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

Seco Rapamycin sodium salt  (Synonyms: Secorapamycin A monosodium)

Cat. No.: HY-19555A Pureza: 90.56%
Instrucciones de manejo Technical Support

Seco Rapamycin sodium salt is the ring-opened product of Rapamycin. Seco-rapamycin is reported not to affect the mTOR function.

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Seco Rapamycin sodium salt

Seco Rapamycin sodium salt Estructura química

No. CAS : 148554-65-8

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Descripciòn

Seco Rapamycin sodium salt is the ring-opened product of Rapamycin. Seco-rapamycin is reported not to affect the mTOR function.

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), 20 μM 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 (100 μM), 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, 20 μM 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.

Peso molecular

936.15

Fòrmula

C51H78NNaO13

No. CAS
Appearance

Solid

Color

White to yellow

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]

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

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

Solvente y solubilidad
In Vitro: 

DMSO : ≥ 46 mg/mL (49.14 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0682 mL 5.3410 mL 10.6820 mL
5 mM 0.2136 mL 1.0682 mL 2.1364 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.

  • Calculadora de molaridad

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Pureza y Documentación
Referencias
Ensayo celular
[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 no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.

Referencias

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.0682 mL 5.3410 mL 10.6820 mL 26.7051 mL
5 mM 0.2136 mL 1.0682 mL 2.1364 mL 5.3410 mL
10 mM 0.1068 mL 0.5341 mL 1.0682 mL 2.6705 mL
15 mM 0.0712 mL 0.3561 mL 0.7121 mL 1.7803 mL
20 mM 0.0534 mL 0.2671 mL 0.5341 mL 1.3353 mL
25 mM 0.0427 mL 0.2136 mL 0.4273 mL 1.0682 mL
30 mM 0.0356 mL 0.1780 mL 0.3561 mL 0.8902 mL
40 mM 0.0267 mL 0.1335 mL 0.2671 mL 0.6676 mL
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Seco Rapamycin sodium salt Related Classifications

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  • 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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Inquiry Information

Nombre del producto:
Seco Rapamycin sodium salt
Cat. No.:
HY-19555A
Cantidad:
MCE Japan Authorized Agent: