Azelaprag
Based on 1 Customer Validation
Azelaprag (Example 263.0) is a candidate active molecule for an Apelin receptor agonist with an EC50 of 0.32 nM for the apelin receptor.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 2049980-18-7
- Formula: C25H29N7O4S
- Molecular Weight:523.61
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
EC50: 0.32 nM (Apelin receptor)[1]
Azelaprag (AMG 986) (0.5 mg/kg for i.v., 2 mg/kg for p.o.) shows a T1/2 of 2.4 h in rat and 4.2 h in dog by i.v., and oral bioavailability (F%) of 73% in rat and 97% in dog[2].
Pharmacokinetic parameters for Azelaprag(AMG 986) in rat and dog[2]
| Species | CL (L/h/kg) | VSS (L/kg) | T1/2 (h) | Oral F(%) |
| Rat | 0.78 | 0.6 | 2.4 | 73 |
| Dog | 0.08 | 0.19 | 4.2 | 97 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ZSF1 obese rats (19 weeks old), rat model of impaired metabolic function[2]
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Dosage:1 mg/kg/min
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Administration:Acute IV infusion
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Result:Increased ejection fraction but not mean arterial pressure in a rat model of impaired metabolic function.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2049980-18-7
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Appearance Solid
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Molecular Weight 523.61
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Formula C25H29N7O4S
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Color White to light yellow
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SMILES
O=S(NC1=NN=C(C2=CN=CC(C)=C2)N1C(C(OC)=CC=C3)=C3OC)([C@@H](C)[C@@H](C4=NC=C(C)C=N4)C)=O
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Synonyms
AMG 986
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 5 mg/mL (9.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (276 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9098 mL | 9.5491 mL | 19.0982 mL | 47.7455 mL |
| 5 mM | 0.3820 mL | 1.9098 mL | 3.8196 mL | 9.5491 mL |
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