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

SB290157 trifluoroacetate 

Cat. No.: HY-101502A Purity: 99.87%
Handling Instructions

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

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10 mM * 1 mL in DMSO USD 69 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target

IC50: 200 nM (C3a)[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].

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].

Molecular Weight

526.51

Formula

C₂₄H₂₉F₃N₄O₆

CAS No.

1140525-25-2

SMILES

N=C(N)NCCC[[email protected]@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 : 125 mg/mL (237.41 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
10 mM 0.1899 mL 0.9496 mL 1.8993 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.95 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.95 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.95 mM); Clear solution

*All of the co-solvents are provided by MCE.
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

Purity: 99.87%

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Keywords:

SB290157SB 290157SB-290157Complement SystemInhibitorinhibitorinhibit

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SB290157 trifluoroacetate
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