Ketotifen (HC 20-511) fumarate 是一种具有口服活性的第二代非竞争性组胺 1 (H1) 受体阻滞剂和肥大细胞稳定剂。Ketotifen fumarate 可在体外阻断 6-磷酸葡萄糖酸脱氢酶 (6-PGD)。Ketotifen fumarate 还对SARS-CoV-2和流感病毒 (Influenza virus) 具有抗病毒活性。Ketotifen fumarate 可用于自身免疫性脑脊髓炎 (EAE) 和预防哮喘发作的研究。
| 生物活性 | Ketotifen (HC 20-511) fumarate is an orally active second-generation noncompetitivehistamine 1 (H1)receptor blocker and mast cell stabilizer. Ketotifen fumarate can block 6-phosphogluconate dehydrogenase (PGD)in vitro. Ketotifen fumarate also has antiviral activity againstSARS-CoV-2andInfluenza virus. Ketotifen fumarate can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention[1][2][3][4]. |
| IC50& Target | Histamine 1, SARS-CoV-2, Influenza virus[1][3][4] |
体外研究
(In Vitro) | Ketotifen (0-100 μM; 2 or 4 days) inhibits SARS-CoV-2 with an EC50of 48.9 μM; and increases the percentage inhibition of SARS-CoV-2 to 79%, 83% and 93% when co-administers with 25, 50 and 100 μM Indomethacin, respectively[3].
Ketotifen (0-50 μM; 24 h) has inhibitory activity against PR8, pH1N1 and H3N2 with EC50s of 5.9 μM, 33.7 μM and 48.5 μM, respectively; and exhibits relatively low cytotoxicity in MDCK cells (EC50=291 μM)[4].
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体内研究
(In Vivo) | Ketotifen (80 mg/kg; i.g.; daily for 3 days) reduces end organ damage and mortality in mice infected with influenza virus[4].
Ketotifen fumarate (0.4 mg/kg; i.p.; daily for 10 days) reduces encephalomyelitis (EAE) prevalence and severity[5].
| Animal Model: | Female C57BL/6 mice (4-6 weeks; intranasal infection with 1×103TCID50of PR8 in 30 μL of DMEM)[4] | | Dosage: | 80 mg/kg | | Administration: | i.g.; daily for 3 days | | Result: | Reduced end organ damage and mortality in infected mice. |
| Animal Model: | Female C57BL/6 mice (5-6 weeks old; subcutaneously immunized with 150 μg of MOG35-55peptide containing 4 mg/mL ofMycobacterium tuberculosis)[5] | | Dosage: | 0.4 mg/kg | | Administration: | i.p.; daily for 10 days (from the 7th day of infection) | | Result: | Reduced EAE prevalence and severity; reduced oxidative stress status and inflammasome activation at the CNS; reduced the amount of T cells, especially Th1, in the CNS; downregulated local mRNA expression for mast cell enzymes and preserves blood-CNS barrier permeability; triggered lymphocyte accumulation in draining lymph nodes. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(235.02 mM) H2O : 16.67 mg/mL(39.18 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.3502 mL | 11.7509 mL | 23.5018 mL | | 5 mM | 0.4700 mL | 2.3502 mL | 4.7004 mL | | 10 mM | 0.2350 mL | 1.1751 mL | 2.3502 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： PBS Solubility: 37.5 mg/mL (88.13 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.88 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。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.88 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 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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