2. Immunology/Inflammation Metabolic Enzyme/Protease
  3. COX Carbonic Anhydrase LOX-1
  4. COX-2-IN-30

COX-2-IN-30 是一种苯磺酰胺衍生物，也是一种具有口服活性的 COX/5-LOX 双重抑制剂，IC50 分别为 49 nM (COX)，10.4 μM (5-LOX)。COX-2-IN-30 还抑制跨膜 hCA IX 和 hCA XII 亚型，具有纳摩尔级 Ki 值。COX-2-IN-30 具有镇痛、抗炎和致溃疡活性，并且不显示急性胃效应。

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COX-2-IN-30 Chemical Structure

COX-2-IN-30 Chemical Structure

CAS No. : 1160498-08-7

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规格 是否有货
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COX-2-IN-30 相关抗体

Top Publications Citing Use of Products

查看 COX 亚型特异性产品:

查看所有亚型
COX COX-1 COX-2 COX-3

查看 Carbonic Anhydrase 亚型特异性产品:

查看所有亚型
CA CA I CA Ⅱ CA Ⅸ CA XII

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

COX-2-IN-30 is a benzenesulfonamide derivative, as well as an orally active and dual inhibitor of COX (IC50=49 nM for COX-2, 10.4 μM for COX-1) and 5-LOX (IC50=2.4 μM). COX-2-IN-30 also inhibits transmembrane hCA IX and hCA XII isoform with nanomolar calss Ki values. COX-2-IN-30 exhibits analgesic, anti-inflammatory, and ulcerogenic activities, and does not show acute gastric effect[1].

IC50 & Target[1]

COX-2

49 nM (IC50)

COX-1

10.4 μM (IC50)

hCA I

183.4 nM (Ki)

hCA II

81.4 nM (Ki)

hCA IX

38.4 nM (Ki)

hCA XII

21.6 nM (Ki)

5-LOX

2.4 μM (IC50)

体外研究
(In Vitro)

COX-2-IN-30 (化合物 7a) 与 hCA 亚型结合，Ki 值分别为 183.4 nM (hCA I)、81.4 nM (hCA II)、38.4 nM (hCA IX)、21.6 nM (hCA XII)[1]。

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

COX-2-IN-30 相关抗体:
体内研究
(In Vivo)

COX-2-IN-30 (化合物 7a) (10 mg/kg；口服；单剂量) 表现出镇痛活性，同时显着减少小鼠的扭动次数[1]。
COX-2-IN-30 (10 mg/kg；口服；单次剂量) 在 Carrageenan (HY-125474) 诱导的大鼠爪水肿试验中导致爪高度显着降低。 COX-2-IN-30 显着降低 TNF-α 和 IL-1β 的水平[1]。
COX-2-IN-30 (10 mg/kg；口服；单剂量) 在雄性白化病大鼠的胃组织中表现出安全性[1]。

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

Animal Model: Albino mice (25-30 g)[1]
Dosage: 10 mg/kg
Administration: PO; single dose; after one hour, 0.1 mL of 1 percent acetic acid in a volume of 0.1 mL/10 g body weight was used to produce writhing.
Result: Decreased the number of writhing responses of mouse conpared with control group.
Animal Model: Paw edema rat induced by Carrageenan (HY-125474)[1]
Dosage: 10 mg/kg
Administration: PO; single dose; after one hour, 0.1 mL of 1% carrageenan solution was injected in the left hind paw; measure inflammation height at 0, 1, 2, and 3 h
Result: Showed a significant reduction of paw height compared to control after 3 h.
分子量

384.41

Formula

C17H16N6O3S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

COX-2-IN-30 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

COX-2-IN-301160498-08-7COXCarbonic AnhydraseLOX-1CyclooxygenaseCarbonate dehydrataseLectin-like oxidized low-density lipoprotein receptor-1analgesicanti-inflammatoryulcerogenicacute gastric effectInhibitorinhibitorinhibit

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产品名称：
COX-2-IN-30
目录号：
HY-149269
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