Art. -Nr.: HY-122402

Umirolimus

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Umirolimus, a macrocyclic triene lactone Rapamycin derivative, is powerful immunosuppressant and anti-inflammatory agent. Umirolimus has highly lipophilicity and can be used agent-eluting stent (DES) applications.

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Reinheit: 98.83%
CAS. Nr.: 851536-75-9
Formel: C₅₅H₈₇NO₁₄
Molecular Weight:986.28

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Umirolimus Chemical Structure

CAS. Nr.: 851536-75-9

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

Umirolimus is a macrocyclic triene lactone, developed with pharmacological properties specifically tailored for localized drug delivery. Umirolimus can be used drug-eluting stent (DES) applications. Owing to its enhanced lipophilicity,it is strongly attracted to binding sites within the vessel wall and small, tortuous vessels, and contributing to cellular absorption and sustained distribution in the vessel wall surrounding the stent^[1].
Umirolimus prevents progression of the cell cycle in G1 phase by inhibiting IL-2/mTOR-mediated P70-KD S6 protein kinase activation. Umirolimus inhibits T-cell growth, as well as smooth muscle cell growth^[1].

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

In Vivo

The elimination half-life of Umirolimus is approximately 25 h in whole blood^[1].

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

Chemical Information

CAS. Nr. 851536-75-9
Appearance Solid
Molecular Weight 986.28
Formel C₅₅H₈₇NO₁₄
Color White to light yellow
SMILES

O=C1N2[C@](CCCC2)([H])C(O[C@](CC([C@@H](/C=C([C@H]([C@H](C([C@@H](C[C@@H](/C=C/C=C/C=C([C@H](C[C@@]3([H])O[C@@](C1=O)([C@@H](CC3)C)O)OC)\C)C)C)=O)OC)O)\C)C)=O)([H])[C@H](C)C[C@H]4C[C@H]([C@@H](CC4)OCCOCC)OC)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (101.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.0139 mL

5.0696 mL

10.1391 mL

5 mM

0.2028 mL

1.0139 mL

2.0278 mL

10 mM

0.1014 mL

0.5070 mL

1.0139 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 90% (20% SBE-β-CD in Saline)

Solubility: 5 mg/mL (5.07 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (2.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Eberhard Grube, et al. BioMatrix Biolimus A9-eluting coronary stent: a next-generation drug-eluting stent for coronary artery disease. Expert Rev Med Devices. 2006 Nov;3(6):731-41. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	1.0139 mL	5.0696 mL	10.1391 mL	25.3478 mL
	5 mM	0.2028 mL	1.0139 mL	2.0278 mL	5.0696 mL
	10 mM	0.1014 mL	0.5070 mL	1.0139 mL	2.5348 mL
	15 mM	0.0676 mL	0.3380 mL	0.6759 mL	1.6899 mL
	20 mM	0.0507 mL	0.2535 mL	0.5070 mL	1.2674 mL
	25 mM	0.0406 mL	0.2028 mL	0.4056 mL	1.0139 mL
	30 mM	0.0338 mL	0.1690 mL	0.3380 mL	0.8449 mL
	40 mM	0.0253 mL	0.1267 mL	0.2535 mL	0.6337 mL
	50 mM	0.0203 mL	0.1014 mL	0.2028 mL	0.5070 mL
	60 mM	0.0169 mL	0.0845 mL	0.1690 mL	0.4225 mL
	80 mM	0.0127 mL	0.0634 mL	0.1267 mL	0.3168 mL
	100 mM	0.0101 mL	0.0507 mL	0.1014 mL	0.2535 mL

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Umirolimus

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Immunology/Inflammation Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Umirolimus

Covalent Screening Library

Macrocyclic Compound Library

Antibacterial Compound Library

Non-steroidal Anti-Inflammatory Compound Library

Heterocyclic Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Infection Compound Library

Immunology/Inflammation Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Umirolimus Related Classifications

HY-122402 Related Classifications