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Chemical Structure| 1140525-25-2 Chemical Structure| 1140525-25-2

Structure of SB290157 trifluoroacetate
CAS No.: 1140525-25-2

Chemical Structure| 1140525-25-2

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

Synonyms: SB 290157 (trifluoroacetate salt)

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Product Details of SB290157 trifluoroacetate

CAS No. :1140525-25-2
Formula : C24H29F3N4O6
M.W : 526.51
SMILES Code : N=C(N)NCCC[C@@H](C(O)=O)NC(COCC(C1=CC=CC=C1)C2=CC=CC=C2)=O.O=C(O)C(F)(F)F
Synonyms :
SB 290157 (trifluoroacetate salt)
MDL No. :MFCD04974198

Safety of SB290157 trifluoroacetate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
CAFs 0.5 μg/ml 24 hours To investigate the effect of C3a on CAFs activation, results showed that C3a stimulation increased α-SMA expression and TGF-β secretion in CAFs. PMC6958674
human polymorphonuclear leukocyte (PMN) 153 nM 60 minutes To evaluate the binding ability of SB290157 to human PMN C3a receptors, showing that it binds to C3a receptors but not to C5a receptors. PMC1575041
microglia 1 μg/μL 9 hours To examine the role of C3aR, microglial were treated with 1 μg/μL C3aR antagonist (SB290157) for 9 h, and the results showed that SB290157 inhibited C3aR expression and pro-inflammatory gene expression PMC10122675
HMC3 microglia cells 100 nM C3a To investigate the effect of C3a on M2 polarization of microglia, results showed that C3a increased the expression of CD206 and CD163, indicating that C3a promoted M2 polarization. PMC11466187
Primary murine macrophages 100 nM C3a To investigate the effect of C3a on M2 polarization of murine macrophages, results showed that C3a increased the expression of CD206 and CD163, indicating that C3a promoted M2 polarization. PMC11466187

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Bilateral common carotid artery occlusion (BCCAO) model Intraperitoneal injection 1 mg/kg Once a day for 28 days SB290157 decreased the number of microglia adhering to myelin, attenuated white matter injury and cognitive deficits PMC6929610
C57BL/6 mice Thromboembolic stroke model Intraperitoneal injection (PT model) and intravenous injection (eMCAo model) 20 mg/kg Single dose SB290157 is neuroprotective in thromboembolic stroke models both alone and in combination with late IVT, improving neurological outcomes and reducing infarct volume. PMC7205805
rat intestinal ischaemia/reperfusion injury model intravenous injection 0.1–1.0 mg/kg single dose, 45 minutes prior to reperfusion To evaluate the effect of SB290157 on intestinal ischaemia/reperfusion injury in rats, showing that it can reduce intestinal edema, elevated ALT levels, and mucosal damage. PMC1575041
Mice 4 T1 breast cancer model Intraperitoneal injection 10 mg/kg body weight Twice a week for 28 days To investigate the effect of C3aR antagonist SB290157 on breast cancer lung metastasis, results showed that SB290157 significantly reduced lung metastasis. PMC6958674
Mice NMRI mice Intravenous injection 10 mg/kg Single dose SB290157 significantly attenuated the hypertensive effect of Abelcet but also caused significant tachycardia, indicating partial involvement of C3a in hypertension. PMC6396670
Mice RCAS-PDGFB and RCAS-shp53 induced glioma model Intraperitoneal injection 1 mg/kg Daily injections for 5 days, followed by 2 days off, for a total of 30 injections To investigate the effect of SB290157 on the survival of glioma-bearing mice, results showed that SB290157 alone or in combination with radiotherapy prolonged survival and reduced the number of M2-polarized macrophages. PMC11466187

Protocol

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10 mM

1.90mL

0.38mL

0.19mL

9.50mL

1.90mL

0.95mL

18.99mL

3.80mL

1.90mL

 

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