Seco Rapamycin sodium salt (Secorapamycin A monosodium)
(Synonyms: Seco雷帕霉素钠盐; Secorapamycin A monosodium) 目录号 : GC31678
A degradation product of rapamycin
Cas No.:148554-65-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >87.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Cell experiment: |
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]. |
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References: [1]. Paine MF, et al. Identification of a novel route of extraction of sirolimus in human small intestine: roles ofmetabolism and secretion. J Pharmacol Exp Ther. 2002 Apr;301(1):174-86. |
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Rapamycin is a natural macrolide immunosuppressant that activates mTORC1. Seco rapamycin (sodium salt) is a nonenzyme-dependent degradation product of rapamycin resulting from ester hydration followed by dehydration.1 It has less than 4% of the potency of rapamycin in a thymocyte proliferation assay.1 Rapamycin quickly degrades to two ring-opened products, including seco rapamycin, in the cytoplasm or in homogenates of Caco-2 cells.2 Like rapamycin, seco rapamycin is secreted from cells by P-glycoprotein and metabolized to a common dihydro species.3 While seco rapamycin poorly activates mTOR, it mimics rapamycin in its ability to inhibit the proteasome.4
1.Wang, C.P., Chan, K.W., Schiksnis, R.A., et al.High performance liquid chromatographic isolation, spectroscopic characterization, and immunosuppressive activities of two rapamycin degradation productsJ. Liq. Chromatogr.17(16)3383-3392(1994) 2.Paine, M.F., Leung, L.Y., Lim, H.K., et al.Identification of a novel route of extraction of sirolimus in human small intestine: Roles of metabolism and secretionJ. Pharmacol. Exp. Ther.301(1)174-186(2002) 3.Paine, M.F., Leung, L.Y., and Watkins, P.B.New insights into drug absorption: Studies with sirolimusTher. Drug Monit.26(5)463-467(2004) 4.Osmulski, P.A., and Gaczynska, M.Rapamycin allosterically inhibits the proteasomeMol. Pharmacol.84(1)104-113(2013)
| Cas No. | 148554-65-8 | SDF | |
| 别名 | Seco雷帕霉素钠盐; Secorapamycin A monosodium | ||
| Canonical SMILES | O=C([C@H]1N(C(C([C@@]2(O)[C@H](C)CC[C@@H](C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C([C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(/C=C/[C@H](C)C[C@H]3C[C@@H](OC)[C@H](O)CC3)=O)=O)O2)=O)=O)CCCC1)[O-].[Na+] | ||
| 分子式 | C51H78NNaO13 | 分子量 | 936.15 |
| 溶解度 | DMSO : ≥ 46 mg/mL (49.14 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.0682 mL | 5.341 mL | 10.682 mL |
| 5 mM | 0.2136 mL | 1.0682 mL | 2.1364 mL |
| 10 mM | 0.1068 mL | 0.5341 mL | 1.0682 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。