2. Membrane Transporter/Ion Channel Neuronal Signaling Metabolic Enzyme/Protease
  3. TRP Channel URAT1 GLUT Cytochrome P450
  4. TRPV1 antagonist 10

TRPV1 antagonist 10 是一种口服有效的强效 TRPV1 拮抗剂 (IC50 = 33.06 nM)，以及中度至弱效的 URAT1 (IC50 = 22.51 μM) 和 GLUT9 (50 μM 时为 60.25%) 抑制剂。TRPV1 antagonist 10 具有镇痛、降尿酸作用。TRPV1 antagonist 10 可用于研究高尿酸血症和炎症性疼痛。

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TRPV1 antagonist 10 Chemical Structure

TRPV1 antagonist 10 Chemical Structure

CAS No. : 896584-55-7

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TRPV1 antagonist 10 相关抗体

Top Publications Citing Use of Products

查看 TRP Channel 亚型特异性产品:

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TRPC TRPM TRPV TRPA TRPML

查看 GLUT 亚型特异性产品:

查看所有亚型
GLUT1 GLUT2 GLUT3 GLUT4

查看 Cytochrome P450 亚型特异性产品:

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TRPV1 antagonist 10 is an orally active and potent TRPV1 antagonist (IC50 = 33.06 nM), moderate to weak URAT1 (IC50 = 22.51 μM) and GLUT9 (60.25% at 50 μM) inhibitor. TRPV1 antagonist 10 has analgesic and urate-lowering effect. TRPV1 antagonist 10 can be studied for research in hyperuricemia and inflammatory pain[1].

IC50 & Target[1]

TRPV1

36.47 nM (IC50)

TRPV3

>100 μM (IC50)

TRPV4

>100 μM (IC50)

TRPA1

>100 μM (IC50)

TRPM8

6.47 μM (IC50)

CYP1A2

28.31 μM (IC50)

CYP2C9

42.85 μM (IC50)

CYP2C19

9.23 μM (IC50)

CYP2D6

>100 μM (IC50)

CYP3A4M

8.73 μM (IC50)

体外研究
(In Vitro)

TRPV1 antagonist 10 (Compound 39) (50 μM，24 小时) 在经 UA (1 mM) 处理的 HEK293T 细胞中对 GLUT9 的抑制率为 60.25%[1]。
TRPV1 antagonist 10 (0-400 μM，24-72 小时) 随着剂量和孵育时间的增加，对 HepG2 和 HK2 细胞表现出更高水平的细胞毒性[1]。
TRPV1 antagonist 10 (0-100 μM，3-20 分钟) 在人和大鼠肝微粒体中表现出较高的代谢稳定性[1]。

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

TRPV1 antagonist 10 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: HepG2 and HK2 cell lines
Concentration: 0-400 μM
Incubation Time: 24 or 72 h incubation
Result: Exhibited little cytotoxicity in HepG2 cells after 24 h incubation.
Caused significant cytotoxicity at the concentration of 50 μM after 72 h incubation in HepG2 cells.
Led to significant inhibition of cell viability in HK2 cell line at 200 μM and 24 h incubation.
Had slightly less toxicity in both cell lines in comparison to Benzbromaron (HY-B1135).
药代动力学
(Parmacokinetics)
Species Dose SampleTime Route Indicator value
Rat 1 mg/kg 24 h i.v. T1/2 14.38 hr
Rat 3 mg/kg 24 h p.o. T1/2 8.27 hr
Rat 1 mg/kg 24 h i.v. Cmax 106.16 ng/mL
Rat 3 mg/kg 24 h p.o. Tmax 0.5 hr
Rat 1 mg/kg 24 h i.v. AUC0-t 121.54 ng·h/mL
Rat 3 mg/kg 24 h p.o. Cmax 37.94 ng/mL
Rat 1 mg/kg 24 h i.v. AUC0-inf 153.12 ng·h/mL
Rat 3 mg/kg 24 h p.o. AUC0-t 141.01 ng·h/mL
Rat 1 mg/kg 24 h i.v. MRT 13.39 hr
Rat 3 mg/kg 24 h p.o. AUC0-inf 157.95 ng·h/mL
Rat 1 mg/kg 24 h i.v. F 100 %
Rat 3 mg/kg 24 h p.o. MRT 8.78 hr
Rat 3 mg/kg 24 h p.o. CL/F 0.018993 mg·h/L
Rat 3 mg/kg 24 h p.o. F 34.4 %
体内研究
(In Vivo)

TRPV1 antagonist 10 (Compound 39) (3-20 mg/kg，口服，单次给药) 在雄性昆明小鼠福尔马林诱发的 I 期和 II 期疼痛模型中均表现出剂量依赖性的镇痛作用[1]。
TRPV1 antagonist 10 (10-20 mg/kg，口服，连续 21 天) 可降低高尿酸血症小鼠模型中的尿酸，20 mg/kg 的剂量可降低尿酸水平并改善肾功能[1]。
TRPV1 antagonist 10 (500 mg/kg，口服，单次给药) 未导致健康昆明小鼠出现明显异常行为，体重和食物摄入量也无明显差异[1]。
TRPV1 antagonist 10 (100 mg/kg，口服，隔日给药，连续 14 天) 未导致健康昆明小鼠出现明显异常行为，体重和食物摄入量也无明显差异[1]。

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

Animal Model: Male Kunming mice, 5% Formalin (injected subcutaneously into the right rear toe)-induced persistent pain model (8 weeks, 22-25 g)[1]
Dosage: 3 mg/kg, 10 mg/kg, 20 mg/kg
Administration: Oral gavage (p.o.), one single dose
Result: Showed no obvious anti-nociceptive activity at dose of 3 mg/kg and 10 mg/kg.
Exhibited significantly better analgesic effect with 20 mg/kg dosage in phase I (0-5 min) and phase II (6-45 min) pain.
Animal Model: Male Kunming hyperuricemia mice model (8 weeks, 22-25 g)[1]
Dosage: 10 mg/kg, 20 mg/kg
Administration: Oral gavage (p.o.), 21 consecutive days
Result: Reduced inflammatory cytokines (IL-1β, TNF-α, and IL-6) with both dosages.
Reduced the level of renal interstitial fibrosis after 21 continuous days.
分子量

314.29

Formula

C16H14N2O5
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

TRPV1 antagonist 10 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

TRPV1 antagonist 10896584-55-7TRP ChannelURAT1GLUTCytochrome P450Transient receptor potential channelsUrate transporter 1SLC22A12Glucose transporter CYPsTRPV1analgesicuric-acidGLUT9hyperuricemiainflammatory paininflammationInhibitorinhibitorinhibit

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