2. Metabolic Enzyme/Protease
  3. Phosphatase
  4. Pimecrolimus

Pimecrolimus  (Synonyms: SDZ-ASM 981)

Cat. No.: HY-13723 Purity: ≥98.0%
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Pimecrolimus (SDZ-ASM 981) is a potent, nonsteroid and orally active calcineurin inhibitor with a Ki of 117 nM. Pimecrolimus shows anti-inflammatory activity.

For research use only. We do not sell to patients.

Pimecrolimus Chemical Structure

Pimecrolimus Chemical Structure

CAS No. : 137071-32-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 25 In-stock
10 mg USD 40 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Based on 3 publication(s) in Google Scholar

Other Forms of Pimecrolimus:

Pimecrolimus Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Pimecrolimus (SDZ-ASM 981) is a potent, nonsteroid and orally active calcineurin inhibitor with a Ki of 117 nM. Pimecrolimus shows anti-inflammatory activity[1][2].

IC50 & Target

Calcineurin[1]
In Vitro

Pimecrolimus (SDZ-ASM 981) (100 nM) targets T-cells and mast cells and inhibits the production and release of cytokines and other inflammatory mediators, as well as the expression of signals essential for the activation of inflammatory T-lymphocytes[1].
Pimecrolimus acts specifically on cells that are crucial for the effector phase of an inflammatory reaction[1].
Pimecrolimus (10 nM; 3 days) inhibits the polyclonal growth of peripheral blood T cells in murine and human mixed lymphocyte reactions[2].
Pimecrolimus inhibits cytokine IL-2, IL-4, IL-10 and interferon-γ release from T-cell clone CFTS4:3.1 with IC50s of 0.28, 0.3, 0.2 and 0.42 nM, respectively after antigen-specific stimulation[2].

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

Pimecrolimus Related Antibodies

Cell Proliferation Assay[2]

Cell Line: T-cell clone (TCC), murine and human mixed lymphocyte reactions (MLR)
Concentration: 0-10 nM
Incubation Time: 3 days
Result: Inhibited proliferation of TCC CFTS 4:3.1 with IC50s of 0.78-2.6 nM. Inhibited murine and human MLR with IC50s of both 1.3 nM.
In Vivo

Pimecrolimus (SDZ-ASM 981) (0-0.4%; topical; 10 μL once) inhibits allergic contact dermatitis in mice and pigs[3].
Pimecrolimus (0-90 mg/kg; p.o. or s.c.; twice or once) potently inhibits allergic contact dermatitis in mice and rats[3].

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

Animal Model: Female NMRl mice, allergic contact dermatitis model[3]
Dosage: 0.004%, 0.01%, 0.04%, 0.13% and 0.4% in10 μL ethanolic solution
Administration: Topical application, once
Result: Inhibited oedema formation by 17% at concentration of 0.004%.
Animal Model: Female NMRl mice, allergic contact dermatitis model[3]
Dosage: 10, 30, 90 mg/kg (oral) or 1.5, 4.5, 13.5 mg/kg (subcutaneous)
Administration: Oral (twice) or subcutaneous administration (once)
Result: Signiticantiy inhibited inflammatory ear oedema formation.
Clinical Trial
Molecular Weight

810.45

Formula

C43H68ClNO11
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@](CCCC1)([H])N1C(C([C@@]2(O)[C@H](C)C[C@H](OC)[C@@](O2)([H])[C@@H](OC)C[C@@H](C)C/C(C)=C/[C@H]3CC)=O)=O)O[C@H](/C(C)=C/[C@H]4C[C@@H](OC)[C@@H](Cl)CC4)[C@H](C)[C@@H](O)CC3=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 32 mg/mL (39.48 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 1.2339 mL 6.1694 mL 12.3388 mL
5 mM 0.2468 mL 1.2339 mL 2.4678 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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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:

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 (3.08 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 (3.08 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

mg/kg

Animal weight
(per animal)

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: ≥98.0%

SDS (419 KB)

COA (261 KB) HNMR (299 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2339 mL 6.1694 mL 12.3388 mL 30.8471 mL
5 mM 0.2468 mL 1.2339 mL 2.4678 mL 6.1694 mL
10 mM 0.1234 mL 0.6169 mL 1.2339 mL 3.0847 mL
15 mM 0.0823 mL 0.4113 mL 0.8226 mL 2.0565 mL
20 mM 0.0617 mL 0.3085 mL 0.6169 mL 1.5424 mL
25 mM 0.0494 mL 0.2468 mL 0.4936 mL 1.2339 mL
30 mM 0.0411 mL 0.2056 mL 0.4113 mL 1.0282 mL
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Pimecrolimus 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:

Pimecrolimus137071-32-0SDZ-ASM 981PhosphataseT-cellsmast cellsorally activeanti-inflammatoryatopic dermatitisoral erosive lichen planusinflammatory skin diseasesInhibitorinhibitorinhibit

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