipocytes, and binding inhibition of Platelet Activating Factor (PAF) with IC50 values of 3687.0 nM and a Ki of 1917.0 nM. Moreover, Cilostamide has been shown to inhibit the SARS-CoV-2 main protease 3CL-Pro with modest effectiveness at 20 µM concentration. These diverse bioactivities suggest that Cilostamide holds potential for therapeutic applications in cardiovascular diseases, inflammatory conditions, thrombotic disorders, malaria, and viral infections, although further investigations are warranted to fully elucidate its mechanisms and optimize its efficacy..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	Cilostamide (OPC3689) is a selective phosphodiesterase (PDE)3A and PDE3B inhibitor(IC50 values of 27 and 50 nM, respectively)
靶点活性	PDE3B:50 nM, PDE3A:27 nM
别名	西洛酰胺, OPC3689

化学信息

分子量	342.43
分子式	C₂₀H₂₆N₂O₃
CAS No.	68550-75-4
Smiles	CN(C1CCCCC1)C(=O)CCCOc1ccc2[nH]c(=O)ccc2c1
密度	1.18 g/cm3

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 31 mg/mL (90.53 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.92 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.9203 mL	14.6015 mL	29.2030 mL	146.0152 mL
5 mM	0.5841 mL	2.9203 mL	5.8406 mL	29.2030 mL
10 mM	0.2920 mL	1.4602 mL	2.9203 mL	14.6015 mL
20 mM	0.1460 mL	0.7301 mL	1.4602 mL	7.3008 mL
50 mM	0.0584 mL	0.2920 mL	0.5841 mL	2.9203 mL