SB290157 trifluoroacetate

Catalog No.S8931 Batch:S893101

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.)

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.50mM)	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
(Cell-free assay)

200 nM

In vitro

SB 290157 functions as a competitive antagonist of 125I-C3a radioligand binding to rat basophilic leukaemia (RBL)-2H3 cells expressing the human C3aR (RBLC3aR), with an IC50 of 200 nM. SB 290157 is a functional antagonist, blocking C3a-induced C3aR internalisation in a concentration-dependent manner and C3a-induced Ca21 mobilisation 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 antagonise the C5aR or six other chemotactic G protein-coupled receptors. Functional antagonism is not solely limited to the human C3aR; SB 290157 also inhibits C3a-induced Ca21 mobilisation 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.

In Vivo

In animal models, SB 290157, inhibits neutrophil recruitment in a guinea pig LPS-induced airway neutrophilia model and decreases paw oedema in a rat adjuvant-induced arthritis model.

Protocol (from reference)

Cell Assay:^{^[1]}	Cell Lines RBL-2H3 cells, HMC-1 cells Concentrations 100 nM to 10 μM Incubation Time 45 min Method 2–5 × 10⁵ RBL-C3aR cells are incubated with 100 pM ¹²⁵I-C3a and varying concentrations of antagonist at room temperature in 20 mM HEPES (pH 7.4), 125 mM NaCl, 5 mM KCl, 1 mM CaCl2, 1 mM MgCl2, 0.25% BSA and 0.5 mM glucose (HAG-CM) for 45 min at room temperature. The unbound ligand is removed by vacuum filtration using the HV Millipore MultiScreen assay plate with a Durapore 0.45-mm pore size membrane equilibrated with HAG-CM. Filters are washed twice with 100 ml/well HAG-CM and dried. Plates are counted on a Beckman gamma counter 5500B.
Animal Study:^{^[1]}	Animal Models Male Hartley guinea pigs, 6–8 week old male Lewis rats Dosages 30 mg/kg, 10 mg/kg, 3 mg/kg Administration IP

Cell Assay:^{^[1]}

Cell Lines
RBL-2H3 cells, HMC-1 cells
Concentrations
100 nM to 10 μM
Incubation Time
45 min
Method
2–5 × 10⁵ RBL-C3aR cells are incubated with 100 pM ¹²⁵I-C3a and varying concentrations of antagonist at room temperature in 20 mM HEPES (pH 7.4), 125 mM NaCl, 5 mM KCl, 1 mM CaCl2, 1 mM MgCl2, 0.25% BSA and 0.5 mM glucose (HAG-CM) for 45 min at room temperature. The unbound ligand is removed by vacuum filtration using the HV Millipore MultiScreen assay plate with a Durapore 0.45-mm pore size membrane equilibrated with HAG-CM. Filters are washed twice with 100 ml/well HAG-CM and dried. Plates are counted on a Beckman gamma counter 5500B.

Animal Study:^{^[1]}

Animal Models
Male Hartley guinea pigs, 6–8 week old male Lewis rats
Dosages
30 mg/kg, 10 mg/kg, 3 mg/kg
Administration
IP

References

https://pubmed.ncbi.nlm.nih.gov/11342658/

Sellecks SB290157 trifluoroacetate Has Been Cited by 5 Publications

C3/C3aR Bridges Spinal Astrocyte-Microglia Crosstalk and Accelerates Neuroinflammation in Morphine-Tolerant Rats [ CNS Neurosci Ther, 2025, 31(1):e70216]	PubMed: 39801259
Complement C3/C3aR Signaling Pathway Inhibition Ameliorates Retinal Damage in Experimental Retinal Vein Occlusion [ Invest Ophthalmol Vis Sci, 2025, 66(5):2]	PubMed: 40310626
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

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

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.