SB290157 trifluoroacetate

Catalog No.S8931 Batch:S893101

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Technical Data

Formula

C24H29F3N4O6
Molecular Weight 526.51 CAS No. 1140525-25-2
Solubility (25°C)* In vitro DMSO 100 mg/mL (189.92 mM)
Ethanol 100 mg/mL (189.92 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/m clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description SB290157 trifluoroacetate (SB 290157 TFA) is a potent, competitive and selective antagonist of C3a receptor (C3aR) with IC50 of 200 nM for RBL-C3aR.
Targets
RBL-C3aR [1]
(Cell-free assay)
200 nM
In vitro

SB 290157 functions as a competitive antagonist of 125I-C3a radioligand binding to rat basophilic leukemia (RBL)-2H3 cells expressing the human C3aR (RBLC3aR), with an IC50 of 200 nM. SB 290157 is a functional antagonist, blocking C3a-induced C3aR internalization in a concentration-dependent manner and C3a-induced Ca21 mobilization in RBL-C3aR cells and human neutrophils with IC50s of 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. Functional antagonism is not solely limited to the human C3aR; SB 290157 also inhibits C3ainduced Ca21 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

In animal models, 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]

Biological Activity

Description SB290157 trifluoroacetate (SB 290157 TFA) is a potent, competitive and selective antagonist of C3a receptor (C3aR) with IC50 of 200 nM for RBL-C3aR.
Targets
RBL-C3aR [1]
(Cell-free assay)
200 nM

Protocol (from reference)

Selleck's SB290157 trifluoroacetate has been cited by 3 publications

Cntnap4 partial deficiency exacerbates α-synuclein pathology through astrocyte-microglia C3-C3aR pathway [ Cell Death Dis, 2023, 14(4):285] PubMed: 37087484
Complement C3a receptor inactivation attenuates retinal degeneration induced by oxidative damage [ Front Neurosci, 2022, 16:951491] PubMed: 36110094
Astrocyte-microglia interaction through C3/C3aR pathway modulates neuropathic pain in rats model of chronic constriction injury [ Mol Pain, 2022, 18:17448069221140532] PubMed: 36341694

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.