1. Metabolic Enzyme/Protease
  2. Drug Metabolite
  3. Seco Rapamycin

Seco Rapamycin  (Synonyms: Seco雷帕霉素; Secorapamycin A)

目录号: HY-19555
产品使用指南

Seco Rapamycin (Secorapamycin A) 是 Rapamycin 的开环代谢物。Seco-Rapamycin 几乎不影响 mTOR 功能。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 Seco Rapamycin sodium salt 通常具有更好的水溶性和稳定性。

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Seco Rapamycin Chemical Structure

Seco Rapamycin Chemical Structure

CAS No. : 147438-27-5

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Seco Rapamycin 的其他形式现货产品:

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Other Forms of Seco Rapamycin:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Seco Rapamycin (Secorapamycin A) is the ring-opened product of Rapamycin. Seco-rapamycin is reported not to affect the mTOR function[1].

体外研究
(In Vitro)

Disposition of Seco Rapamycin in Human Tissue Homogenates and Caco-2 Cell Monolayers. To determine whether Seco Rapamycin (D2) can be metabolized to dihydro Sirolimus (M2), 20μM Seco Rapamycin is incubated with human liver, jejunal mucosal, and Caco-2 homogenates. All of these homogenates produced M2 in an NADPH-dependent manner. Ketoconazole, at a high concentration (100μM), has no effect on the formation of M2 in any of the homogenates examined. To determine whether Seco Rapamycin can be metabolized to M2 in intact cells, 20μM Seco Rapamycin is added to Caco-2 cell monolayers. When applied to the apical compartment, little Seco Rapamycin is detected in the basolateral compartment and in the cellular fraction after 4 h. In addition, little M2 is detected. LY335979 has little effect on the distribution of Seco Rapamycin after an apical dose, although M2 became detectable in the apical compartment. In contrast, when Seco Rapamycin is applied to the basolateral compartment, both Seco Rapamycin and M2 are readily detected in the apical compartment; LY335679 decreases the flux of Seco Rapamycin to the apical compartment and increases the amount of M2 in both apical and basolateral compartments[1].

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

分子量

914.17

Formula

C51H79NO13

CAS 号
中文名称

Seco雷帕霉素

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
Cell Assay
[1]

To determine whether the Sirolimus metabolite M2 is formed from the degradation product Seco Rapamycin, duplicate Caco-2 cell cultures are dosed apically or basolaterally with 20 μM Seco Rapamycin and incubated for 4 h. To determine whether Seco Rapamycin is a substrate for P-gp, duplicate cultures are incubated with 0.5 μM LY335979 in the same manner for Sirolimus. For comparison, a parallel set of cultures is incubated similarly with 20 μM Sirolimus, but dosed apically only. M2 formation is also examined in human jejunal mucosal and liver homogenates and Caco-2 homogenates by incubating each preparation, in duplicate, with 20 μM Seco Rapamycin in the same manner for Sirolimus. For comparison, a parallel set of incubations containing 20 μM Sirolimus is also performed. To determine whether a high dose of Ketoconazole (100 μM) inhibits the formation of M2, parallel experiments with Caco-2 cells and the various homogenates are performed in a similar manner, only Ketoconazole (dissolved as a 100-fold concentration solution in ethanol) is included in the incubation medium/mixtures[1].

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

参考文献

Seco Rapamycin 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 *
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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.

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产品名称:
Seco Rapamycin
目录号:
HY-19555
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