1. GPCR/G Protein Apoptosis
  2. Formyl Peptide Receptor (FPR) Apoptosis
  3. T0080

T0080 is a central nervous system-penetrant FPR1 inhibitor. By functionally blocking the FPR1 signaling pathway, T0080 effectively reduces neutrophil infiltration into ischemic brain tissue and maintains the integrity of the blood-brain barrier. T0080 alleviates tPA-associated hemorrhagic transformation, inhibits demyelination responses and the expression of NOX2. T0080 also possesses anti-apoptotic (apoptosis) and anti-inflammatory properties, thereby protecting myelin and reducing neurological deficits. T0080 is widely used in studies related to ischemic stroke complicated by hemorrhagic transformation after tPA thrombolysis, as well as multiple sclerosis.

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T0080

T0080 Chemical Structure

CAS No. : 2785323-68-2

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

T0080 is a central nervous system-penetrant FPR1 inhibitor. By functionally blocking the FPR1 signaling pathway, T0080 effectively reduces neutrophil infiltration into ischemic brain tissue and maintains the integrity of the blood-brain barrier. T0080 alleviates tPA-associated hemorrhagic transformation, inhibits demyelination responses and the expression of NOX2. T0080 also possesses anti-apoptotic (apoptosis) and anti-inflammatory properties, thereby protecting myelin and reducing neurological deficits. T0080 is widely used in studies related to ischemic stroke complicated by hemorrhagic transformation after tPA thrombolysis, as well as multiple sclerosis[1][2].

In Vitro

T0080 (5 µM; 2-6 h) suppresses activation of primary mouse neutrophils isolated from pMCAO mice, reduces their migration across bEnd.3 endothelial cell monolayers, and preserves bEnd.3 cell tight junction integrity and viability in vitro[1].
T0080 reduces mtFP-induced apoptosis in human induced pluripotent stem cell-derived neurons and oligodendrocytes cocultured with microglia[2].

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

In Vivo

T0080 (5 mg/kg; i.p.; single dose; 1 or 2 h post-pMCAO) significantly attenuates tPA-induced hemorrhagic transformation and neurological deficits, reduces neutrophil brain infiltration, and preserves blood-brain barrier integrity in mice[1].
T0080 (5 mg/kg; i.p.; single dose; 3 h post-tMCAO at time of tPA thrombolysis) significantly reduces tPA-induced hemorrhagic transformation and neurological deficits in the tMCAO mouse model[1].
T0080 (5 mg/kg; i.p.; daily) reduces clinical deficits, demyelination, CNS immune cell infiltration, and spinal cord inflammation in C57BL/6 EAE mice[2].
T0080 (5 mg/kg; i.p.; daily) reduces clinical deficits, demyelination, and axonal loss in the secondary progressive NOD-EAE mouse model of MS[2].
T0080 (5 mg/kg; i.p.; daily) reduces myelin loss in the cuprizone-induced demyelination mouse model of MS[2].
T0080 (5 mg/kg; i.p.; daily) reduces human FPR1-expressing microglia in humanized FPR1 transgenic EAE mice[2].

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

Animal Model: C57BL/6 mice with Ischemic stroke (male, 8-10 weeks old, photothrombotic middle cerebral artery occlusion model)[1]
Dosage: 5 mg/kg (1 h post-pMCAO); 5 mg/kg (2 h post-pMCAO)
Administration: i.p.; single dose
Result: Significantly reduced modified Neurological Severity Score (mNSS) values compared to vehicle controls.
Increased rotarod test performance times compared to vehicle controls.
Significantly decreased cerebral hemoglobin content and Evans blue extravasation in the ischemic hemisphere compared to vehicle controls.
Reduced brain infiltration of Ly6G+ neutrophils compared to vehicle controls.
Increased relative fluorescence intensity of tight junction proteins Claudin-5 and ZO-1 compared to vehicle controls.
Molecular Weight

457.44

Formula

C24H22F3N3O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC1=CC=C(C)C=C1C2=C(C(C3=CC=C(C(F)(F)F)C=C3)N(C4CCOCC4)C5=O)C5=NN2

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 (218.61 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 2.1861 mL 10.9304 mL 21.8608 mL
5 mM 0.4372 mL 2.1861 mL 4.3722 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.

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  • Dilution Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2

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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 (5.47 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 (5.47 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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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
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 2.1861 mL 10.9304 mL 21.8608 mL 54.6520 mL
5 mM 0.4372 mL 2.1861 mL 4.3722 mL 10.9304 mL
10 mM 0.2186 mL 1.0930 mL 2.1861 mL 5.4652 mL
15 mM 0.1457 mL 0.7287 mL 1.4574 mL 3.6435 mL
20 mM 0.1093 mL 0.5465 mL 1.0930 mL 2.7326 mL
25 mM 0.0874 mL 0.4372 mL 0.8744 mL 2.1861 mL
30 mM 0.0729 mL 0.3643 mL 0.7287 mL 1.8217 mL
40 mM 0.0547 mL 0.2733 mL 0.5465 mL 1.3663 mL
50 mM 0.0437 mL 0.2186 mL 0.4372 mL 1.0930 mL
60 mM 0.0364 mL 0.1822 mL 0.3643 mL 0.9109 mL
80 mM 0.0273 mL 0.1366 mL 0.2733 mL 0.6831 mL
100 mM 0.0219 mL 0.1093 mL 0.2186 mL 0.5465 mL
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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.

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T0080
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