2. Immunology/Inflammation
  3. Complement System
  4. PMX 205 Trifluoroacetate

PMX 205 Trifluoroacetate is a specific complement C5aR1 isoform antagonist.

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

PMX 205 Trifluoroacetate Chemical Structure

PMX 205 Trifluoroacetate Chemical Structure

Size Price Stock Quantity
1 mg USD 75 In-stock
5 mg USD 180 In-stock
10 mg USD 290 In-stock
25 mg USD 560 In-stock
50 mg USD 890 In-stock
100 mg USD 1350 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of PMX 205 Trifluoroacetate:

PMX 205 Trifluoroacetate Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

PMX 205 Trifluoroacetate is a specific complement C5aR1 isoform antagonist[1][2][3][4].

IC50 & Target

C5aR[1]
In Vitro

A complement activation product, C5a, is known to recruit and activate microglia and astrocytes in vitro by activation of a G protein-coupled cell-surface C5aR. In the MTT assay, in 24 h plate, it shows that all groups are significant when compared with negative control group. For PMX 205 (PMX205) group, the value recorded is in between 0.09893 to 0.2465, EP54 group, 0.02724 to 0.1748 and Tamoxifen group, the value recorded in between 0.09880 to 0.2464. For the 48 h plate of incubation time, only two groups show a significant result, which are PMX 205 and Tamoxifen. The values recorded are in between 0.04987 to 0.3273 and 0.5777 to 0.8551 respectively. For the 72 h plate, only one group shows a significant result, PMX 205 (antagonist group) with the value recorded in between 0.02136 to 0.5322[1].

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

PMX 205 Trifluoroacetate Related Antibodies
In Vivo

PMX 205 (PMX205) is an orally active, selective C5aR antagonist. Animals treated with PMX 205 (1 mg/kg/day, oral) display a significant extension of survival time and a reduction in end-stage motor scores, as compared with vehicle-treated rats. PMX 205-treated animals also display reduced levels of astroglial proliferation in the lumbar spinal cord. SOD1G93A rats are orally dosed with PMX 205 (1 mg/kg/day) from two time points (days 28 and 70) before the onset of major clinical symptoms. Both treatment groups have a significant extension in survival time compared with untreated rats (p=0.022, day 28; p=0.015, day 70), with no clear differences in outcomes between the two treatment regimens[2]. Tg2576 mice are treated with PMX 205 (PMX205) at 20 μg/mL in the drinking water (n=17) from 12 to 15 mo of age, the time frame at which there is a rapid accumulation of amyloid deposits in these animals. Untreated Tg2576 animals (n=11) are used as controls. After 3 mo, animals treated with PMX 205 show significantly less fibrillar plaque load (thioflavine reactivity) than do untreated animals. In 3×Tg mice, PMX 205 also significantly reduces hyperphosphorylated tau (69%)[3].

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

953.06

Formula

C47H63F3N10O8
Appearance

Solid

Color

White to off-white

SMILES

OC(C(F)(F)F)=O.O=C([C@H](NC([C@@]1([H])N(CCC1)C([C@](NC(CCC2=CC=CC=C2)=O)([H])CCCNC([C@H](CCCNC(N)=N)NC3=O)=O)=O)=O)CC4CCCCC4)N[C@@]3([H])CC5=CNC6=CC=CC=C56
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (104.93 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0493 mL 5.2463 mL 10.4925 mL
5 mM 0.2099 mL 1.0493 mL 2.0985 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 (sealed storage, away from moisture). 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)

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 (2.62 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (2.62 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 99.50%

COA (251 KB) LCMS (90 KB) Elemental Analysis Report (111 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

The mouse mammary tumor cell lines 4T1 are plated at a density 5.0×104 cells/ml/well of 96-multiwell plates in complete medium. After 24 h of incubation, the medium is changed with serum starve medium to synchronize the cell cycle and growth as to ensure that the cells reaches its plateau phase. After 24 h of serum-starving, cells are treated with 5 μL/well of 0.1 M of agonist, EP54, antagonist, PMX 205 and the positive control is treated with Tamoxifen drug. 5 μL/well of the 12 mM ck solution is added 5 h before reading is taken and about 50 μL/well of the SDS-HCL solution is added and mixed thoroughly using pipette 3 h before reading is taken. The MTT assay is assessed at different time point; 0, 24, 48 and 72 h at wavelength 570 nm respectively by using ELISA plate reader Infinite M200[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2][3]

Rats[2]
Transgenic SOD1G93A rats expressing human mutant G93A SOD1 (NTac:SD-Tg SOD1G93A L26H) are used. Three experimental groups are chosen: untreated, PMX 205 treats from day 28 onward, and PMX 205 treats from day 70 onward. Animals are administered PMX 205 via drinking water (1 mg/kg/day) , from day 28 or day 70 onward; controls receive water only[2].
Mice[3]
Tg2576 mice are treated (starting at or after the initiation of plaque pathology) for 2-3 mo with PMX 205 given in the drinking water only (10-20 μg/mL, equivalent to ~3-6 mg/kg/day) or both in drinking water (10-20 μg/mL) and s.c. (1 mg/kg) twice weekly throughout the treatment period. Untreated transgenic animals of same age are used as controls. Nontransgenic littermates are similarly treated or not treated with the drug. 3×Tg mice are also treated with PMX 205 in the drinking water. Due to the low pathology of the males, only female mice of this strain are used for these studies[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 (sealed storage, away from moisture). 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 1.0493 mL 5.2463 mL 10.4925 mL 26.2313 mL
5 mM 0.2099 mL 1.0493 mL 2.0985 mL 5.2463 mL
10 mM 0.1049 mL 0.5246 mL 1.0493 mL 2.6231 mL
15 mM 0.0700 mL 0.3498 mL 0.6995 mL 1.7488 mL
20 mM 0.0525 mL 0.2623 mL 0.5246 mL 1.3116 mL
25 mM 0.0420 mL 0.2099 mL 0.4197 mL 1.0493 mL
30 mM 0.0350 mL 0.1749 mL 0.3498 mL 0.8744 mL
40 mM 0.0262 mL 0.1312 mL 0.2623 mL 0.6558 mL
50 mM 0.0210 mL 0.1049 mL 0.2099 mL 0.5246 mL
60 mM 0.0175 mL 0.0874 mL 0.1749 mL 0.4372 mL
80 mM 0.0131 mL 0.0656 mL 0.1312 mL 0.3279 mL
100 mM 0.0105 mL 0.0525 mL 0.1049 mL 0.2623 mL
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PMX 205 Trifluoroacetate 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:

PMX 205PMX205PMX-205Complement SystemInhibitorinhibitorinhibit

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