1. GPCR/G Protein
  2. Apelin Receptor (APJ)
  3. Azelaprag

Azelaprag (Example 263.0) is an apelin receptor agonist agent candidate.

For research use only. We do not sell to patients.

Azelaprag Chemical Structure

Azelaprag Chemical Structure

CAS No. : 2049980-18-7

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 1670 In-stock
Solid
1 mg USD 480 In-stock
5 mg USD 1450 In-stock
10 mg USD 2400 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Azelaprag (Example 263.0) is an apelin receptor agonist agent candidate[1].

IC50 & Target

Apelin receptor[1]

In Vivo

Azelaprag (AMG 986) (1 mg/kg/min, acute i.v. infusion) increases cardiac reserve during Dobutamine (HY-15746A) challenge in a rat model of impaired metabolic function[2].
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]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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
Animal Model: ZSF1 obese rats (19 weeks old), rat model of impaired metabolic function[2]
Dosage: 1 mg/kg/min
Administration: Acute IV infusion
Result: Increased ejection fraction but not mean arterial pressure in a rat model of impaired metabolic function.
Clinical Trial
Molecular Weight

523.61

Formula

C25H29N7O4S

CAS No.
Appearance

Solid

Color

White to light yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9098 mL 9.5491 mL 19.0982 mL
5 mM 0.3820 mL 1.9098 mL 3.8196 mL
View the 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.

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.84%

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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Azelaprag Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Azelaprag
Cat. No.:
HY-109111
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