BIO5192 hydrate 是一种选择性强的整合素α4β1 (VLA-4)抑制剂 (Kd<10 pm)。bio5192 hydrate 选择性地与 α4β1 (IC50=1.8 nM) 结合,选择性高过其他一系列整合素。BIO5192 hydrate 导致小鼠造血干细胞和祖细胞 (HSPCs) 的动员比基础水平增加 30 倍。
生物活性 | BIO5192 hydrate is a selective and potentintegrinα4β1(VLA-4)inhibitor (Kd<10 pm). bio5192 hydrate selectively binds toα4β1(IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels[1][2]. |
IC50& Target[1] | α4β1 1.8 nM (IC50) | α9β1 138 nM (IC50) | α2β1 1053 nM (IC50) | α4β7 >500 nM (IC50) |
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体内研究 (In Vivo) | The combination of BIO5192 hydrate (1 mg/kg; i.v.) and Plerixafor (5 mg/kg; s.c.) exert an additive effect on progenitor mobilization[1]. BIO5192 hydrate (30 mg/kg; s.c; bid; during days 5 through 14) delays paralysis associated with EAE (experimental autoimmune encephalomyelitis)[2]. BIO5192 hydrate (1 mg/kg, i.v.) shows the terminal half-life is 1.1 hours. BIO5192 hydrate (3, 10, and 30 mg/kg; s.c.) shows half-lives of 1.7, 2.7, and 4.7 hours, respectively. The blood plasma curves show that the AUC for the s.c. route of administration increased about 2.5-fold from 5,460 h*ng/ml for the 3 mg/kg dose to 14,175 h*ng/ml for the 30 mg/kg[1].
Animal Model: | C57BL/6J x 129Sv/J F1 mice[1] | Dosage: | 1 mg/kg (with Plerixafor: 5 mg/kg) | Administration: | I.v. | Result: | Exerted an additive effect on progenitor mobilization. |
Animal Model: | Healthy female Lewis rats weighing 150g[2] | Dosage: | 30 mg/kg | Administration: | S.c; bid; during days 5 through 14 | Result: | Showed a 3-day delay in onset of disease. |
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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 | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(120.95 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 1.2095 mL | 6.0475 mL | 12.0950 mL | 5 mM | 0.2419 mL | 1.2095 mL | 2.4190 mL | 10 mM | 0.1209 mL | 0.6047 mL | 1.2095 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: ≥ 2.5 mg/mL (3.02 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.02 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。 2. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (3.02 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.02 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。 *以上所有助溶剂都可在本网站选购。
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