规格 | 价格 | |
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100mg | ||
250mg | ||
500mg |
体外研究 (In Vitro) |
680C91 是一种有效 (Ki=51 nM) 的选择性 TDO 抑制剂,在 10 μM 浓度下对吲哚胺 2,3-双加氧酶、单胺氧化酶 A 和 B、5-HT 摄取和 5-HT1A,1D,2A 无抑制活性、 和 2C 受体[2]。
大鼠原位肝脏灌注和大鼠肝细胞分解代谢色氨酸的能力被 680C91 抑制[2]。 Tdo2 可能控制细胞分裂并促进蜕膜标志物 Dtprp 的表达在蜕膜和子宫基质细胞中。 24 小时时,子宫蜕膜细胞的增殖能力同样受到 Tdo2 抑制剂 680C91 的抑制[3]。 I 型胶原蛋白 (COL1A1) 和 III 型胶原蛋白 (COL3A1) 的表达受到剂量依赖性的显着抑制。将 680C91(25 和 50 μM)应用于平滑肌瘤平滑肌细胞 (LSMC) 和子宫肌层平滑肌细胞 (MSMC) 的球体时的方式[4]。 |
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体内研究 (In Vivo) |
在急性治疗中,15 mg/kg 剂量的 680C91 会升高大脑中的色氨酸水平[5]。
|
细胞实验 |
细胞系: 子宫基质细胞
浓度: 0.01, 0.05, 0.1, 0.5, 1, 5, 10 μM 孵育时间: 24 小时 结果: 5 ℃时基质细胞增殖活性显着降低和10μM。 |
动物实验 |
Animal Model: C57Bl6/NCrl male mice, 13–18 weeks of age[5]
Dosage: 15 mg/kg Administration: Administered per os Result: caused a notable rise in tryptophan in the brain. |
参考文献 |
分子式 |
C15H11FN2
|
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分子量 |
238.26
|
CAS号 |
163239-22-3
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SMILES |
C1=CC(=CN=C1)/C=C/C2=CNC3=C2C=CC(=C3)F
|
InChi Key |
YBSDQTBCNYWBMX-ONEGZZNKSA-N
|
InChi Code |
InChI=1S/C15H11FN2/c16-13-5-6-14-12(10-18-15(14)8-13)4-3-11-2-1-7-17-9-11/h1-10,18H/b4-3+
|
化学名 |
6-fluoro-3-[(E)-2-pyridin-3-ylethenyl]-1H-indole
|
存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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)
|
溶解度 (体外) |
DMSO : 48~125 mg/mL ( 201.46~524.64 mM )
Ethanol : 25 mg/mL |
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溶解度 (体内) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 请根据您的实验动物和给药方式选择适当的溶解配方/方案: 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 | 4.1971 mL | 20.9855 mL | 41.9710 mL | |
5 mM | 0.8394 mL | 4.1971 mL | 8.3942 mL | |
10 mM | 0.4197 mL | 2.0985 mL | 4.1971 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) 。
In situ hybridization of Tdo2 expression in mouse uteri during early pregnancy on days 3 (B), 5 (C), 6 (D), 7 (E), and 8 (F). [1].Differential expression and regulation of Tdo2 during mouse decidualization. J Endocrinol. 2013 Dec 2;220(1):73-83. td> |
Real-time PCR analysis of Tdo2 expression in mouse uterus on days 1–8 during pregnancy. [1].Differential expression and regulation of Tdo2 during mouse decidualization. J Endocrinol. 2013 Dec 2;220(1):73-83. td> |
Tdo2 expression during pseudopregnancy and artificial decidualization.[1].Differential expression and regulation of Tdo2 during mouse decidualization. J Endocrinol. 2013 Dec 2;220(1):73-83. td> |
Real-time PCR analysis of Dtprp (A) and Tdo2 (B) expression in in vitro decidualization of uterine stromal cells.[1].Differential expression and regulation of Tdo2 during mouse decidualization. J Endocrinol. 2013 Dec 2;220(1):73-83. td> |
Effects of 8-Br-cAMP and H89 on Tdo2 expression in the uterine stromal cells. [1].Differential expression and regulation of Tdo2 during mouse decidualization. J Endocrinol. 2013 Dec 2;220(1):73-83. td> |
Hormonal regulation of Tdo2 expression. (A) Real-time PCR analysis of Tdo2 expression in ovariectomized mouse uterus after estrogen (E) treatments for 0, 1, 3, 6, 12, and 24 h.[1].Differential expression and regulation of Tdo2 during mouse decidualization. J Endocrinol. 2013 Dec 2;220(1):73-83. td> |