2. Membrane Transporter/Ion Channel
  3. URAT1
  4. URAT1 inhibitor 10

URAT1 inhibitor 10 (Compound 23a) 是 URAT1 抑制剂 (IC50 = 0.052 μM)。具有口服有效性，低细胞毒性。对 OAT1 有高选择性 (IC50 =9.17 μM)。

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URAT1 inhibitor 10 Chemical Structure

URAT1 inhibitor 10 Chemical Structure

CAS No. : 3012586-38-5

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URAT1 inhibitor 10 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

URAT1 inhibitor 10 (Compound 23a) is a URAT1 inhibitor. URAT1 inhibitor 10 has oral efficacy and low cytotoxicity. URAT1 inhibitor 10 has high selectivity for OAT1 [1].

体外研究
(In Vitro)

URAT1 inhibitor 10 (5 μM; 30min) 在 MDCK-hOAT 细胞中对 OAT1 的活性抑制(IC50 =9.17 μM)[1]。
URAT1 inhibitor 10 (24 h) 在 RAW264.7 细胞中，对 IL-6 有中度抑制作用 (IR = 25.6%)，可能缓解与 MSU 晶体介导的炎性细胞因子相关的症状[1]。
URAT1 inhibitor 10 对 HepG2 细胞显示低细胞毒性 (IC50 > 64 μg/mL)[1]。

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

URAT1 inhibitor 10 相关抗体:
体内研究
(In Vivo)

URAT1 inhibitor 10 (50 mg/kg; p.o.) 具有良好的药代动力学特性[1]。
URAT1 inhibitor 10 (10 mg/kg; p.o.一天一次持续七天) 用氧酸钾诱导的高尿酸血症小鼠模型中,血清尿酸 (SUA) 显示出显着的活性降低，降低比率为 53.9 %, 相当于相同剂量下的阳性对照 Lesinurad (HY-15258)[1]。

Pharmacokinetic Analysis in URAT1 inhibitor 10 Model[1]

药代动力学分析[1]

Route Dose (mg/kg) t1/2 (h) tmax (h) Cmax (ng/mL) AUC(0-t) (ng·h/mL) AUC(0-∞) (ng·h/mL) MRT(0-∞) (h)
p.o. 50 1.9 0.25 8187 10050 10255 1.43

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

Animal Model: hyperuricemia mice [1]
Dosage: 10 mg/kg； Once a day for seven days
Administration: p.o.
Result: Exhibited significant serum uric acid-lowering activity. The serum uric acid (SUA) levels decreased to 424 μM, achieving a reduction ratio of 53.9%. This performance was comparable to that of the positive control, Lesinurad (HY-15258), which also demonstrated significant SUA-lowering effects at the same dose.
分子量

427.44

Formula

C19H20F3N3O3S
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

URAT1 inhibitor 10 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:

URAT1 inhibitor 103012586-38-5URAT1Urate transporter 1SLC22A12Quinoline formamides， Hyperuricemia， Anti-inflammatory activity， Druggability， hyperuricemia miceInhibitorinhibitorinhibit

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目录号：
HY-163431
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