5-HT2B antagonist-1 |
| رقم الكتالوجGC65568 |
5-HT2B antagonist-1 هو مضاد لمستقبلات 5-HT2B النشط عن طريق الفم بقيمة IC50 تبلغ 33.4 نانومتر
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Cas No.: 393129-91-4
Sample solution is provided at 25 µL, 10mM.
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5-HT2B antagonist-1 is an orally active 5-HT2B receptor antagonist with an IC50 value of 33.4 nM. 5-HT2B antagonist-1 can be used in studies of diseases characterized by 5-HT2B receptor signaling, such as hepatocellular carcinoma, cardiovascular disease or gastrointestinal disease[1][2].
5-HT2B antagonist-1 (compound 5g) has some sodium channel binding activity with IC50 values in the range of 12.6 to 57.5 μM[1].5-HT2B antagonist-1 (coumpound 1-e) inhibits 5-HT2B receptor activity by less than 50% at 1 μM in CHO-K1 cell lines[3].
5-HT2B antagonist-1 (compound 15) (oral gavage, 30 mg/kg) can reduce visceral hypersensitivity significantly in irritable bowel syndrome (IBS) rats[2].
[1]. Xiang Ma, et al. Synthesis and in vitro evaluation of 2,4-diamino-1,3,5-triazine derivatives as neuronal voltage-gated sodium channel blockers. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5644
[2]. Yu Zhou, et al. Structure-Based Discovery of Novel and Selective 5-Hydroxytryptamine 2B Receptor Antagonists for the Treatment of Irritable Bowel Syndrome. J Med Chem. 2016 Jan 28;59(2):707-20.
[3]. Huang Niu, et al. 5-HT2B Antagonists. WO2015158214
5-HT2BReceptor 33.4nM(IC50) |
| Cas No. | 393129-91-4 | SDF | |
| Formula | C11H14BrN5 | M.Wt | 296.17 |
| الذوبان | DMSO : ≥ 33.33 mg/mL (112.54 mM); H2O : 12.5 mg/mL (42.21 mM; ultrasonic and warming and heat to 60°C) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.3764 mL | 16.8822 mL | 33.7644 mL |
| 5 mM | 0.6753 mL | 3.3764 mL | 6.7529 mL |
| 10 mM | 0.3376 mL | 1.6882 mL | 3.3764 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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