COX2-IN-1

目录号: GC32030纯度: >98%

COX2-IN-1是选择性的，诱导型的COX2抑制剂，IC50值为0.24μM。COX2-IN-1是具有抗炎和止痛活性的抗炎物。

Cas No.: 134729-13-8

规格	价格	库存	数量	操作
1mg	¥1,908.00	现货	1
5mg	¥4,770.00	现货	1

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610, 366–372 (2022)
Cell
187(9):2288-2304 (2024)
Cell
183(7):1867-1883 (2020)
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388(6745) (2025)
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387(6739) (2025)
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产品描述 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.

实验参考方法 Experimental Reference Method

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.

产品文档 Product Documents

Purity:>98%

COA SDS Data Sheet

化学性质Chemical Properties

CAS 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 g/mol

溶解性

DMSO : 50 mg/mL (146.47 mM; Need ultrasonic)

保存条件

Store at -20°C

General tips

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。

Shipping Condition

评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

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