GNE-9822 是一种口服有效的选择性的ITK抑制剂，Ki值为 0.7 nM。GNE-9822 具有良好的 ADME 特性。GNE-9822 可用于哮喘的研究。
| 生物活性 | GNE-9822 is a potent, orally active and selectiveITKinhibitor with aKivalue of 0.7 nM. GNE-9822 has good ADME properties. GNE-9822 can be used in research of asthma[1]. |
体外研究
(In Vitro) | GNE-9822 (compound 28) 抑制 PLCγ 的磷酸化，IC50值为 55 nM[1]。
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体内研究
(In Vivo) | GNE-9822 (compound 28; po and iv; 1 and 5 mg/kg) 在小鼠和大鼠中观察到良好的生物利用度和半衰期[1]。
| Animal Model: | BALB/c mouse and Sprague-Dawley rats[1] | | Dosage: | 1 and 5 mg/kg | | Administration: | po (5 mg/kg) and iv (1 mg/kg) | | Result: | 1.19| species | route | dose volume (mL/kg) | dose (mg/kg) | Cmax(μM) | AUC (μM·h) | Cl (mL/min/kg) | T1/2(h) | Vss(L/kg) | %F | | mouse (BALB/c) | IV | 1.0 | 1.0 | | 1.5 | 40 | 2.9 | 10 | | | mouse (BALB/c) | PO | 5.0 | 50 | 3.8 | 2.7 | | | | 36 |
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| Animal Model: | BALB/c mouse and Sprague-Dawley rats[1] | | Dosage: | 1 and 5 mg/kg | | Administration: | po (5 mg/kg) and iv (1 mg/kg) | | Result: | 1.19| species | route | dose volume (mL/kg) | dose (mg/kg) | Cmax(μM) | AUC (μM·h) | Cl (mL/min/kg) | T1/2(h) | Vss(L/kg) | %F | | rat (Sprague-Dawley | IV | 1.0 | 1.0 | | 0.6 | 70 | 3.0 | 14 | | | rat (Sprague-Dawley | PO | 2.0 | 5.0 | 0.2 | 1.1 | | | | 40 |
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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 : 62.5 mg/mL(148.61 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.3778 mL | 11.8892 mL | 23.7784 mL | | 5 mM | 0.4756 mL | 2.3778 mL | 4.7557 mL | | 10 mM | 0.2378 mL | 1.1889 mL | 2.3778 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。 |
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