1. Cell Cycle/DNA Damage Epigenetics
  2. HDAC
  3. PTER-IN-1

PTER-IN-1 是一种 PTER 选择性抑制剂,对 HDACs 有选择性。PTER-IN-1 可提高瘦小鼠和肥胖小鼠体内的 N-乙酰牛磺酸水平,降低肥胖小鼠的食物摄入量。PTER-IN-1 可用于肥胖症的研究。

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PTER-IN-1

PTER-IN-1 Chemical Structure

CAS No. : 3114432-21-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PTER-IN-1 is a selective inhibitor of PTER with selectivity towards HDACs. PTER-IN-1 increases the level of N-acetyltaurine in both lean and obese mice, and reduces food intake in obese mice. PTER-IN-1 can be used in the research of obesity[1].

体外研究
(In Vitro)

PTER-IN-1 (Compound 41) (1 h) 可强效且选择性地抑制重组小鼠 PTER 介导的 N-乙酰牛磺酸水解,对 HDAC 酶的选择性超过 250 倍[1]
PTER-IN-1 对 HDACs 1-11 和 SIRTs 1-4 仅表现出微弱的抑制活性,对 PTER 具有高选择性[1]

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

体内研究
(In Vivo)

PTER-IN-1 (100 mg/kg;腹腔注射;每日/单次) 在肥胖小鼠中可呈剂量依赖性地升高血浆 N-乙酰牛磺酸水平、减少食物摄入与体重、降低脂肪量、提升 Semaglutide (HY-114118) 的减重疗效,并预防 GLP-1R 激动剂停后的体重反弹[1]

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

Animal Model: C57BL/6J (male; diet-induced obese)[1]
Dosage: 100 mg/kg (acute studies; 1 week; 3 weeks; 27 days; 10 days rebound study)
Administration: i.p.; daily (chronic/rebound/combination studies); single dose (acute studies)
Result: Induced a dose-dependent increase in plasma N-acetyltaurine levels in lean mice, and increased levels up to 1 hour post-injection in lean mice and 2 hours post-injection in obese mice.
Reduced food intake at 6 and 18 hours post-single injection in obese mice.
Decreased cumulative food intake and reduced body weight over 8 days and 3 weeks of daily treatment in obese mice.
Resulted in loss of adipose mass with no changes in liver, kidney, or heart mass after 27 days of daily treatment.
When combined with semaglutide, further reduced cumulative food intake and lowered body weight compared to vehicle-treated obese mice over 1 week.
Prevented weight regain in obese mice switched from semaglutide to PTER-IN-1 after 15 days of semaglutide treatment; these mice maintained weight loss at a level comparable to mice continuing semaglutide therapy, whereas mice switched to vehicle gained weight.
分子量

372.37

Formula

C19H20N2O6

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
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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.

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产品名称:
PTER-IN-1
目录号:
HY-185341
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