2. Immunology/Inflammation Membrane Transporter/Ion Channel
  3. NOD-like Receptor (NLR) URAT1 Interleukin Related OAT GLUT
  4. NLRP3/URAT1-IN-1

NLRP3/URAT1-IN-1 是一种具有口服活性的 NLRP3 和 URAT1 双重抑制剂 (IC50 = 3.81 μM)。NLRP3/URAT1-IN-1 抑制 LPS (HY-D1056) 和 ATP 刺激的小鼠骨髓源性巨噬细胞 (BMDMs) 中 IL-1β 的释放，IC50 值为 2.61 μM。NLRP3/URAT1-IN-1 降低急性高尿酸血症 (HUA) 小鼠的血清尿酸 (SUA) 水平，并缓解肝/肾损伤。NLRP3/URAT1-IN-1 可用于痛风和高尿酸血症的研究。

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NLRP3/URAT1-IN-1

NLRP3/URAT1-IN-1 Chemical Structure

CAS No. : 2994637-53-3

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NLRP3/URAT1-IN-1 相关抗体

Top Publications Citing Use of Products

查看 NOD-like Receptor (NLR) 亚型特异性产品:

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NLRP3 NLRP1 NOD1 NOD2

查看 Interleukin Related 亚型特异性产品:

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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

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GLUT1 GLUT2 GLUT3 GLUT4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NLRP3/URAT1-IN-1 is an orally active double inhibitor of NLRP3 and URAT1 (IC50 = 3.81 μM). NLRP3/URAT1-IN-1 inhibits IL-1β release in LPS (HY-D1056) and ATP-stimulated mouse bone marrow-derived macrophages (BMDMs), with an IC50 of 2.61 μM. NLRP3/URAT1-IN-1 reduces serum uric acid (SUA) and alleviates liver/kidney damage in mice with acute hyperuricemia (HUA). NLRP3/URAT1-IN-1can be used for the study of gout and hyperuricemia[1].

IC50 & Target[1]

IL-1β

2.61 μM (IC50)

NLRP3

 

OAT4

6.08 μM (IC50)

URAT1

3.81 μM (IC50)

GLUT9

11.02 μM (IC50)

体外研究
(In Vitro)

NLRP3/URAT1-IN-1 (Compound 32) 在 HEK293-URAT1 过表达细胞中对 URAT1 表现出强效抑制活性，IC50 值为 3.81 μM[1]。
NLRP3/URAT1-IN-1 在 HEK293-OAT4 过表达细胞中使用 6-羧基荧光素 (6-CFL) 作为底物时，对 OAT4 显示出抑制作用，IC50 值为 6.08 μM[1]。
NLRP3/URAT1-IN-1 通过全细胞膜片钳记录在 HEK293-GLUT9 过表达细胞中对 GLUT9 发挥抑制活性，IC50 值为 11.02 μM[1]。
NLRP3/URAT1-IN-1 (3 μM, 45 min) 抑制 LPS (HY-D1056) 和 ATP 刺激的小鼠骨髓源性巨噬细胞 (BMDMs) 中 IL-1β 的释放，IC50 值为 2.61 μM，且不影响 TNF-α 和 IL-6 的产生[1]。
NLRP3/URAT1-IN-1 在人肝微粒体中对 CYP2C9 (IC50 = 2.77 μM) 和 CYP2C19 (IC50 = 2.03 μM) 表现出适中的抑制活性[1]。

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

NLRP3/URAT1-IN-1 相关抗体:
体内研究
(In Vivo)

NLRP3/URAT1-IN-1 (Compound 32) (2 mg/kg，口服，单次剂量) 显著降低由 Hypoxanthine (HY-N0091) 和 Potassium oxonate (HY-17511) 诱导的急性高尿酸血症 (HUA) 小鼠的血清尿酸 (SUA) 水平[1].
NLRP3/URAT1-IN-1 (2 mg/kg，口服，每日给药，3 天) 显著减轻由关节腔内注射 MSU 晶体诱导的急性痛风性关节炎大鼠的踝关节肿胀[1].

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

Animal Model: 3-week-old healthy Kunming (KM) mice with acute hyperuricemia (HUA) induced by hypoxanthine and potassium oxonate[1]
Dosage: 2 mg/kg
Administration: p.o., single dose
Result: Reduced serum uric acid (SUA) levels.
Animal Model: 7-8-week-old male Sprague-Dawley (SD) rats (180-220 g) with acute gouty arthritis induced by intra-articular injection of MSU crystals[1]
Dosage: 2 mg/kg
Administration: p.o., daily, 3 days
Result: Reduced ankle swelling and IL-1β release.
分子量

525.44

Formula

C24H17BrN2O3S2
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

NLRP3/URAT1-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:

NLRP3/URAT1-IN-12994637-53-3NOD-like Receptor (NLR)URAT1Interleukin RelatedOATGLUTUrate transporter 1SLC22A12ILOrganic anion transporterGlucose transporterInhibitorinhibitorinhibit

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