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

Azelaprag  (Synonyms: AMG 986)

製品番号: HY-109111 純度: 99.94%
COA 取扱説明書 Technical Support

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.

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Azelaprag

Azelaprag 構造式

CAS 番号 : 2049980-18-7

容量 価格（税別） 在庫状況 数量
1 mg $160 在庫あり
5 mg $320 在庫あり
10 mg $500 在庫あり
25 mg $760 在庫あり
50 mg $1140 在庫あり
100 mg $1600 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Azelaprag 関連抗体

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製品説明

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[1].

IC50 & Target

EC50: 0.32 nM (Apelin receptor)[1]
体内実験

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]

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.

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.
臨床実験
分子量

523.61

分子式

C25H29N7O4S
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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
10 mM --- --- ---
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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
純度とドキュメンテーション

純度: 99.94%

COA (253 KB) HNMR (268 KB) LCMS (94 KB)

取扱説明書 (2659 KB)
参考文献

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

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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.

Keywords:

Azelaprag2049980-18-7AMG 986AMG986AMG-986Apelin Receptor (APJ)apelin receptor agonistneurological diseasescardiovascular diseasesInhibitorinhibitorinhibit

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製品名:
Azelaprag
製品番号:
HY-109111
数量:
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