| 中文名称: | TAN-452 | ||||
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| 英文名称: | TAN-452 | ||||
| 别名: | Ethyl (4bS,8R,8aS,14bR)-7-(cyclopropylmethyl)-5,6,7,8,8a,9,14,14b-octahydro-1,8a-dihydroxy-4,8-methanobenzofuro[2,3-a]pyrido[4,3-b]carbazole-12-carboxylate | ||||
| CAS No: | 892039-23-5 | 分子式: | C29H30N2O5 | 分子量: | 486.56 |
| CAS No: | 892039-23-5 | ||||
| 分子式: | C29H30N2O5 | ||||
| 分子量: | 486.56 | ||||
基本信息
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产品编号： |
T11469 |
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产品名称： |
TAN-452 |
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CAS: |
892039-23-5 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
二年 |
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分子量 |
486.56 |
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化学名： |
Ethyl(4bS,8R,8aS,14bR)-7-(cyclopropylmethyl)-5,6,7,8,8a,9,14,14b-octahydro-1,8a-dihydroxy-4,8-methanobenzofuro[2,3-a]pyrido[4,3-b]carbazole-12-carboxylate |
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Solubility (25°C)： |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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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。 |
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生物活性
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产品描述 |
一种具有口服活性，选择性的外周作用的 δ 阿片受体 (DOR) 拮抗剂。 |
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靶点 |
Ki:0.47nM (DOR),36.56nM (MOR) and 5.31nM (KOR) Kb:0.21nM (DOR),9.43nM (MOR) and 7.18nM (KOR) |
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体内研究 |
TAN-452 (1,3,10mg/kg for p.o.or 0.3,1,3 mg/kg for s.c.) suppresses morphine-induced emesis in ferrets.TAN-452 (30mg/kg/2mL for PO or 3mg/kg/mL for IV) has a T1/2 of 2.1 hours.TAN-452 suppresses morphine-induced small intestinal transit (SIT) inhibition in a dose-dependent manner.Administration of TAN-452 at 30mg/kg alone does not affect SIT.TAN-452 (10,30mg/kg;s.c.) significantly suppresses morphine-induced antinociception 30 min after administration.TAN-452 (po) produces no effect up to 300mg/kg. |
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Animal Model: |
Male ferrets (1.3-1.9kg) |
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Dosage: |
1,3,10mg/kg (p.o.) or 0.3,1,3mg/kg (s.c.) |
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Administration: |
PO or SC; before morphine |
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Result: |
Prevented morphine-induced emesis in half of the animals with orally administered of 1mg/kg and completely abolished emesis at 3 and 10mg/kg.Completely abolished emesis by subcutaneous injection at 0.3,1,and 3mg/kg. |
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Animal Model: |
Crj:CD(SD) IGS male rats (7 weeks old) |
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Dosage: |
30mg/kg/2mL for PO or 3mg/kg/mL for IV (Pharmacokinetic Analysis) |
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Administration: |
Orally or intravenously |
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Result: |
Had a T1/2 of 2.1 hours,a CL of 78.1mL/min•kg,a Vss of 12.1L/kg,and a Cmax of 526ng/mL. |
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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 )
