5-HT4 antagonist 1 |
| رقم الكتالوجGC30314 |
مضاد 5-HT4 1 هو مضاد لمستقبلات 5-HT4 مع pKi يبلغ 9.6
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 261766-73-8
Sample solution is provided at 25 µL, 10mM.
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5-HT4 antagonist 1 is a 5-HT4 receptor antagonist with a pKi of 9.6.
5-HT4 antagonist 1 (compound 6b) is a 5-HT4 receptor antagonist with a pKi of 9.6.
5-HT4 antagonist 1 (compound 6b) demonstrates good exposure and prolongs t1/2 in other species, including the mouse (t1/2 7 h), rat (t1/2 12 h) and mini-pig (t1/2 21 h). In Phase I clinical trial, it is found that 5-HT4 antagonist 1 has good oral bioavailability with a steady state plasma t1/2 of >100 h[1].
[1]. Clark RD, et al. Identification of a 5-HT4 receptor antagonist clinical candidate through side-chain modification. Bioorg Med Chem Lett. 2005 Mar 15;15(6):1697-700.
| Cas No. | 261766-73-8 | SDF | |
| Canonical SMILES | O=C(C1=C2OCCOC2=CC=C1)NCC3CCN(CCCS(=O)(N4CCN(C)CC4)=O)CC3 | ||
| Formula | C23H36N4O5S | M.Wt | 480.62 |
| الذوبان | DMSO : 20 mg/mL (41.61 mM; ultrasonic and warming and adjust pH to 3 with HCl 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0806 mL | 10.4032 mL | 20.8065 mL |
| 5 mM | 0.4161 mL | 2.0806 mL | 4.1613 mL |
| 10 mM | 0.2081 mL | 1.0403 mL | 2.0806 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)
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