中文名称: | DMP 777 | ||||
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英文名称: | DMP 777 | ||||
别名: | DMP 777 L-694458;(S)-N-((R)-1-(Benzo[d][1,3]dioxol-5-yl)butyl)-3,3-diethyl-2-(4-(4-methylpiperazine-1-carbonyl)phenoxy)-4-oxoazetidine-1-carboxamide | ||||
CAS No: | 157341-41-8 | 分子式: | C31H40N4O6 | 分子量: | 564.67 |
CAS No: | 157341-41-8 | ||||
分子式: | C31H40N4O6 | ||||
分子量: | 564.67 |
基本信息
产品编号: |
D11100 |
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产品名称: |
DMP 777 |
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CAS: |
157341-41-8 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
564.67 |
-20℃ |
一个月 |
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化学名: |
(S)-N-((R)-1-(Benzo[d][1,3]dioxol-5-yl)butyl)-3,3-diethyl-2-(4-(4-methylpiperazine-1-carbonyl)phenoxy)-4-oxoazetidine-1-carboxamide |
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Solubility (25°C): |
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体外:
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DMSO |
35mg/mL (61.9831mM; Need ultrasonic) |
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Ethanol |
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Water |
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体内(现配现用): |
1.请依序添加每种溶剂:10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility: ≥ 2.5mg/mL (4.43mM); Clear solution |
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此⽅案可获得 ≥ 2.5mg/mL (4.43mM,饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例,取 100μL 25.0mg/mL 的澄清 DMSO 储备液加到 400μL PEG300 中,混合均匀;向上述体系中加⼊ 50μL Tween-80,混合均匀;然后继续加⼊ 450μL ⽣理盐⽔定容⾄ 1mL。 |
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2.请依序添加每种溶剂:10% DMSO→90% (20% SBE-β-CD in saline) Solubility: 2.5mg/mL (4.43mM); Suspended solution; Need ultrasonic |
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此⽅案可获得 2.5mg/mL (4.43mM) 的均匀悬浊液,悬浊液可⽤于⼝服和腹腔注射。 以 1mL ⼯作液为例,取 100μL 25.0mg/mL 的澄清 DMSO 储备液加到 900μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中,混合均匀。 |
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3.请依序添加每种溶剂:10% DMSO→90% corn oil Solubility: ≥ 2.5mg/mL (4.43mM); Clear solution |
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此⽅案可获得 ≥ 2.5mg/mL (4.43mM,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 1mL ⼯作液为例,取 100μL 25.0mg/mL 的澄清 DMSO 储备液加到 900μL ⽟⽶油中,混合均匀。 |
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4.请依序添加每种溶剂:5% DMSO→40% PEG300→5% Tween-80→50% saline Solubility: ≥ 2.5mg/mL (4.43mM); Clear solution |
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5.请依序添加每种溶剂:5% DMSO→95% (20% SBE-β-CD in saline) Solubility: ≥ 2.5mg/mL (4.43mM); Clear solution |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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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。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
1.7709mL |
8.8547mL |
17.7095mL |
5mM |
0.3542mL |
1.7709mL |
3.5419mL |
10mM |
0.1771mL |
0.8855mL |
1.7709mL |
生物活性
产品描述 |
一种有效的,选择性的,可口服的 human leukocyte elastase (HLE) 抑制剂。 |
靶点 |
Human leukocyte elastase (HLE) |
体内研究 |
DMP-777-treated rats show a marked decrease in H/K-ATPase staining parietal cells. DMP-777-induced loss of parietal cells is significantly ameliorated with coadministration of omeprazole. DMP-777-treated animals demonstrates marked foveolar hyperplasia in the fundus with prominent expansion of diastase-resistant, PAS-positive surface mucous cells. When DMP-777 is coadministeredwith omprazole, there is a significant decrease in BrdUpositive S-phase cells compared with rats thatreceive DMP-777 alone. After oral dosing of monkeys at 40mg/kg with DMP-777 the only stereoisomer detected in the post-dose plasma samples is the starting material DMP-777, and no inversion of the configuration at positions 'a' and 'b' of DMP-777 has occurred in vivo. Mist1-/- mice treated with DMP-777 show fewer chief cell to SPEM transitions. Mist1-/- mice treated with L635 demonstrates significantly fewer proliferative SPEM cells compared to control mice |
推荐实验方法(仅供参考)
Animal Administration |
Groups 1A and 1B receive control vehicle instead of omeprazole and DMP-777. Group 2A and 2B are dosed with DMP-777 once daily on Study Day 3 or Days 3 and 4, respectively, and receive control vehicle instead of omeprazole. Groups 3A and 3B are treated with omeprazole twice daily on Study Days 1 to 3 or Days 1 to 4, respectively, and receive control vehicle instead of DMP-777. Groups 4A and 4B are dosed with both omeprazole and DMP-777. On Study Days 1 and 2, animals are pretreated with omeprazole twice daily, the dosing intervals separated by approximately 6 hr. On Study Day 3 (Group 4A) or Days 3 and 4 (Group 4B), omeprazole is coadministered with DMP-777. The first dose of omeprazole is administered approximately 1 hr prior to the dose of DMP-777. The second dose is approximately 6 hr after the last dose of DMP-777. Groups 1A, 2A, 3A, and 4A are sacrificed on Day 4. Groups 1B, 2B, 3B, and 4B are sacrificed on Day 5. Bromodeoxyuridine (BrdU) is administered by intraperitoneal injection to all the rats, 2 hr prior to necropsy. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )