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  3. FKBP Calcium Channel
  4. ILS-920

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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ILS-920

ILS-920 Chemical Structure

CAS No. : 892494-07-4

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ILS-920 Related Antibodies

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Description

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[1].

IC50 & Target

L-type calcium channel

 

FKBP52

 

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.

ILS-920 Related Antibodies
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
Molecular Weight

1023.30

Formula

C57H86N2O14
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9772 mL 4.8862 mL 9.7723 mL
5 mM 0.1954 mL 0.9772 mL 1.9545 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. 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)

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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

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: ≥ 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.

    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% 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

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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.
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).
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.
Purity & Documentation

Purity: 99.9%

SDS (252 KB)

COA (262 KB) LCMS (127 KB)

Handling Instructions (2659 KB)
References

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. 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 Related Classifications

Help & FAQs
  • 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.

Keywords:

ILS-920892494-07-4ILS920ILS 920FKBPCalcium ChannelFK506-binding proteinCa2+ channelsCa channelsCa2+homeostasisRapamycinneuroprotectiveFKBP52VGCCnonimmunosuppressiveimmunosuppressiveimmunophilinbrain-penetrantInhibitorinhibitorinhibit

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