Factor D inhibitor 6|cas:1386455-51-1|西域试剂

Factor D inhibitor 6,99.45%

产品编号：Bellancom-122700| CAS NO：1386455-51-1| 分子式：C₂₃H₂₂ClFN₆O₃| 分子量：484.91

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-122700		￥5900.00	杭州北京（现货）
Bellancom-122700		￥9500.00	杭州北京（现货）

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Factor D inhibitor 6

产品介绍

Factor D inhibitor 6 是一种有效的，高选择性，具有口服活性的因子 D (factor D) 抑制剂，IC₅₀ 为 30 nM，K_d 为 6 nM。Factor D inhibitor 6 对因子 B，激肽和凝集素补体途径激活以及广泛的受体，离子通道，激酶和蛋白酶等无活性。

生物活性

Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC₅₀ of 30 nM and a K_d of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases.

体外研究

Factor D inhibitor 6 (compound 6) effectively blocks both alternative pathway (AP)-mediated hemolysis in 10% human serum (IC₅₀ = 6 nM) and AP-induced membrane-attack complex (MAC) formation in lepirudinanticoagulated 50% human whole blood (IC₅₀ = 0.14 μM).
Factor D inhibitor 6 (compound 6) shows modest inhibition of murine FD (IC₅₀ = 0.86 μM).
Factor D inhibitor 6 (compound 6) inhibits both hemolysis and component 3 (C3) deposition on the surface of red blood cells (RBCs) with an IC₅₀ value of 70 nM, consistent with inhibition of the AP amplification loop.

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

体内研究

Factor D inhibitor 6 (Compound 6; 1-10 mg/kg; Oral gavage; once; C57Bl/6 mice) treatment dosed-ependently inhibits complement activation, with full inhibition at 10 mg/kg. Factor D inhibitor 6 shows sustained inhibition of LPS-induced AP activation for at least 8 h post-dose with an EC₅₀ of 0.034 μM.

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

Animal Model:	C57Bl/6 mice induced by lipopolysaccharide (LPS)
Dosage:	1 mg/kg, 3 mg/kg, 10 mg/kg
Administration:	Oral gavage; once
Result:	Dosed-ependently inhibited complement activation, with full inhibition at 10 mg/kg.

体内研究

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

Animal Model:	C57Bl/6 mice induced by lipopolysaccharide (LPS)
Dosage:	1 mg/kg, 3 mg/kg, 10 mg/kg
Administration:	Oral gavage; once
Result:	Dosed-ependently inhibited complement activation, with full inhibition at 10 mg/kg.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (515.56 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0622 mL	10.3112 mL	20.6224 mL
5 mM	0.4124 mL	2.0622 mL	4.1245 mL
10 mM	0.2062 mL	1.0311 mL	2.0622 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: ≥ 2.08 mg/mL (4.29 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.29 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
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.29 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.29 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 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: ≥ 2.08 mg/mL (4.29 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.29 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。