Seco Rapamycin ethyl ester

製品番号: HY-133770: Data Sheet SDS 取扱説明書
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Seco Rapamycin ethyl ester is an open-ring metabolite of Rapamycin derivative. Seco-rapamycin is reported not to affect the mTOR function.

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Seco Rapamycin ethyl ester 構造式

容量	価格（税別）	在庫状況
5 mg	$450	見積もりとリードタイムを求めるのご確認
10 mg	$750	見積もりとリードタイムを求めるのご確認
50 mg	$2200	見積もりとリードタイムを求めるのご確認

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

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生物活性
純度とドキュメンテーション
参考文献
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製品説明

Seco Rapamycin ethyl ester is an open-ring metabolite of Rapamycin derivative. Seco-rapamycin is reported not to affect the mTOR function^[1].

体外実験

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].

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

分子量

942.23

分子式

C₅₃H₈₃NO₁₃

Appearance

Oil

Color

Light yellow to yellow

SMILES

C[C@H]1[C@@](C(C(N2[C@H](C(OCC)=O)CCCC2)=O)=O)(O)O[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]3CC[C@@H](O)[C@H](OC)C3)=O)=O)CC1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

-20°C, protect from light, stored under nitrogen

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

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (106.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.0613 mL	5.3066 mL	10.6131 mL
5 mM	0.2123 mL	1.0613 mL	2.1226 mL
10 mM	0.1061 mL	0.5307 mL	1.0613 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 5 mg/mL (5.31 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (5.31 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (5.31 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

データシート (269 KB) SDS (251 KB) 取扱説明書 (2659 KB)

参考文献

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.0613 mL	5.3066 mL	10.6131 mL	26.5328 mL
	5 mM	0.2123 mL	1.0613 mL	2.1226 mL	5.3066 mL
	10 mM	0.1061 mL	0.5307 mL	1.0613 mL	2.6533 mL
	15 mM	0.0708 mL	0.3538 mL	0.7075 mL	1.7689 mL
	20 mM	0.0531 mL	0.2653 mL	0.5307 mL	1.3266 mL
	25 mM	0.0425 mL	0.2123 mL	0.4245 mL	1.0613 mL
	30 mM	0.0354 mL	0.1769 mL	0.3538 mL	0.8844 mL
	40 mM	0.0265 mL	0.1327 mL	0.2653 mL	0.6633 mL
	50 mM	0.0212 mL	0.1061 mL	0.2123 mL	0.5307 mL
	60 mM	0.0177 mL	0.0884 mL	0.1769 mL	0.4422 mL
	80 mM	0.0133 mL	0.0663 mL	0.1327 mL	0.3317 mL
	100 mM	0.0106 mL	0.0531 mL	0.1061 mL	0.2653 mL