GLPBio

COX2-IN-1

Catalog No.: GC32030Purity:>98%
COASDSData Sheet

製品は研究用途にのみ使用できます。人体には使用できません。患者への販売は行っておりません。

COX2-IN-1
Cas No.: 134729-13-8
1mgIn Stock
$191.00
1
5mgIn Stock
$477.00
1
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引用文献 (Citations)

現在、この製品の引用文献はありません。以下はGlpBio製品を引用した代表的な文献です。
  • Nature cover
    Nature
    641, 529–536 (2025)
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    Nature
    628, 630–638 (2024)
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    Nature
    632, 686–694 (2024)
  • Nature cover
    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
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    Science
    387(6739) (2025)
  • Science cover
    Science
    387(6734) (2025)
  • Cell Research cover
    Cell Research
    35, 97–116 (2025)
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    Cell Research
    34, 683–706 (2024)
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    33, 273–287 (2023)
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    Cell Research
    33, 546–561 (2023)
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    Cell Research
    33, 904–922 (2023)
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    Cell Research
    31, 1291–1307 (2021)

製品説明 (Description)

COX2-IN-1 is a selective and inducible COX2 inhibitor with an IC50 of 0.24 μM. COX2-IN-1 is an anti-inflammatory compound with anti-inflammatory and analgesic activities.

COX2-IN-1 shows no COX-1 inhibition even at 100μM[1].

COX2-IN-1 has oral ED50 values of 0.030 and 0.47mg/kg on adjuvant-induced arthritis and collagen-induced arthritis, respectively, and an ED30 value of 7.4mg/kg in the yeast-induced hyperalgesia (Randall-Selitto) assay. COX2-IN-1 shows good analgesic activity and no ulcerogenicity[1].

[1]. Tsuji K, et al. Studies on anti-inflammatory agents. IV. Synthesis and pharmacological properties of 1,5-diarylpyrazoles and related derivatives. Chem Pharm Bull (1997), 45(6), 987-995.

実験プロトコル (Protocol)

Kinase experiment:

hCOX1 or hCOX2 is preincubated with COX2-IN-2 in 0.1 M Tris-HCl buffer containing 2 μM hematin and 5 mM L-tryptophan at 30°C for 5 min, followed by a 5 min incubation with arachidonic acid. The enzyme reaction is stopped by the addition of 1 N HCl. The PGE2 formed is extracted with EtOAc and measured by RIA[1].

Animal experiment:

Rats: Ten male Sprague Dawley rats are used per group. A suspension of 0.5% brewer's yeast in 0.5% methyl cellulose is injected into the right hind paw. The pain threshold us determined 3h after yeast injection. COX-2-IN-2 is given orally 2 h after yeast injection. The pain threshold in the treated rats are compared with that in the control rats[1].

References:

[1]. Tsuji K, et al. Studies on anti-inflammatory agents. IV. Synthesis and pharmacological properties of 1,5-diarylpyrazoles and related derivatives. Chem Pharm Bull (1997), 45(6), 987-995.

化学的性質 (Chemical Properties)

CAS番号
134729-13-8
SMILES
N#CC1=NN(C2=CC=C(F)C=C2)C(C3=CC=C(S(=O)(C)=O)C=C3)=C1
分子式
C17H12FN3O2S
分子量
341.36
溶解性
DMSO : 50 mg/mL (146.47 mM; Need ultrasonic)
保存条件
Store at -20°C
一般的な注意事項
製品の溶解性データに基づいて適切な溶媒を選択してください。調製後は、凍結融解の繰り返しを避けるため、ストック溶液を小分けしてください。
ストック溶液は、-80°Cで保存する場合は6か月以内、-20°Cで保存する場合は1か月以内に使用してください。
溶解性を高めるには、チューブを37°Cに温め、適切な時間超音波処理してください。
配送条件
評価用サンプルは保冷剤とともに発送します。その他の容量は室温で発送し、ご要望に応じて保冷剤を同梱します。

計算ツール (Calculators)モル濃度 / 希釈 / 分子量 / 単位変換 / in vivo製剤 / 溶解度

g/mol

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