1. Epigenetics
  2. Histone Acetyltransferase
  3. Remodelin

Remodelin是一种具有口服活性的乙酰基转移酶 NAT10 的选择性抑制剂。Remodelin 抑制前列腺癌细胞中 NAT10 活性,减缓 DNA 复制,抑制细胞生长。Remodelin 在异种移植模型中抑制前列腺癌和肝细胞性肝癌的生长,并能延长早年衰老综合症鼠模型的健康寿命。

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Remodelin Chemical Structure

Remodelin Chemical Structure

CAS No. : 949912-58-7

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10 mM * 1 mL in DMSO ¥660
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5 mg ¥600
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10 mg ¥790
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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Remodelin is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model[1][2][3][4].

体外研究
(In Vitro)

Remodelin (10-40 μM,1-7 天) 在 AR 阳性和 AR 阴性前列腺癌细胞中以剂量依赖性方式抑制 NAT10 活性和细胞增殖[2]
Remodelin (20 μM,24 小时) 抑制前列腺癌细胞中的 NAT10 并减慢 DNA 复制[2]
Remodelin (1 μM,7 天) 减少 LmnaG609G/G609G 成纤维细胞核形态缺陷并增加基因组稳定性[3]

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

Cell Proliferation Assay[2]

Cell Line: Prostate cancer cell lines VCaP, PC3, and DU145
Concentration: 0,10,20,40 μM
Incubation Time: 1,2,7 days
Result: Inhibited NAT10 and suppressed the growth of both AR-positive and AR-negative prostate cancer cells.
Displayed significantly decreased cell proliferation activity over time, compared to the control group.
Decreased colony formation ability with a dose-dependent manner.

Immunofluorescence[2]

Cell Line: Prostate cancer cell lines VCaP, PC3, and DU145
Concentration: 0,10,20,40 μM
Incubation Time: 24 hours
Result: Showed a significant decrease in both the positive labeling rate and the fluorescence intensity compared to the control group.
Significantly reduced both the staining foci of IdU and the staining foci of CldU compared to control group.

Western Blot Analysis[3]

Cell Line: Skin fibroblasts from LmnaG609G/G609G and wildtype (WT) littermates
Concentration: 1 μM
Incubation Time: 7 days
Result: Decreased the higher level of the DNA double-strand break (DSB) marker gamma H2AX (γH2AX, Ser-139 phosphorylated histone H2AX).
体内研究
(In Vivo)

Remodelin (2 或 20 mg/kg,腹腔注射,每两天一次,持续 4 周) 显著降低肿瘤异种移植裸鼠模型中 AR 阴性前列腺癌的生长[2]
Remodelin (100 mg/kg,口服) 在 LmnaG609G/G609G 小鼠早年衰老综合症 (HGPS) 模型中抑制 NAT10 并显著延长健康寿命[3]
Remodelin (5 mg/kg,口服) 显示在小鼠中 T1/2 为 1.81 小时,口服生物利用度 (F%) 为 43.5%[3]
Pharmacokinetic parameters for Remodelin in Mice[1]

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

Route Dose (mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng/h/mL) AUC0-Ꝏ (ng/h/mL) MRT_last (h) F(%)
p.o. 5 1.81 0.25 409 235 259 0.84 43.5%
Animal Model: PC-3 cells tumor xenograft model in nude athymic BALB/c nu/nu mice[2]
Dosage: 2 or 20 mg/kg
Administration: Intraperitoneal injection (i.p.), once every two days for 4 weeks
Result: Significantly reduced AR-negative prostate cancer tumor growth.
In the high-dose group, xenograft tumor weight at the endpoint was much smaller than that in the low-dose group.
Animal Model: LmnaG609G/G609G hutchinson-gilford progeria syndrome (HGPS) mouse model[3]
Dosage: 100 mg/kg
Administration: Oral gavage (p.o.), daily schedule for 3 weeks of age onward, until the end-point Ameliorated age-dependent weight loss.
Result: Ameliorated cardiac pathology.
Led to the dramatic amelioration of HGPS cardiac pathologies, including reduction of adventitial fibrosis of the aorta, rescue of vascular smooth muscle cell loss, and salvage of smooth muscle actin (SMA) loss, both in the aorta and the coronary arteries.
Animal Model: WT Mice (Pharmacokinetic assay)[3]
Dosage: 5 mg/kg
Administration: Oral gavage (p.o.)
Result: Showed a T1/2 of 1.81 hours and oral bioavailability (F%) of 43.5% in mice[3].
分子量

282.36

Formula

C15H14N4S

CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 125 mg/mL (442.70 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.5416 mL 17.7079 mL 35.4158 mL
5 mM 0.7083 mL 3.5416 mL 7.0832 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.92%

参考文献

Remodelin 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.5416 mL 17.7079 mL 35.4158 mL 88.5395 mL
5 mM 0.7083 mL 3.5416 mL 7.0832 mL 17.7079 mL
10 mM 0.3542 mL 1.7708 mL 3.5416 mL 8.8539 mL
15 mM 0.2361 mL 1.1805 mL 2.3611 mL 5.9026 mL
20 mM 0.1771 mL 0.8854 mL 1.7708 mL 4.4270 mL
25 mM 0.1417 mL 0.7083 mL 1.4166 mL 3.5416 mL
30 mM 0.1181 mL 0.5903 mL 1.1805 mL 2.9513 mL
40 mM 0.0885 mL 0.4427 mL 0.8854 mL 2.2135 mL
50 mM 0.0708 mL 0.3542 mL 0.7083 mL 1.7708 mL
60 mM 0.0590 mL 0.2951 mL 0.5903 mL 1.4757 mL
80 mM 0.0443 mL 0.2213 mL 0.4427 mL 1.1067 mL
100 mM 0.0354 mL 0.1771 mL 0.3542 mL 0.8854 mL
Help & FAQs
  • 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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Remodelin
目录号:
HY-16706
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