LY2886721生物活性
| 產(chǎn)品描述 | LY2886721是BACE抑制劑，用于治療阿爾茨海默癥。Phase 1/2。 | |||||
|---|---|---|---|---|---|---|
| 體外研究 | is an oral, small molecule of β-site amyloid protein cleaving enzyme (BACE) inhibitor with the potential to inhibit the synthesis of β-amyloid and thereby to slow the clinical progression of AD. [1] can also targetγ-secretase to nhibit the synthesis of β-amyloid. [2] | |||||
| 體內(nèi)研究 | ||||||
| 特征 | ||||||
不同實(shí)驗(yàn)動(dòng)物依據(jù)體表面積的等效劑量轉(zhuǎn)換表（數(shù)據(jù)來(lái)源于FDA指南）
| 狒狒 | 狗 | 猴 | 兔 | 豚鼠 | 大鼠 | 倉(cāng)鼠 | 小鼠 | |
| 重量 (kg) | 12 | 10 | 3 | 1.8 | 0.4 | 0.15 | 0.08 | 0.02 |
| 體表面積 (m2) | 0.6 | 0.5 | 0.24 | 0.15 | 0.05 | 0.025 | 0.02 | 0.007 |
| Km 系數(shù) | 20 | 20 | 12 | 12 | 8 | 6 | 5 | 3 |
| 動(dòng)物A (mg/kg) = 動(dòng)物B (mg/kg) × | 動(dòng)物B的Km系數(shù) |
| 動(dòng)物A的Km系數(shù) |
例如，依據(jù)體表面積折算法，將白藜蘆醇用于小鼠的劑量22.4 mg/kg 換算成大鼠的劑量，需要將22.4 mg/kg 乘以小鼠的Km系數(shù)（3），再除以大鼠的Km系數(shù)（6），得到白藜蘆醇用于大鼠的等效劑量為11.2 mg/kg。
| 大鼠劑量 (mg/kg) = 小鼠劑量 (22.4 mg/kg) × | 小鼠的Km系數(shù)(3) | = 11.2 mg/kg |
| 大鼠的Km系數(shù)(6) |
1
參考文獻(xiàn)
[1] Adru studies, 2012
[2] Townsend M, et al. J Alzheimers Dis, 2011, 24 Suppl 2, 43-52.
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01807026 | Completed | Alzheimer Disease|Healthy Volunteers | Eli Lilly and Company | March 2013 | Phase 1 |
| NCT01775904 | Completed | Healthy Volunteers | Eli Lilly and Company | February 2013 | Phase 1 |
| NCT01561430 | Terminated | Alzheimers Disease | Eli Lilly and Company | March 2012 | Phase 1|Phase 2 |
| NCT01534273 | Completed | Healthy Volunteers | Eli Lilly and Company | February 2012 | Phase 1 |
| NCT01367262 | Completed | Healthy Subjects | Eli Lilly and Company | June 2011 | Phase 1 |
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化學(xué)數(shù)據(jù)
點(diǎn)擊下載 (SDF格式文件)
| 分子量 | 390.41 |
|---|---|
| 化學(xué)式 | C18H16F2N4O2S |
| CAS號(hào) | 1262036-50-9 |
| 穩(wěn)定性 | 3年 -20℃粉狀 |
|---|---|
| 6月-80℃溶于DMSO | |
| 別名 |
| 溶解性 (25°C) * | 體外 | DMSO | 9 mg/mL (23 mM) |
|---|---|---|---|
| 水 | <1 mg/mL (<1 mM) | ||
| 乙醇 | <1 mg/mL (<1 mM) | ||
| * <1 mg/ml 指產(chǎn)品微溶或不溶 * 溶解度檢測(cè)是由Selleck技術(shù)部門檢測(cè)的，可能會(huì)和文獻(xiàn)中提供的溶解度有所差異，這是由于生產(chǎn)工藝和批次不同產(chǎn)生的正?，F(xiàn)象。 | |||
| Chemical Name | N-(3-((4aS,7aS)-2-amino-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4-fluorophenyl)-5-fluoropicolinamide |
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