1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. AMG-009

AMG-009 is a potent antagonist of prostaglandin D2, with IC50 of 3 nM and 12 nM for CRTH2 and DP receptors, respectively.

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AMG-009

AMG-009 構造式

CAS 番号 : 1027847-67-1

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 192 在庫あり
Solution
10 mM * 1 mL in DMSO USD 192 在庫あり
Solid
5 mg $150 在庫あり
10 mg $240 在庫あり
25 mg $470 在庫あり
50 mg $750 在庫あり
100 mg $1100 在庫あり
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500 mg   お問い合わせ  

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製品説明

AMG-009 is a potent antagonist of prostaglandin D2, with IC50 of 3 nM and 12 nM for CRTH2 and DP receptors, respectively.

IC50 & Target[3]

DP

12 nM (IC50)

CRTH2

3 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
3 1
Compound: 31, AMG-009
Displacement of [3H]-PGD2 from guinea pig CRTH2 receptor expressed in HEK293 cells
Displacement of [3H]-PGD2 from guinea pig CRTH2 receptor expressed in HEK293 cells
[PMID: 19804971]
HEK293 IC50
0.003 3
Compound: 1, AMG-009
Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin
Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin
[PMID: 24900313]
HEK293 IC50
0.003 3
Compound: AMG-009
Displacement of [3H]PGD2 from human CRTH2 receptor expressed in 293 cells by scintillation counting in presence of 0.5 % BSA
Displacement of [3H]PGD2 from human CRTH2 receptor expressed in 293 cells by scintillation counting in presence of 0.5 % BSA
[PMID: 22119474]
HEK293 IC50
0.003 3
Compound: 31, AMG-009
Displacement of [3H]-PGD2 from human CRTH2 expressed in HEK 293 cells in presence of 0.5% BSA by scintillation counting
Displacement of [3H]-PGD2 from human CRTH2 expressed in HEK 293 cells in presence of 0.5% BSA by scintillation counting
[PMID: 19804971]
HEK293 IC50
3 1
Compound: AMG 009
Displacement of [3H]-PGD2 from human CRTH2 expressed in HEK293 cells in buffer solution with 0.5% bovine serum albumin by scintillation counting
Displacement of [3H]-PGD2 from human CRTH2 expressed in HEK293 cells in buffer solution with 0.5% bovine serum albumin by scintillation counting
[PMID: 24825301]
HEK293 IC50
0.003 3
Compound: 31, AMG-009
Displacement of [3H]-PGD2 from human CRTH2 expressed in HEK 293 cells in presence of 0.5% BSA by scintillation counting
Displacement of [3H]-PGD2 from human CRTH2 expressed in HEK 293 cells in presence of 0.5% BSA by scintillation counting
[PMID: 19804971]
HEK293 IC50
0.003 3
Compound: 31, AMG-009
Displacement of [3H]-PGD2 from human CRTH2 expressed in HEK 293 cells in presence of 0.5% BSA by scintillation counting
Displacement of [3H]-PGD2 from human CRTH2 expressed in HEK 293 cells in presence of 0.5% BSA by scintillation counting
[PMID: 19804971]
HEK293 IC50
0.003 3
Compound: 1, AMG-009
Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin
Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin
[PMID: 24900313]
HEK293 IC50
0.003 3
Compound: AMG-009
Displacement of [3H]PGD2 from human CRTH2 receptor expressed in 293 cells by scintillation counting in presence of 0.5 % BSA
Displacement of [3H]PGD2 from human CRTH2 receptor expressed in 293 cells by scintillation counting in presence of 0.5 % BSA
[PMID: 22119474]
HEK293 IC50
0.003 3
Compound: AMG-009
Displacement of [3H]PGD2 from human CRTH2 receptor expressed in 293 cells by scintillation counting in presence of 0.5 % BSA
Displacement of [3H]PGD2 from human CRTH2 receptor expressed in 293 cells by scintillation counting in presence of 0.5 % BSA
[PMID: 22119474]
HEK293 IC50
0.012 3
Compound: 1, AMG-009
Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin
Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin
[PMID: 24900313]
HEK293 IC50
0.012 3
Compound: AMG-009
Displacement of [3H]PGD2 from human DP receptor expressed in 293 cells by scintillation counting in presence of 0.5 % BSA
Displacement of [3H]PGD2 from human DP receptor expressed in 293 cells by scintillation counting in presence of 0.5 % BSA
[PMID: 22119474]
HEK293 IC50
0.021 3
Compound: AMG-009
Displacement of [3H]PGD2 from human CRTh2 receptor expressed in 293 cells by scintillation counting in presence of 50 % human plasma
Displacement of [3H]PGD2 from human CRTh2 receptor expressed in 293 cells by scintillation counting in presence of 50 % human plasma
[PMID: 22119474]
HEK293 IC50
0.012 3
Compound: 31, AMG-009
Displacement of [3H]-PGD2 from human DP receptor expressed in HEK 293 cells in presence of 0.5% BSA by scintillation counting
Displacement of [3H]-PGD2 from human DP receptor expressed in HEK 293 cells in presence of 0.5% BSA by scintillation counting
[PMID: 19804971]
HEK293 IC50
0.012 3
Compound: 31, AMG-009
Displacement of [3H]-PGD2 from human DP receptor expressed in HEK 293 cells in presence of 0.5% BSA by scintillation counting
Displacement of [3H]-PGD2 from human DP receptor expressed in HEK 293 cells in presence of 0.5% BSA by scintillation counting
[PMID: 19804971]
HEK293 IC50
0.021 3
Compound: AMG-009
Displacement of [3H]PGD2 from human CRTH2 receptor expressed in HEK293 cells by scintillation counting in presence of 50% plasma
Displacement of [3H]PGD2 from human CRTH2 receptor expressed in HEK293 cells by scintillation counting in presence of 50% plasma
[PMID: 22264478]
HEK293 IC50
0.012 3
Compound: 1, AMG-009
Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin
Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin
[PMID: 24900313]
HEK293 IC50
0.012 3
Compound: AMG-009
Displacement of [3H]PGD2 from human DP receptor expressed in 293 cells by scintillation counting in presence of 0.5 % BSA
Displacement of [3H]PGD2 from human DP receptor expressed in 293 cells by scintillation counting in presence of 0.5 % BSA
[PMID: 22119474]
HEK293 IC50
0.021 3
Compound: AMG-009
Displacement of [3H]PGD2 from human CRTH2 receptor expressed in HEK293 cells by scintillation counting in presence of 50% plasma
Displacement of [3H]PGD2 from human CRTH2 receptor expressed in HEK293 cells by scintillation counting in presence of 50% plasma
[PMID: 22264478]
HEK293 IC50
0.003 3
Compound: 1, AMG-009
Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin
Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin
[PMID: 24900313]
HEK293 IC50
0.021 3
Compound: 1, AMG-009
Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma
Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma
[PMID: 24900313]
HEK293 IC50
0.021 3
Compound: 1, AMG-009
Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma
Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma
[PMID: 24900313]
HEK293 IC50
0.021 3
Compound: AMG-009
Displacement of [3H]PGD2 from human CRTh2 receptor expressed in 293 cells by scintillation counting in presence of 50 % human plasma
Displacement of [3H]PGD2 from human CRTh2 receptor expressed in 293 cells by scintillation counting in presence of 50 % human plasma
[PMID: 22119474]
HEK293 IC50
0.021 3
Compound: AMG-009
Displacement of [3H]PGD2 from human CRTh2 receptor expressed in 293 cells by scintillation counting in presence of 50 % human plasma
Displacement of [3H]PGD2 from human CRTh2 receptor expressed in 293 cells by scintillation counting in presence of 50 % human plasma
[PMID: 22119474]
HEK293 IC50
0.012 3
Compound: AMG-009
Displacement of [3H]PGD2 from human DP receptor expressed in 293 cells by scintillation counting in presence of 0.5 % BSA
Displacement of [3H]PGD2 from human DP receptor expressed in 293 cells by scintillation counting in presence of 0.5 % BSA
[PMID: 22119474]
HEK293 IC50
0.021 3
Compound: AMG-009
Displacement of [3H]PGD2 from human CRTH2 receptor expressed in HEK293 cells by scintillation counting in presence of 50% plasma
Displacement of [3H]PGD2 from human CRTH2 receptor expressed in HEK293 cells by scintillation counting in presence of 50% plasma
[PMID: 22264478]
HEK293 IC50
0.021 3
Compound: 1, AMG-009
Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma
Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma
[PMID: 24900313]
HEK293 IC50
0.28 3
Compound: AMG-009
Displacement of [3H]PGD2 from human DP receptor expressed in HEK293 cells by scintillation counting in presence of 50% plasma
Displacement of [3H]PGD2 from human DP receptor expressed in HEK293 cells by scintillation counting in presence of 50% plasma
[PMID: 22264478]
HEK293 IC50
0.28 3
Compound: AMG-009
Displacement of [3H]PGD2 from human DP receptor expressed in 293 cells by scintillation counting in presence of 50 % human plasma
Displacement of [3H]PGD2 from human DP receptor expressed in 293 cells by scintillation counting in presence of 50 % human plasma
[PMID: 22119474]
HEK293 IC50
0.28 3
Compound: 1, AMG-009
Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma
Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma
[PMID: 24900313]
HEK293 IC50
0.012 3
Compound: 31, AMG-009
Displacement of [3H]-PGD2 from human DP receptor expressed in HEK 293 cells in presence of 0.5% BSA by scintillation counting
Displacement of [3H]-PGD2 from human DP receptor expressed in HEK 293 cells in presence of 0.5% BSA by scintillation counting
[PMID: 19804971]
HEK293 IC50
0.28 3
Compound: AMG-009
Displacement of [3H]PGD2 from human DP receptor expressed in 293 cells by scintillation counting in presence of 50 % human plasma
Displacement of [3H]PGD2 from human DP receptor expressed in 293 cells by scintillation counting in presence of 50 % human plasma
[PMID: 22119474]
HEK293 IC50
0.28 3
Compound: AMG-009
Displacement of [3H]PGD2 from human DP receptor expressed in 293 cells by scintillation counting in presence of 50 % human plasma
Displacement of [3H]PGD2 from human DP receptor expressed in 293 cells by scintillation counting in presence of 50 % human plasma
[PMID: 22119474]
HEK293 IC50
0.28 3
Compound: AMG-009
Displacement of [3H]PGD2 from human DP receptor expressed in HEK293 cells by scintillation counting in presence of 50% plasma
Displacement of [3H]PGD2 from human DP receptor expressed in HEK293 cells by scintillation counting in presence of 50% plasma
[PMID: 22264478]
HEK293 IC50
0.28 3
Compound: 1, AMG-009
Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma
Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma
[PMID: 24900313]
HEK293 IC50
0.28 3
Compound: AMG-009
Displacement of [3H]PGD2 from human DP receptor expressed in HEK293 cells by scintillation counting in presence of 50% plasma
Displacement of [3H]PGD2 from human DP receptor expressed in HEK293 cells by scintillation counting in presence of 50% plasma
[PMID: 22264478]
HEK293 IC50
0.012 3
Compound: 1, AMG-009
Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin
Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin
[PMID: 24900313]
HEK293 IC50
12 1
Compound: AMG 009
Displacement of [3H]-PGD2 from human DP receptor expressed in HEK293 cells in buffer solution with 0.5% bovine serum albumin by scintillation counting
Displacement of [3H]-PGD2 from human DP receptor expressed in HEK293 cells in buffer solution with 0.5% bovine serum albumin by scintillation counting
[PMID: 24825301]
HEK293 IC50
12 1
Compound: AMG 009
Displacement of [3H]-PGD2 from human DP receptor expressed in HEK293 cells in buffer solution with 0.5% bovine serum albumin by scintillation counting
Displacement of [3H]-PGD2 from human DP receptor expressed in HEK293 cells in buffer solution with 0.5% bovine serum albumin by scintillation counting
[PMID: 24825301]
HEK293 IC50
0.28 3
Compound: 1, AMG-009
Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma
Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma
[PMID: 24900313]
HEK293 IC50
3 1
Compound: AMG 009
Displacement of [3H]-PGD2 from human CRTH2 expressed in HEK293 cells in buffer solution with 0.5% bovine serum albumin by scintillation counting
Displacement of [3H]-PGD2 from human CRTH2 expressed in HEK293 cells in buffer solution with 0.5% bovine serum albumin by scintillation counting
[PMID: 24825301]
HEK293 IC50
3 1
Compound: 31, AMG-009
Displacement of [3H]-PGD2 from guinea pig CRTH2 receptor expressed in HEK293 cells
Displacement of [3H]-PGD2 from guinea pig CRTH2 receptor expressed in HEK293 cells
[PMID: 19804971]
HEK293 IC50
12 1
Compound: AMG 009
Displacement of [3H]-PGD2 from human DP receptor expressed in HEK293 cells in buffer solution with 0.5% bovine serum albumin by scintillation counting
Displacement of [3H]-PGD2 from human DP receptor expressed in HEK293 cells in buffer solution with 0.5% bovine serum albumin by scintillation counting
[PMID: 24825301]
HEK293 IC50
3 1
Compound: AMG 009
Displacement of [3H]-PGD2 from human CRTH2 expressed in HEK293 cells in buffer solution with 0.5% bovine serum albumin by scintillation counting
Displacement of [3H]-PGD2 from human CRTH2 expressed in HEK293 cells in buffer solution with 0.5% bovine serum albumin by scintillation counting
[PMID: 24825301]
HEK293-EBNA IC50
30 3
Compound: 31, AMG-009
Displacement of [3H]SQ29548 from human TP receptor transfected in HEK 293 EBNA cells
Displacement of [3H]SQ29548 from human TP receptor transfected in HEK 293 EBNA cells
[PMID: 19804971]
HEK293-EBNA IC50
30 3
Compound: 31, AMG-009
Displacement of [3H]SQ29548 from human TP receptor transfected in HEK 293 EBNA cells
Displacement of [3H]SQ29548 from human TP receptor transfected in HEK 293 EBNA cells
[PMID: 19804971]
体外実験

AMG-009 inhibits PGD2-induced down-modulation of CRTH2 on CD16 negative granulocytes (eosinophils) in human whole blood with a Ki of 1 nM. AMG 009 also inhibits PGD2-induced cAMP response mediated by DP in platelets in 80% human whole blood with a Ki of 148 nM. AMG 009 inhibits guinea pig CRTH2 receptors (IC50=3 nM) and a PGD2-induced cAMP response assay with cells expressing the guinea pig DP receptors (Ki=131 nM)[1].

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

体内実験

AMG 009 (3, 10 or 30 mg/kg, s.c.) results in a dose dependent decrease in airway resistance provoked by PGD2 aerosol in an acute guinea pig model[1]. In a guinea pig model of PGD2-induced airway constriction, AMG 009 significantly improves DP potency, with Kb of 82 nM[2].

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

分子量

581.46

分子式

C26H26Cl2N2O7S

CAS 番号
Appearance

Solid

Color

White to light brown

SMILES

O=C(O)CC1=CC=C(OC2=CC=C(C(NCCCC)=O)C=C2NS(=O)(C3=CC=C(Cl)C=C3Cl)=O)C(OC)=C1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 125 mg/mL (214.98 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 1.7198 mL 8.5990 mL 17.1981 mL
5 mM 0.3440 mL 1.7198 mL 3.4396 mL
10 mM 0.1720 mL 0.8599 mL 1.7198 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.

  • Molarity Calculator

  • Dilution Calculator

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

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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

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体積 (開始)

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濃度 (終了)

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In Vivo Dissolution Calculator
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純度とドキュメンテーション
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 1.7198 mL 8.5990 mL 17.1981 mL 42.9952 mL
5 mM 0.3440 mL 1.7198 mL 3.4396 mL 8.5990 mL
10 mM 0.1720 mL 0.8599 mL 1.7198 mL 4.2995 mL
15 mM 0.1147 mL 0.5733 mL 1.1465 mL 2.8663 mL
20 mM 0.0860 mL 0.4300 mL 0.8599 mL 2.1498 mL
25 mM 0.0688 mL 0.3440 mL 0.6879 mL 1.7198 mL
30 mM 0.0573 mL 0.2866 mL 0.5733 mL 1.4332 mL
40 mM 0.0430 mL 0.2150 mL 0.4300 mL 1.0749 mL
50 mM 0.0344 mL 0.1720 mL 0.3440 mL 0.8599 mL
60 mM 0.0287 mL 0.1433 mL 0.2866 mL 0.7166 mL
80 mM 0.0215 mL 0.1075 mL 0.2150 mL 0.5374 mL
100 mM 0.0172 mL 0.0860 mL 0.1720 mL 0.4300 mL
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  • 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 *
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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
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製品名:
AMG-009
製品番号:
HY-19499
数量:
MCE 日本正規代理店: