GRA Ex-25 |
رقم الكتالوجGC31379
One-Click Copy Product Info
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GRA Ex-25 هو مثبط لمستقبلات الجلوكاجون ، مع IC من 56 و 55 نانومتر لمستقبلات الجرذان والجلوكاجون البشري ، على التوالي
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.
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GRA Ex-25 is a potent glucagon receptor inhibitor with IC50 of 56nm and 55nM for rat and human glucagon receptors, respectively[1]. GRA Ex-25 binds to the human glucagon receptor (h-GlucRbind) with a Ki of 63nM and moderates glucagon-induced adenylate cyclase inhibition (h-GlucRcyclase) with a Ki of 254nM[2]. GRA Ex-25 (3mg/kg; i.v.; once) reduces blood glucose levels induced by exogenous glucagon in a rat model, possibly due to direct inhibition of glucagon-stimulated hepatic glucose output[2].
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.
[2].Lau J, Behrens C, et,al . New beta-alanine derivatives are orally available glucagon receptor antagonists. J Med Chem. 2007 Jan 11;50(1):113-28.
| Molecular Docking of the Receptor¨CLigand Complex[1]: | |
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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. |
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Applications |
Gra Ex-25 is bonded to Ser350 and Lys349 amino acids of GCGR through hydrogen bonding. |
| Animal experiment [2]: | |
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Animal models |
Glucagon challenged rats |
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Preparation Method |
Anesthetized animals were given an intravenous dose of GRA Ex-25 min prior to a 3mg/kg glucagon load. |
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Dosage form |
3mg/kg; i.v.; once |
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Applications |
GRA Ex-25 (3mg/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. [2].Lau J, Behrens C, et,al . New beta-alanine derivatives are orally available glucagon receptor antagonists. J Med Chem. 2007 Jan 11;50(1):113-28. | |
| 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 |
| الذوبان | DMSO : ≥ 32 mg/mL (56.78 mM) | Storage | Store at -20°C |
| 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 | 1.7743 mL | 8.8714 mL | 17.7428 mL |
| 5 mM | 354.9 μL | 1.7743 mL | 3.5486 mL |
| 10 mM | 177.4 μL | 887.1 μL | 1.7743 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: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)