1. Immunology/Inflammation
  2. Complement System
  3. SB290157 trifluoroacetate

SB290157 trifluoroacetate is a potent and selective C3a receptor antagonist with an IC50 of 200 nM.

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

SB290157 trifluoroacetate Chemical Structure

SB290157 trifluoroacetate Chemical Structure

CAS No. : 1140525-25-2

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 76 In-stock
Solution
10 mM * 1 mL in DMSO USD 76 In-stock
Solid
5 mg USD 55 In-stock
10 mg USD 92 In-stock
25 mg USD 200 In-stock
50 mg USD 340 In-stock
100 mg USD 590 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 14 publication(s) in Google Scholar

Top Publications Citing Use of Products

    SB290157 trifluoroacetate purchased from MedChemExpress. Usage Cited in: Animals (Basel). 2023 Feb 24.

    SB290157 trifluoroacetate (10 mg/kg; i.p.; single) significantly down-regulates the protein level of C3aR in mouse ileum tissues, 3 hours after injection.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    SB290157 trifluoroacetate is a potent and selective C3a receptor antagonist with an IC50 of 200 nM.

    IC50 & Target

    IC50: 200 nM (C3aR)[1]

    In Vitro

    SB 290157, functions as a competitive antagonist of 125I-C3a radioligand binding to rat basophilic leukemia-2H3 cells expressing the human C3aR (RBL-C3aR), with an IC50 of 200 nM. SB 290157 blocks C3a-induced C3aR internalization in a concentration-dependent manner and C3a-induced Ca2+ mobilization in RBL-C3aR cells and human neutrophils with IC50s f 27.7 and 28 nM, respectively. SB 290157 is selective for the C3aR in that it does not antagonize the C5aR or six other chemotactic G protein-coupled receptors. SB 290157 also inhibits C3a-induced Ca2+ mobilization of RBL-2H3 cells expressing the mouse and guinea pig C3aRs. It potently inhibits C3a-mediated ATP release from guinea pig platelets and inhibits C3a-induced potentiation of the contractile response to field stimulation of perfused rat caudal artery[1].

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

    In Vivo

    SB 290157, inhibits neutrophil recruitment in a guinea pig LPS-induced airway neutrophilia model and decreases paw edema in a rat adjuvant-induced arthritis model[1]. The antagonist is able to reduce joint swelling only at 3 h, and about 50% inhibition of joint swelling is observed with the concentration of 30 mg/kg. The C3 level is significantly decreased at 3 h compared with naive mice showing complement consumption. Furthermore, the C3 activation is observed and increased corresponding to the graded concentration of anti-OVA pAb[2].

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

    Molecular Weight

    526.51

    Formula

    C24H29F3N4O6

    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    N=C(N)NCCC[C@@H](C(O)=O)NC(COCC(C1=CC=CC=C1)C2=CC=CC=C2)=O.OC(C(F)(F)F)=O

    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 (189.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 100 mg/mL (189.93 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8993 mL 9.4965 mL 18.9930 mL
    5 mM 0.3799 mL 1.8993 mL 3.7986 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% EtOH    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 5 mg/mL (9.50 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (50.0 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% EtOH    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 5 mg/mL (9.50 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (50.0 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: 99.87%

    References
    Animal Administration
    [1][2]

    Rats: SB 290157 is administered b.i.d. at 30, 10, and 3 mg/kg i.p. in a final volume of 0.5 mL starting on the day of adjuvant injection. Cages are modified to allow the compromised animals free access to food and water. Control animals are given vehicle alone. Change in paw volume is presented as mean and SEM of 10-12 animals/group, and the percentage inhibition of hind paw edema is calculated[1].

    Mice: Administration of SB 290157, a C3aR antagonist, (10 or 30 mg/kg) is injected i.p. two times, at 0 (right after OVA injection) and 2 h while 5% ethanol in PBS is used as a vehicle control. Joint swelling is measured using a dial thickness gauge before injection, at 0.5 h, and then every hour until 5 h after OVA injection[2].

    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 / Ethanol 1 mM 1.8993 mL 9.4965 mL 18.9930 mL 47.4825 mL
    5 mM 0.3799 mL 1.8993 mL 3.7986 mL 9.4965 mL
    10 mM 0.1899 mL 0.9496 mL 1.8993 mL 4.7482 mL
    15 mM 0.1266 mL 0.6331 mL 1.2662 mL 3.1655 mL
    20 mM 0.0950 mL 0.4748 mL 0.9496 mL 2.3741 mL
    25 mM 0.0760 mL 0.3799 mL 0.7597 mL 1.8993 mL
    30 mM 0.0633 mL 0.3165 mL 0.6331 mL 1.5827 mL
    40 mM 0.0475 mL 0.2374 mL 0.4748 mL 1.1871 mL
    50 mM 0.0380 mL 0.1899 mL 0.3799 mL 0.9496 mL
    60 mM 0.0317 mL 0.1583 mL 0.3165 mL 0.7914 mL
    80 mM 0.0237 mL 0.1187 mL 0.2374 mL 0.5935 mL
    100 mM 0.0190 mL 0.0950 mL 0.1899 mL 0.4748 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    SB290157 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.

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

     

    Salutation

    Applicant Name *

     

    Email Address *

    Phone Number *

     

    Organization Name *

    Department *

     

    Requested quantity *

    Country or Region *

         

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    SB290157 trifluoroacetate
    Cat. No.:
    HY-101502A
    Quantity:
    MCE Japan Authorized Agent: