MS48107 |
カタログ番号GC63081
One-Click Copy Product Info
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MS48107 は、G タンパク質共役受容体 68 (GPR68) の強力かつ選択的なポジティブ アロステリック モジュレーターです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2375070-79-2
Sample solution is provided at 25 µL, 10mM.
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MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can readily cross the blood-brain barrier (BBB) in mice[1].
5-HT2B has moderate binding affinity to MS48107 (compound 71) with a Ki value of 219 nM. At 5-HT2B receptors, MS48107 shows no agonist activity but display weak antagonist activity with a Ki value of 310 nM, respectively[1].MS48107 (compound 71) has agonist activity only at the MT1 and MT2 receptors. MS48107 is a weak full agonist at the MT1 receptor (EC50 = 320 nM) and a weak partial agonist activity at the MT2 receptor (EC50 = 540 nM). MS48107 displays low binding affinities to MT1 (5900 nM) and MT2 (1100 nM) receptors[1].
For MS48107 (compound 71), a single intraperitoneal injection at the dose of 25 mg/kg leads to high exposure levels (above 10 μM) in both plasma and brain at 0.5 h in mice (Swiss Albino mice). The high compound exposure levels in both plasma and brain are maintained for 2 h[1].
[1]. Xufen Yu, et al. Design, Synthesis, and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68). J Med Chem. 2019 Aug 22;62(16):7557-7574.
| Cas No. | 2375070-79-2 | SDF | |
| Formula | C23H20FN5O2 | M.Wt | 417.44 |
| 溶解度 | DMSO : 100 mg/mL (239.56 mM; Need ultrasonic) | 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 | 2.3956 mL | 11.9778 mL | 23.9555 mL |
| 5 mM | 479.1 μL | 2.3956 mL | 4.7911 mL |
| 10 mM | 239.6 μL | 1.1978 mL | 2.3956 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 saline, 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: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)