ML314 |
カタログ番号GC18216
One-Click Copy Product Info
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ML314 は NTR1 の強力な分子アゴニストです (EC50 =1.9 μM)。はNTR2とGPR35に対して良好な選択性を示したが、Ca2+ 動員を刺激しなかった。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1448895-09-7
Sample solution is provided at 25 µL, 10mM.
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ML314 is a potent molecule agonist of NTR1 (EC50 = 1.9 μM); showed good selectivity against NTR2 and GPR35, but did not stimulate Ca2+ mobilization.IC50 value: 1.9 uM (EC50) [1]Target: NTR1 agonistMedicinal chemistry optimization of MLS-0233108 led to ML314, the most potent molecule in this second series that exhibited full agonist behavior (100 %) on NTR1 (EC50 = 1.9 μM). ML314 showed good selectivity against NTR2 and GPR35, but did not stimulate Ca2+ mobilization. ML314 is potentially a biased agonist operating via the β-arrestin pathway rather than the traditional Gq coupled pathway. Signaling mediated by β-arrestin has distinct biochemical and functional consequences that may lead to physiological advantages as described below. This probe report describes the discovery and properties of ML301 and summarizes the HTS and follow-up campaign, which identified ML314.
References:
[1]. Hershberger P, et al. Small Molecule Agonists for the Neurotensin 1 Receptor (NTR1 Agonists). Probe Reports from the NIH Molecular Libraries Program
| Cas No. | 1448895-09-7 | SDF | |
| Chemical Name | 2-cyclopropyl-6,7-dimethoxy-4-[4-(2-methoxyphenyl)-1-piperazinyl]-quinazoline | ||
| Canonical SMILES | COC1=C(OC)C=C(C(N2CCN(C3=CC=CC=C3OC)CC2)=NC(C4CC4)=N5)C5=C1 | ||
| Formula | C24H28N4O3 | M.Wt | 420.5 |
| 溶解度 | DMSO: >100mM | 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 | 2.3781 mL | 11.8906 mL | 23.7812 mL |
| 5 mM | 475.6 μL | 2.3781 mL | 4.7562 mL |
| 10 mM | 237.8 μL | 1.1891 mL | 2.3781 mL |
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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.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)