2. Immunology/Inflammation Neuronal Signaling Membrane Transporter/Ion Channel Apoptosis
  3. COX Calcium Channel Interleukin Related TNF Receptor
  4. COX-2/CaV2.2-IN-1

COX-2/CaV2.2-IN-1 是一种具有口服活性的选择性双靶点 COX-2/CaV2.2 抑制剂，其对 COX-2 的 IC50 为 0.26 μM，对 CaV2.2 的 IC50 为 0.29 μM。COX-2/CaV2.2-IN-1 可抑制炎症反应及炎症介质 (IL-6、TNF-α、NO) 的产生。COX-2/CaV2.2-IN-1 在炎症性疼痛、神经性疼痛和内脏疼痛等多种模型中均表现出显著的镇痛效果。COX-2/CaV2.2-IN-1 可用于慢性疼痛相关研究。

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COX-2/CaV2.2-IN-1

COX-2/CaV2.2-IN-1 Chemical Structure

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COX-2/CaV2.2-IN-1 相关抗体

Top Publications Citing Use of Products

查看 COX 亚型特异性产品:

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COX COX-1 COX-2 COX-3

查看 Calcium Channel 亚型特异性产品:

查看所有亚型
N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

查看 Interleukin Related 亚型特异性产品:

查看所有亚型
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

查看 TNF Receptor 亚型特异性产品:

查看所有亚型
TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

COX-2/CaV2.2-IN-1 is an orally active and selective dual COX-2/CaV2.2 inhibitor, exhibiting a COX-2 IC50 of 0.26 μM and a CaV2.2 IC50 of 0.29 μM. COX-2/CaV2.2-IN-1 suppresses inflammatory responses and inflammatory mediator (IL-6, TNF-α, NO) production. COX-2/CaV2.2-IN-1 produces pronounced analgesic effects in diverse models of inflammatory, neuropathic, and visceral pain. COX-2/CaV2.2-IN-1 can be used for the research of chronic pain[1].

IC50 & Target[1]

COX-2

0.26 μM (IC50)

CaV2.2

0.29 μM (IC50)

IL-6

 

体外研究
(In Vitro)

COX-2/CaV2.2-IN-1 (Compound 5d) 可强效且选择性地抑制重组人源 COX-2，其 IC50 为 257.4 ± 166.0 nM[1]。
COX-2/CaV2.2-IN-1 可在转染的 HEK293T 细胞中强效且选择性地抑制人源 CaV2.2 通道，其 IC50 为 288.7 ± 75.5 nM[1]。
COX-2/CaV2.2-IN-1 (10-50 μM; 24 h) 可剂量依赖性地抑制小鼠 BV2 小胶质细胞中 LPS (HY-D1056) 诱导的炎症介质 (IL-6、TNF-α、NO) 产生[1]。

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

COX-2/CaV2.2-IN-1 相关抗体:

ELISA Assay[1]

Cell Line: Mouse BV2 microglial cells
Concentration: 10, 50 μM
Incubation Time: 24 h
Result: Dose-dependently suppressed LPS-induced IL-6, TNF-α, and NO production at 10 μM and 50 μM.
Exhibited a stronger anti-inflammatory effect than Rofecoxib (HY-17372) at 10 μM, as evidenced by superior suppression of IL-6, TNF-α, and NO levels.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Tmax Cmax AUC0-∞ F
Mice[1] 20 mg/kg i.g. 6.08 ± 0.58 h 1.17 ± 0.44 h 1713 ± 129 ng/mL 16134 ± 2934 ng·h/mL 42.38 ± 7.71 %
Mice[1] 5 mg/kg i.v. 7.62 ± 0.57 h 0.03 ± 0 h 5433 ± 500 ng/mL 9601 ± 265 ng·h/mL /
体内研究
(In Vivo)

COX-2/CaV2.2-IN-1 (Compound 5d) (30-120 μmol/kg；灌胃；单剂量) 可在小鼠 CFA (HY-153808) 诱导的炎性疼痛模型中产生剂量依赖性的镇痛作用，其 ED50 为 41.3 μmol/kg[1]。
COX-2/CaV2.2-IN-1 (62.0 μmol/kg；灌胃；单剂量) 可在小鼠福尔马林试验中减轻炎症疼痛相关的舔爪行为[1]。
COX-2/CaV2.2-IN-1 (62.0 μmol/kg；灌胃；单剂量) 可减少小鼠内脏痛相关的扭体行为[1]。
COX-2/CaV2.2-IN-1 (62.0 μmol/kg；灌胃；单剂量) 可减轻小鼠 CCI 模型中的神经病理性疼痛[1]。
COX-2/CaV2.2-IN-1 (62.0 μmol/kg；灌胃；单剂量) 可减轻小鼠 PTX (HY-B0715) 诱导的神经病理性疼痛模型的冷异常性疼痛[1]。

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

Animal Model: C57BL/6 (6−8 weeks old; inflammatory pain model via intraplantar CFA injection)[1]
Dosage: 30, 60,120 μmol/kg
Administration: I.g.; single dose
Result: Produced dose-dependent antinociceptive effects, with a median effective dose (ED50) of 41.3 μmol/kg.
Exhibited a favorable peak analgesic efficacy at 62.0 μmol/kg, with an area under the curve (AUC) of 1320.0 ± 73.2, which was significantly greater than the Rofecoxib (HY-17372) group.
Animal Model: C57BL/6 (6−8 weeks old; neuropathic pain model via intraperitoneal PTX injection)[1]
Dosage: 62.0 μmol/kg
Administration: I.g.; single dose
Result: Conferred pronounced antinociceptive effects, with a significantly increased PWT compared to the vehicle group, and an AUC significantly higher than the Rofecoxib group.
分子量

486.51

Formula

C25H21F3N2O3S
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/CaV2.2-IN-1 相关分类

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  • 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/CaV2.2-IN-1COXCalcium ChannelInterleukin RelatedTNF ReceptorCyclooxygenaseCa2+ channelsCa channelsILTumor Necrosis Factor ReceptorTNFRCaV2.2COX-1visceral paininflammatory painCOX-2CaV3.2HEK293T cellsmouse BV2 microglial cellsCaV1.2neuropathic painInhibitorinhibitorinhibit

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