AZD8848 是一种选择性的TLR7前体药激动剂，用于哮喘和过敏性鼻炎的研究。
| 生物活性 | AZD8848 is a selectivetoll-like receptor7 (TLR7)antedrug agonist which is developed for the research of asthma and allergic rhinitis[1]. |
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体外研究
(In Vitro) | AZD8848 shows good activity against TLR7, with cellular pEC50s of 7.0 and 6.6 for human TLR7 and rat TLR7, respectively[1].
AZD8848 has an EC50of 4 nM in the induction of IFNα from human PBMCs and an IC50of 0.2-1.0 nM for the inhibition of IL-5, irrespective of whether the T cells have been polyclonally stimulated with PHA or via antigen presentation[1].
AZD8848 is a potent, selective TLR7 agonist antedrug able to inhibit Th2 responses in vitro[1].
AZD8848 has no activity against human TLR8 or against any of the other human TLRs[1].
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体内研究
(In Vivo) | AZD8848 (0.1-1 mg/kg; intratracheal) has a good pharmacokinetics in the Brown Norway rat[1].
AZD8848 (0.3 mg/kg; Intratracheal) suppresses the ovalbumin (OVA) challenge in the rat allergy model[1].
| Animal Model: | Brown Norway rat allergy model[1] | | Dosage: | 0.1 mg/kg, 1 mg/kg | | Administration: | Intratracheal (24 hours prior to and 24 hours after the OVA challenge) | | Result: | Suppressed OVA challenge in a dose-dependent manner. |
| Animal Model: | Brown Norway rat[1] | | Dosage: | 0.3 mg/kg (Pharmacokinetic Analysis) | | Administration: | Intratracheal | | Result: | Has a very short half-life (0.2 min) in rat blood and declined slowly after this point and levels above 1000 nmol/kg were maintained for over 5 hours. |
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| Clinical Trial | |
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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 : 25 mg/mL(43.88 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 1.7553 mL | 8.7765 mL | 17.5531 mL | | 5 mM | 0.3511 mL | 1.7553 mL | 3.5106 mL | | 10 mM | 0.1755 mL | 0.8777 mL | 1.7553 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 (4.39 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.39 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% (20%SBE-β-CDin saline) Solubility: 2.5 mg/mL (4.39 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (4.39 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 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 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: ≥ 2.5 mg/mL (4.39 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.39 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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