GRA Ex-25 |
| Catalog No.GC31379 |
GRA Ex-25는 쥐와 인간 글루카곤 수용체에 대해 IC50이 각각 56 및 55nM인 글루카곤 수용체 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 307983-31-9
Sample solution is provided at 25 µL, 10mM.
GlpBio Products Cited In Reputable Papers
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Product Documents
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Protocol
| Molecular Docking of the Receptor¨CLigand Complex[1]: | |
|
Preparation Method |
The receptor and small ligand molecules Gra EX-25 were used to conduct molecular docking of 5XEZ-A with dauricine and Gra Ex-25 using Vina computing under the calculation conditions screened. In addition, scoring data and PyMol were used to analyze the ligand and receptor amino acid binding way. |
|
Applications |
Gra Ex-25 is bonded to Ser350 and Lys349 amino acids of GCGR through hydrogen bonding. |
| Animal experiment [2]: | |
|
Animal models |
Glucagon challenged rats |
|
Preparation Method |
Anesthetized animals were given an intravenous dose of GRA Ex-25 min prior to a 3 ¦̧/kg glucagon load. |
|
Dosage form |
1-3mg/ml GRA Ex-25 |
|
Applications |
GRA Ex-25 (3 mg/kg) significantly reduced blood glucose levels in rats with elevated blood glucose induced by exogenous glucagon. |
|
References: [1]. Li L, Dai S, et,al . Antagonistic Effect and In Vitro Activity of Dauricine on Glucagon Receptor. J Nat Prod. 2022 Aug 26;85(8):2035-2043. doi: 10.1021/acs.jnatprod.2c00446. Epub 2022 Jul 14. PMID: 35834753. | |
| Cas No. | 307983-31-9 | SDF | |
| Canonical SMILES | O=C(O)CCNC(C1=CC=C(CN([C@H]2CC[C@H](C(C)(C)C)CC2)C(NC3=CC=C(OC(F)(F)F)C=C3)=O)C=C1)=O | ||
| Formula | C29H36F3N3O5 | M.Wt | 563.61 |
| Solubility | DMSO : ≥ 32 mg/mL (56.78 mM) | 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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
Complete Stock Solution Preparation Table
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.7743 mL | 8.8714 mL | 17.7428 mL |
| 5 mM | 0.3549 mL | 1.7743 mL | 3.5486 mL |
| 10 mM | 0.1774 mL | 0.8871 mL | 1.7743 mL |
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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.
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리뷰
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