2. Membrane Transporter/Ion Channel
  3. Amino acid Transporter
  4. INSP-0154

INSP-0154 是一种强效的肌酸激酶 B (CKB)/肌酸转运体 (SLC6A8) 抑制剂。INSP-0154 可结合至 SLC6A8 的闭合口袋，阻止肌酸转运进入细胞，并保护 SLC6A8 的半胱氨酸残基 C144 免受不可逆失活。INSP-0154 可抑制小鼠心脏组织中的肌酸摄取。INSP-0154 可用于癌症研究。

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INSP-0154

INSP-0154 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

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INSP-0154 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

INSP-0154 is a potent creatine kinase B (CKB)/creatine transporter (SLC6A8) inhibitor. INSP-0154 binds to the SLC6A8 occluded pocket, prevents creatine transport into cells, and protects SLC6A8 cysteine residue C144 from irreversible inactivation. INSP-0154 inhibits creatine uptake in mouse heart tissue. INSP-0154 can be used for the research of cancer[1].

体外研究
(In Vitro)

INSP-0154 (Compound 46) (0.46-1000 μM; 1 h) 可强效抑制 HCT-116 细胞中由 SLC6A8 介导的肌酸摄取，其 IC50 为 8.2 μM[1]。
INSP-0154 (0.46-1000 μM) 可抑制 GAT-2、GAT-3、BGT-1 和 TAUT 介导的肌酸摄取，其 IC50 分别为 22.7、150、116 和 11.9 μM，而在最高 1000 μM 的浓度下对 GAT-1 无活性[1]。
INSP-0154 表现出较强的体外血浆稳定性与代谢稳定性，Caco-2 通透性较低，且并非 P-gp 外排底物[1]。

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

INSP-0154 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Tmax AUClast T1/2 F C0
Mice[1] 3 mg/kg i.v. / / 2151 ng·h/mL 0.9 h / 7698 ng/mL
Mice[1] 100 mg/kg p.o. 13517 ng/mL 0.5 h 30616 ng·h/mL 2.7 h 42.7 % /
Mice[1] 100 mg/kg i.p. 42700 ng/mL 0.5 h 27742 ng·h/mL 3.3 h 59.6 % /
体内研究
(In Vivo)

INSP-0154 (Compound 46) (100 mg/kg；腹腔注射；单剂量) 有效地抑制小鼠心脏组织中的 肌酸转运[1]。

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

Animal Model: C57BL/6 (male, 6−9 weeks old)[1]
Dosage: 100 mg/kg
Administration: i.p.; single dose
Result: Achieved inhibition of creatine-d3 uptake in heart tissue, with greater potency than β-GPA under the tested conditions.
分子量

170.17

Formula

C6H10N4O2
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

INSP-0154 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

INSP-0154INSP0154INSP 0154Amino acid Transporter氨基酸转运蛋白creatineC57BL/6 micecancerC144HCT-116 cellsGAT-3TAUTBGT-1GAT-2SLC6A8Inhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-181753
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