2. Membrane Transporter/Ion Channel
  3. GLUT URAT1
  4. URAT1/GLUT9-IN-1

URAT1/GLUT9-IN-1 (compound 29) 能抑制尿酸转运蛋白1 (URAT1) (IC50=2.01 μM) 和葡萄糖转运蛋白9 (GLUT9) (IC50=18.21 μM)。 URAT1/GLUT9-IN-1 具有良好的药代动力学特性和口服生物利用度。 URAT1/GLUT9-IN-1 可用于痛风和高尿酸血症的研究。

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URAT1/GLUT9-IN-1 Chemical Structure

URAT1/GLUT9-IN-1 Chemical Structure

CAS No. : 2883011-18-3

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URAT1/GLUT9-IN-1 相关抗体

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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

URAT1/GLUT9-IN-1 (compound 29) can inhibit both uric acid transporter 1 (URAT1) (IC50=2.01 μM) and glucose transporter 9 (GLUT9) (IC50=18.21 μM). URAT1/GLUT9-IN-1 exhibits favorable pharmacokinetic properties and oral bioavailability. URAT1/GLUT9-IN-1 can be uesd for gout and hyperuricemia research[1].

IC50 & Target[1]

GLUT9

18.21 μM (IC50)

体外研究
(In Vitro)

URAT1/GLUT9-IN-1 对 urat1 介导的 14c-尿酸摄取具有最有效的抑制作用(IC50= 2.01 μM)，是 Lesinurad(HY-15258)(IC50= 5.54 μM) 的 3 倍左右[1]。
URAT1/GLUT9-IN-1 (5 μM) 对 GLUT9 的体外抑制活性略优于 Benzbromarone(HY-B1135)， IC50 值为 18.21±1.03 μM[1]。
URAT1/GLUT9-IN-1 (10 μM) 对 XOD 的抑制率小于 20%，表明其抑制作用可以忽略不计[1]。
URAT1/GLUT9-IN-1 抑制 CYP(CYP2C9 (IC50= 2.00 μM) 和 CYP2C19 (IC50= 5.93 μM)) 药物代谢酶的抑制电位，表明具有较低的肝毒性[1]。

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

URAT1/GLUT9-IN-1 相关抗体:
体内研究
(In Vivo)

URAT1/GLUT9-IN-1 (0.25，0.5，1mg/kg，po) 对急性高尿酸血症小鼠模型的降低 SUA 活性最小有效剂量约为 0.5 mg/kg [1]。
URAT1/GLUT9-IN-1 (2mg/kg，po) 显示出作为降低 SUA 活性的候选药物的巨大潜力，与 Lesinurad (HY-15258) 相比，其效力高约 1.8 倍在稳定的高尿酸血症大鼠模型中[1]。
URAT1/GLUT9-IN-1 (100 mg/kg，100 mg/kg，隔一天口服，为期 14 天) 较 Lesinurad (HY-15258) 组安全性显著提高在慢性高尿酸血症小鼠[1]。
Pharmacokinetic Analysis in SD rats[1]

Route Dose (mg/kg) AUC0_t (ng•h/mL) AUC0_INF (ng•h/mL) MRT0_INF (h) T1/2 (h) Tmax (h) Cmax (ng/mL) Cl (L•h/kg) F (%)
p.o. 2 1813.4 7929.1 2.5 1.8 0.25 1272.7 / 20.1
i.v. 2 1903.7 1922.9 0.5 1.6 0.083 6591.8 17.5 /

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

Animal Model: stable hyperuricemia rat model
Dosage: 2 mg/kg
Administration: Oral gavage (p.o.)
Result: Had 90.12% titer ratio of decreasing sua activity.
Animal Model: 14-day model of chronic hyperuricemia
Dosage:
Administration: i.g.
Result: Exhibited superior therapeutic efficacy (76.33%) in chronic hyperuricemia in mice compared to lesinurad (33.56%)
Animal Model: Healthy Mice
Dosage: 100 mg/kg every other day for a period of 14 days
Administration: Oral gavage (p.o.)
Result: Caused slight weight loss and mild kidney damage.
分子量

435.56

Formula

C23H21N3O2S2
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/GLUT9-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:

URAT1/GLUT9-IN-12883011-18-3GLUTURAT1Glucose transporter Urate transporter 1SLC22A12Gout and hyperuricemiaURAT1/GLUT9 inhibotorhyperuricemia rat modelInhibitorinhibitorinhibit

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