BIO-1211 是高度选择性的、具有口服活性的α4β1 (VLA-4)抑制剂，其对 α4β1 和 α4β7 的IC50值分别为 4 nM 和 2 μM。
| 生物活性 | BIO-1211 is a highly selective and orally activeα4β1(VLA-4)inhibitor, withIC50values of 4 nM and 2 μM forα4β1andα4β7, respectively[1][2][3]. |
| IC50& Target[3] | α4β1 4 nM (IC50) | α4β7 2 μM (IC50) |
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体外研究
(In Vitro) | BIO-1211 almostly exhibits no activity for α1β1, α5β1, α6β1, αLβ2 and αIIbβ3[3].
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体内研究
(In Vivo) | BIO-1211 (5 and 10 mg/kg, orally, once every other day) results in reduced cytokines expression, leukocyte trafficking, and inhibition of inflammatory responses in EAE in a dose-independent manner. BIO-1211 exhibits a considerable depletion in the EAE clinical score, which correlated with decreased expression of TNF-α, IL-17, IFN-γ and pervade of CD11b+ and CD45+ cells into the cerebral cortex[2].
| Animal Model: | Naive, C57BL/6 mice (male, 8 weeks old, 20-25 g weight)[2]. | | Dosage: | 5 and 10 mg/kg. | | Administration: | Orally once every other day starting the day before immunization until day 21 post-immunization. | | Result: | Could prevent the induction of EAE.
Significantly delayed the onset of EAE and reduced the severity of clinical EAE compared to the vehicle group.
Markedly reduced the expression of both CD11b and CD45 in comparison with the vehicle group.
mRNA and soluble form of a subset of target inflammatory cytokines (IFNγ, IL-17, and TNF-α) was dramatically decreased.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Sealed storage, away from moisture | Powder | -80°C | 2 years | | -20°C | 1 year |
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 250 mg/mL(352.71 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.4108 mL | 7.0542 mL | 14.1084 mL | | 5 mM | 0.2822 mL | 1.4108 mL | 2.8217 mL | | 10 mM | 0.1411 mL | 0.7054 mL | 1.4108 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 (sealed storage, away from moisture)。-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 (2.93 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (2.93 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 (2.93 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (2.93 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 (2.93 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (2.93 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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