Purfalcamine|cas:1038620-68-6|西域试剂

Purfalcamine,99.71%

产品编号：Bellancom-117015| CAS NO：1038620-68-6| 分子式：C₂₉H₃₃FN₈O| 分子量：528.62

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-117015	￥5000.00	杭州北京（现货）
Bellancom-117015	￥8500.00	杭州北京（现货）
Bellancom-117015	￥18000.00	杭州北京（现货）
Bellancom-117015	￥30000.00	杭州北京（现货）
Bellancom-117015	￥46000.00	杭州北京（现货）

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Purfalcamine

产品介绍

Purfalcamine 是一种具有口服活性，选择性的恶性疟原虫钙依赖性蛋白激酶 1 (PfCDPK1) 抑制剂，IC₅₀ 为 17 nM，EC₅₀ 为 230 nM。Purfalcamine 具有抗疟疾活性，可以引起疟原虫在裂殖体阶段的发育停滞。

生物活性

Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC₅₀ of 17 nM and an EC₅₀ of 230 nM. Purfalcamine has antimalarial activity and causes malaria parasites developmental arrest at the schizont stage.

体外研究

Purfalcamine has low activity against Toxoplasma gondii calcium-dependent protein kinase 3 (TgCDPK3).
Purfalcamine (225, 450 nM) has no effect on the parasitemia in the first 32 hours. After about 40 hours, parasite level remains stable and then begins dropping.
Purfalcamine inhibits proliferation with EC₅₀s of 171-259 nM for P. falciparum strains (3D7, Dd2, FCB, HB3 and W2), which indicates effectiveness against drug-resistant parasites.
Given that the EC₅₀ value for P. falciparum (3D7) is 230 nM, Purfalcamine shows a therapeutic window ranging from 23-fold to 36-fold (EC₅₀s for CHO=12.33 μM, HEp2=7.235 μM, HeLa=7.029 μM and Huh7=5.476 μM).

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

体内研究

Purfalcamine (10 mg/kg; oral gavage; BID; for 6 days) demonstrates a delay in the onset of parasitemia in treated mice.
Purfalcamine (20 mg/kg; orally gavage) exhibits a C_max of 2.6 μM with a half-life of 3.1 hours.

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

Animal Model:	Male BALB/c mice, 7 weeks of age with the malaria parasite
Dosage:	10 mg/kg
Administration:	Oral gavage; BID; for 6 days
Result:	Demonstrated a delay in the onset of parasitemia in treated mice when compared with control mice.

Animal Model:	Five- to six-week-old male Balb/c mice (22-25 g)
Dosage:	20 mg/kg (Pharmacokinetic Analysis)
Administration:	Orally gavage
Result:	Exhibited a maximum plasma exposure (C_max) of 2.6 μM with a half-life of 3.1 hours.

体内研究

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

Animal Model:	Male BALB/c mice, 7 weeks of age with the malaria parasite
Dosage:	10 mg/kg
Administration:	Oral gavage; BID; for 6 days
Result:	Demonstrated a delay in the onset of parasitemia in treated mice when compared with control mice.

Animal Model:	Five- to six-week-old male Balb/c mice (22-25 g)
Dosage:	20 mg/kg (Pharmacokinetic Analysis)
Administration:	Orally gavage
Result:	Exhibited a maximum plasma exposure (C_max) of 2.6 μM with a half-life of 3.1 hours.

性状

Solid

溶解性数据

In Vitro:

DMSO : 12.5 mg/mL (23.65 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8917 mL	9.4586 mL	18.9172 mL
5 mM	0.3783 mL	1.8917 mL	3.7834 mL
10 mM	0.1892 mL	0.9459 mL	1.8917 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。-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: ≥ 1.25 mg/mL (2.36 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (2.36 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 12.5 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: ≥ 1.25 mg/mL (2.36 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (2.36 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 12.5 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: ≥ 1.25 mg/mL (2.36 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (2.36 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 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。