2. GPCR/G Protein Immunology/Inflammation
  3. CXCR
  4. NVP CXCR2 20

NVP CXCR2 20 是一种具有镇痛和抗伤害感受活性的选择性 CXCR2 抑制剂。NVP CXCR2 20 可选择性阻断 CXCR2 信号通路，并减轻大鼠慢性缩窄损伤 (CCI) 模型中的机械性和热痛觉过敏。NVP CXCR2 20 可抑制正常小鼠中 CXCL3 诱导的痛觉过敏，并降低 CCI 模型大鼠脊髓和背根神经节 (DRG) 中升高的 CXCL3 蛋白水平。NVP CXCR2 20 可用于神经病理性疼痛和慢性阻塞性肺疾病 (COPD) 的研究。

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NVP CXCR2 20

NVP CXCR2 20 Chemical Structure

CAS No. : 1029521-30-9

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NVP CXCR2 20 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NVP CXCR2 20 is a selective CXCR2 inhibitor with analgesic and antinociceptive activities. NVP CXCR2 20 selectively blocks CXCR2 signaling and attenuates mechanical and thermal hypersensitivity in rat chronic constriction injury (CCI) models. NVP CXCR2 20 inhibits CXCL3-induced hypersensitivity in naive mice and reduces elevated CXCL3 protein levels in the spinal cord and dorsal root ganglia (DRG) of CCI-exposed rats. NVP CXCR2 20 can be used for the research of neuropathic pain and chronic obstructive pulmonary disease (COPD)[1][2][3].

IC50 & Target[1]

CXCR2

4.9 μM (IC50)

体外研究
(In Vitro)

NVP CXCR2 20 (100 nM; 30 min pre-incubation, 24 h with LPS) 可降低原代大鼠小胶质细胞培养物和星形胶质细胞培养物中 LPS 诱导的 CXCL1、CXCL2 和 CXCL3 蛋白表达[1]。
NVP CXCR2 20 (0.0005-10 μM) 可结合 CHO 细胞膜上的人重组 CXCR2，IC50 为 0.04 μM；其[35S]-GTPγS IC50 为 0.14 μM；该化合物的 cLogP 为 3.9，功能性配体亲脂性效率 (LLE) 为 3.0[3]。
NVP CXCR2 20 (10 μM) 对 CXCR2 具有选择性，针对其他 49 种 GPCR 组成的筛选组无显著抑制活性 (IC50 > 10 μM)[3]。

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

NVP CXCR2 20 相关抗体:
体内研究
(In Vivo)

NVP CXCR2 20 (10-30 μg/5 μL；鞘内给药；单次给药，或在 CCI 后 16 h 和 1 h 给药，之后每日 1 次连续 7 天) 可剂量依赖性地减轻 CCI 诱导的大鼠神经性疼痛中的机械性和热痛觉过敏；重复给予 10 μg/5 μL 剂量可在 CCI 后第 2 天和第 7 天减轻痛觉过敏，并使脊髓和 DRG 中的 CXCL3 蛋白水平恢复正常，且不影响胶质细胞活化[1]。
NVP CXCR2 20 (10 μg/5 μL；鞘内注射；CCI 术后第 7 天单次给药，阿片类药物联合给药前 4 小时) 可在神经病理性疼痛大鼠中产生镇痛作用[1]。
NVP CXCR2 20 (60 μg/5 μL；鞘内给药；单剂量，于鞘内给予 CXCL3 前 2 小时) 可预防 CXCL3 诱导的未致敏小鼠机械性及热痛觉过敏[1]。

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

Animal Model: Wistar rats (male, adult, 250-300 g, chronic constriction injury of the sciatic nerve with intrathecal catheter implantation 7 days prior)[1]
Dosage: 10 μg/5 μL (repeated administration); 20 μg/5 μL (single administration); 30 μg/5 μL (single administration)
Administration: intrathecal; single dose (single treatment); 16 h and 1 h post-CCI, then once daily for 7 days (repeated treatment)
Result: Produced significant analgesic effects on mechanical and thermal hypersensitivity at 2, 4, and 6 h after single administration (20 and 30 μg/5 μL).
Reduced mechanical hypersensitivity and thermal hypersensitivity after repeated dosing (10 μg/5 μL).
Normalized elevated CXCL3 protein in spinal cord and DRG to naive levels.
Did not affect CCI-induced spinal IBA1 (microglia) or GFAP (astroglia) upregulation.
Animal Model: Wistar rats (male, adult, 250-300 g, chronic constriction injury of the sciatic nerve with intrathecal catheter implantation 7 days prior)[1]
Dosage: 10 μg/5 μL
Administration: intrathecal; single dose (day 7 post-CCI, 4 hours prior to opioid co-administration)
Result: Produced analgesic effects similar to single doses of morphine or buprenorphine in the von Frey and cold plate tests.
Animal Model: Albino Swiss mice (20-22 g)[1]
Dosage: 60 μg/5 μL
Administration: intrathecal; single dose, 2 hours prior to intrathecal CXCL3
Result: Completely prevented the mechanical and thermal hypersensitivity induced by CXCL3 in naive mice at all tested time points (1.5, 5, and 24 hours post-CXCL3 administration).
分子量

319.33

Formula

C15H11F2N3OS
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

NVP CXCR2 20 相关分类

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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:

NVP CXCR2 201029521-30-9CXCRCXC chemokine receptorsC-X-C motif chemokine receptorsspinal cordCXCR2primary rat astroglial cell culturesnaive micedorsal root gangliaCXCL3chronic obstructive pulmonary diseaseprimary rat microglial cell culturesrat chronic constriction injury modelsneuropathic painInhibitorinhibitorinhibit

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