| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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| 体内研究 (In Vivo) |
在胆汁淤积性肝损伤 (CLI) 大鼠中,京尼平 1-β-D-龙胆二糖苷 (京尼平龙胆二糖苷) 具有中等的终末消除半衰期 (11.4 mg/kg),t1/2=1.65±0.87 小时和 2.43±2.30 小时分别(分别为 11.4 mg/kg)[1]。
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| 动物实验 |
- Cholestatic liver disease rat model establishment: Male Sprague-Dawley rats (200–220 g) were randomly divided into normal group and cholestatic group. The cholestatic model was induced by intragastric administration of α-naphthylisothiocyanate (ANIT) at a dose of 60 mg/kg. The normal group received an equal volume of vehicle. After 72 hours of ANIT administration, the success of the cholestatic model was confirmed by detecting serum biochemical indicators (ALT, AST, ALP, TBIL) [1]
- Comparative pharmacokinetic study protocol: Both normal and cholestatic rats were given Zhi-Zi-Da-Huang decoction intragastrically at a dose of 10 mL/kg (equivalent to the crude drug dose of 13.5 g/kg). Blood samples (0.3 mL) were collected from the orbital venous plexus at pre-determined time points (0, 0.083, 0.167, 0.25, 0.5, 1, 2, 4, 6, 8, 12, 24, 48 h) after administration. The blood samples were centrifuged at 3500 rpm for 10 minutes to separate plasma, which was stored at -80°C until analysis [1] |
| 药代性质 (ADME/PK) |
- In normal rats: The main pharmacokinetic parameters of Genipin 1-β-D-gentiobioside were as follows: Cmax (peak plasma concentration) = 128.6 ± 15.3 ng/mL; Tmax (time to reach Cmax) = 0.25 ± 0.08 h; AUC0-t (area under the plasma concentration-time curve from 0 to last measurable time) = 326.8 ± 38.5 ng·h/mL; AUC0-∞ (area under the plasma concentration-time curve from 0 to infinity) = 342.5 ± 41.2 ng·h/mL; t1/2z (terminal elimination half-life) = 8.6 ± 1.2 h; CLz/F (apparent clearance) = 39.4 ± 4.8 L/kg/h; Vz/F (apparent volume of distribution) = 486.3 ± 56.7 L/kg [1]
- In cholestatic rats: The pharmacokinetic parameters of Genipin 1-β-D-gentiobioside were significantly altered: Cmax = 89.3 ± 11.6 ng/mL (decreased by 30.6% compared to normal rats); Tmax = 0.5 ± 0.12 h (prolonged); AUC0-t = 489.6 ± 52.3 ng·h/mL (increased by 50.1%); AUC0-∞ = 512.8 ± 55.7 ng·h/mL (increased by 50.0%); t1/2z = 15.3 ± 2.1 h (prolonged by 77.9%); CLz/F = 26.3 ± 3.2 L/kg/h (decreased by 33.2%); Vz/F = 598.7 ± 68.4 L/kg (increased by 23.1%) [1] - The absorption rate of Genipin 1-β-D-gentiobioside was reduced, while its plasma exposure and elimination half-life were significantly increased in cholestatic rats, indicating that cholestatic liver disease affects the absorption and elimination of the compound [1] |
| 参考文献 | |
| 其他信息 |
Genipin 1-beta-gentiobioside is a terpene glycoside.
Genipin 1-gentiobioside has been reported in Gardenia jasminoides and Genipa americana with data available. - Genipin 1-β-D-gentiobioside is an iridoid glycoside component isolated from Zhi-Zi-Da-Huang decoction, a traditional Chinese medicinal formula [1] - The pharmacokinetic behavior of Genipin 1-β-D-gentiobioside differs significantly between normal and cholestatic rats, which provides a pharmacokinetic basis for the clinical application of Zhi-Zi-Da-Huang decoction in the treatment of cholestatic liver disease [1] |
| 分子式 |
C₂₃H₃₄O₁₅
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|---|---|
| 分子量 |
550.51
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| 精确质量 |
550.189
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| CAS号 |
29307-60-6
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| PubChem CID |
3082301
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| 外观&性状 |
White to light yellow solid powder
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| 密度 |
1.6±0.1 g/cm3
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| 沸点 |
835.3±65.0 °C at 760 mmHg
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| 闪点 |
281.0±27.8 °C
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| 蒸汽压 |
0.0±0.6 mmHg at 25°C
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| 折射率 |
1.647
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| LogP |
-1.62
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| tPSA |
234.29
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| 氢键供体(HBD)数目 |
8
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| 氢键受体(HBA)数目 |
15
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| 可旋转键数目(RBC) |
9
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| 重原子数目 |
38
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| 分子复杂度/Complexity |
894
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| 定义原子立体中心数目 |
13
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| SMILES |
COC(=O)C1=CO[C@H]([C@H]2[C@@H]1CC=C2CO)O[C@H]3[C@@H]([C@H]([C@@H]([C@H](O3)CO[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O)O)O)O
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| InChi Key |
FYZYXYLPBWLLGI-AUOPOVQUSA-N
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| InChi Code |
InChI=1S/C23H34O15/c1-33-20(32)10-6-34-21(13-8(4-24)2-3-9(10)13)38-23-19(31)17(29)15(27)12(37-23)7-35-22-18(30)16(28)14(26)11(5-25)36-22/h2,6,9,11-19,21-31H,3-5,7H2,1H3/t9-,11-,12-,13-,14-,15-,16+,17+,18-,19-,21+,22-,23+/m1/s1
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| 化学名 |
methyl (1S,4aS,7aS)-7-(hydroxymethyl)-1-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-[[(2R,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxymethyl]oxan-2-yl]oxy-1,4a,5,7a-tetrahydrocyclopenta[c]pyran-4-carboxylate
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| 别名 |
Genipin 1-gentiobiosideGenipin 1 β D gentiobioside
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| HS Tariff Code |
2934.99.9001
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| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month 注意: 本产品在运输和储存过程中需避光。 |
| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| 溶解度 (体外实验) |
Ethanol : ~125 mg/mL (~227.06 mM)
DMSO : ~100 mg/mL (~181.65 mM) |
|---|---|
| 溶解度 (体内实验) |
配方 1 中的溶解度: ≥ 2.5 mg/mL (4.54 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
例如,若需制备1 mL的工作液,可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中,混匀;然后向上述溶液中加入50 μL Tween-80,混匀;加入450 μL生理盐水定容至1 mL。 *生理盐水的制备:将 0.9 g 氯化钠溶解在 100 mL ddH₂O中,得到澄清溶液。 配方 2 中的溶解度: ≥ 2.5 mg/mL (4.54 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 例如,若需制备1 mL的工作液,可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中,混匀。 *20% SBE-β-CD 生理盐水溶液的制备(4°C,1 周):将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中,得到澄清溶液。 View More
配方 3 中的溶解度: ≥ 2.5 mg/mL (4.54 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8165 mL | 9.0825 mL | 18.1650 mL | |
| 5 mM | 0.3633 mL | 1.8165 mL | 3.6330 mL | |
| 10 mM | 0.1816 mL | 0.9082 mL | 1.8165 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。