2. GPCR/G Protein
  3. Prostaglandin Receptor
  4. AAT-008

AAT-008 is a potent, selective, and orally active prostaglandin EP4 receptor antagonist with Kis of 0.97 and 6.1 nM for recombinant human EP4 and recombinant rat EP4, respectively. AAT-008 exerts tumor growth delay in mice bearing CT26WT colon tumors when combined with radiotherapy. AAT-008 can be used for the study of acute and chronic inflammatory pain and cancer .

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AAT-008

AAT-008 構造式

CAS 番号 : 847727-81-5

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 132 在庫あり
Solution
10 mM * 1 mL in DMSO USD 132 在庫あり
Solid
5 mg $120 在庫あり
10 mg $210 在庫あり
25 mg $450 在庫あり
50 mg $720 在庫あり
100 mg $1150 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Based on 1 publication(s) in Google Scholar

AAT-008 関連抗体

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製品説明

AAT-008 is a potent, selective, and orally active prostaglandin EP4 receptor antagonist with Kis of 0.97 and 6.1 nM for recombinant human EP4 and recombinant rat EP4, respectively. AAT-008 exerts tumor growth delay in mice bearing CT26WT colon tumors when combined with radiotherapy. AAT-008 can be used for the study of acute and chronic inflammatory pain and cancer [1][2].

IC50 & Target[1]

EP4

0.97 nM (Ki)

EP4

6.1 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
16.3 nM
Compound: 4j; AAT-008
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
Antagonist activity at human EP4 receptor expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP level by HTS assay
[PMID: 28169162]
HEK293 IC50
2.4 nM
Compound: 4j; AAT-008
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
Displacement of [3H]PGE from human EP4 receptor expressed in HEK293 cell membranes
[PMID: 28169162]
Parmacokinetics
Species Dose Route T1/2 AUC0-inf CLtotal Vdss F Cmax Tmax
Dog[1] 1 mg/kg i.v. 8.43 h 7490 ng·h/mL 2.30 mL/min/kg 1.21 L/kg / / /
Dog[1] 1 mg/kg p.o. 7.95 h 6080 ng·h/mL / / 80.6 % 1450 ng/mL 0.438 h
Monkey[1] 1 mg/kg i.v. 14.5 h 3390 ng·h/mL 5.31 mL/min/kg 4.70 L/kg / / /
Monkey[1] 1 mg/kg p.o. 21.9 h 2460 ng·h/mL / / 73.3 % 76.0 ng/mL 8 h
Rat[1] 1 mg/kg i.v. 4.59 h 9620 ng·h/mL 1.75 mL/min/kg 0.593 L/kg / / /
Rat[1] 1 mg/kg p.o. 3.71 h 7090 ng·h/mL / / 73.6 % 994 ng/mL 0.750 h
体内実験

AAT-008 (1 mg/kg, p.o., once) significantly reduces Carrageenan (HY-125474) and Complete Freund’s adjuvant (CFA) (HY-153808B)-induced mechanical hyperalgesia in rats[1].
AAT-008 (3-30 mg/kg, p.o., once or twice daily, up to 18 days) exerts tumor growth delay in Balb/c mice bearing CT26WT colon tumors alone or combined with radiotherapy[2].

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

Animal Model: CT26WT cells (5 × 105) were subcutaneously injected into the right hind legs of 7-week-old female Balb/c mice[2]
Dosage: 3, 10, 30 mg/kg
Administration: p.o., once or twice daily, up to 18 days
Result: Showed minimal tumor growth delay alone.
Prolonged tumor doubling time when combined with radiotherapy (9 Gy on day 3).
Increased the mean proportion of intratumoral Teff (CD45+CD8+CD69+).
分子量

414.81

分子式

C21H16ClFN2O4
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C1=CC=C([C@@H](NC(C2=CC(Cl)=CN=C2OC3=CC=CC(F)=C3)=O)C)C=C1
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 : 100 mg/mL (241.07 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 2.4107 mL 12.0537 mL 24.1074 mL
5 mM 0.4821 mL 2.4107 mL 4.8215 mL
10 mM 0.2411 mL 1.2054 mL 2.4107 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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  • 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

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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 2.4107 mL 12.0537 mL 24.1074 mL 60.2686 mL
5 mM 0.4821 mL 2.4107 mL 4.8215 mL 12.0537 mL
10 mM 0.2411 mL 1.2054 mL 2.4107 mL 6.0269 mL
15 mM 0.1607 mL 0.8036 mL 1.6072 mL 4.0179 mL
20 mM 0.1205 mL 0.6027 mL 1.2054 mL 3.0134 mL
25 mM 0.0964 mL 0.4821 mL 0.9643 mL 2.4107 mL
30 mM 0.0804 mL 0.4018 mL 0.8036 mL 2.0090 mL
40 mM 0.0603 mL 0.3013 mL 0.6027 mL 1.5067 mL
50 mM 0.0482 mL 0.2411 mL 0.4821 mL 1.2054 mL
60 mM 0.0402 mL 0.2009 mL 0.4018 mL 1.0045 mL
80 mM 0.0301 mL 0.1507 mL 0.3013 mL 0.7534 mL
100 mM 0.0241 mL 0.1205 mL 0.2411 mL 0.6027 mL
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AAT-008 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:

AAT-008847727-81-5AAT008AAT 008Prostaglandin ReceptororalprostaglandinEP4 receptorinflammationInhibitorinhibitorinhibit

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製品名:
AAT-008
製品番号:
HY-122168
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