Art. -Nr.: HY-106345

ILS-920

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ILS-920 is a nonimmunosuppressive Rapamycin analog with reduced immunosuppressive activity and potent neuroprotective activity. ILS-920 binds selectively to the immunophilin FKBP52 and to the β1-subunit of L-type voltage-gated calcium channels (VGCC). ILS-920 shows 200-fold selectivity for FKBP52 versus FKBP12.

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Reinheit: 99.26%
CAS. Nr.: 892494-07-4
Formel: C₅₇H₈₆N₂O₁₄
Molecular Weight:1023.30

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

ILS-920 Chemical Structure

CAS. Nr.: 892494-07-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

L-type calcium channel

FKBP52

Alle Calcium Channel Isoform-spezifische Produkte anzeigen :

In Vitro

ILS-920 promotes neuronal survival and stimulates neurite outgrowth with potent neurotrophic activities in cortical neuronal cultures^[1].
ILS-920 can inhibit L-type Ca²⁺ channels in rat hippocampal neurons and F-11 dorsal root ganglia (DRG)/neuroblastoma cells. ILS-920 can protect neurons from Ca²⁺-induced cell death by modulating Ca²⁺ channels and promote neurite outgrowth via FKBP52 binding^[1].

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

In Vivo

In a transient middle cerebral artery occlusion (tMCAO) model of ischemic stroke, ILS-920, administered 4 h postocclusion at 10 and 30 mg/kg, significantly reduces infarct volume by 24% and 23% in 72 h, respectively, and robustly enhances functional recovery measured by improvement in neurological deficits^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 892494-07-4
Appearance Solid
Molecular Weight 1023.30
Formel C₅₇H₈₆N₂O₁₄
Color Off-white to light yellow
SMILES

O[C@H]1[C@H](OC)C[C@H](C[C@@H](C)[C@@H](OC([C@@H]2CCCCN2C(C([C@@]3(O)[C@H](C)CC[C@@H](C[C@H](OC)/C(C)=C/[C@@H]4ON(C5=CC=CC=C5)[C@H]([C@H](C[C@H]6C)C)CC4)O3)=O)=O)=O)CC([C@H](C)/C=C(C)/[C@@H](O)[C@@H](OC)C6=O)=O)CC1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (97.72 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

0.9772 mL

4.8862 mL

9.7723 mL

5 mM

0.1954 mL

0.9772 mL

1.9545 mL

10 mM

0.0977 mL

0.4886 mL

0.9772 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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (2.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (2.44 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 (280 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]. Ruan B, et al. Binding of rapamycin analogs to calcium channels and FKBP52 contributes to their neuroprotective activities. Proc Natl Acad Sci U S A. 2008 Jan 8;105(1):33-8. [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	0.9772 mL	4.8862 mL	9.7723 mL	24.4308 mL
	5 mM	0.1954 mL	0.9772 mL	1.9545 mL	4.8862 mL
	10 mM	0.0977 mL	0.4886 mL	0.9772 mL	2.4431 mL
	15 mM	0.0651 mL	0.3257 mL	0.6515 mL	1.6287 mL
	20 mM	0.0489 mL	0.2443 mL	0.4886 mL	1.2215 mL
	25 mM	0.0391 mL	0.1954 mL	0.3909 mL	0.9772 mL
	30 mM	0.0326 mL	0.1629 mL	0.3257 mL	0.8144 mL
	40 mM	0.0244 mL	0.1222 mL	0.2443 mL	0.6108 mL
	50 mM	0.0195 mL	0.0977 mL	0.1954 mL	0.4886 mL
	60 mM	0.0163 mL	0.0814 mL	0.1629 mL	0.4072 mL
	80 mM	0.0122 mL	0.0611 mL	0.1222 mL	0.3054 mL

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ILS-920

Covalent Screening Library

Macrocyclic Compound Library

Neuroprotective Compound Library

Mechanoreceptors Compound Library

Calcium Channel Blocker Library

Heterocyclic Compound Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Covalent Screening Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Alle Calcium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ILS-920

Covalent Screening Library

Macrocyclic Compound Library

Neuroprotective Compound Library

Mechanoreceptors Compound Library

Calcium Channel Blocker Library

Heterocyclic Compound Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Covalent Screening Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Alle Calcium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ILS-920 Related Classifications

HY-106345 Related Classifications