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,Kd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 Dinhibitor 6 is a potent, highly selective and orally activefactor D(FD)inhibitor with an IC50of 30 nM and aKdof 6 nM.Factor Dinhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases[1]. |
IC50& Target | IC50: 30 nM (Factor D)[1] Kd: 6 nM (Factor D)[1] |
体外研究 (In Vitro) | 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)[1]. Factor D inhibitor 6 (compound 6) shows modest inhibition of murine FD (IC50= 0.86 μM)[1]. Factor D inhibitor 6 (compound 6) inhibits both hemolysis and component 3 (C3) deposition on the surface of red blood cells (RBCs) with an IC50value of 70 nM, consistent with inhibition of the AP amplification loop[1].
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体内研究 (In Vivo) | 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 EC50of 0.034 μM[1].
Animal Model: | C57Bl/6 mice induced by lipopolysaccharide (LPS)[1] | 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. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 250 mg/mL(515.56 mM;Need ultrasonic) 配制储备液 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 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。 *以上所有助溶剂都可在本网站选购。
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