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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. J Exp Clin Cancer Res. 2020 Jan 13;39(1):11.
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. Br J Pharmacol. 2004 Jun;142(4):756-64.
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 Cell Death Dis. 2023 Apr 22;14(4):285.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
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. Br J Pharmacol. 2004 Jun;142(4):756-64.
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. JCI Insight. 2024 Aug 22;9(19):e179854.
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 Theranostics. 2020 Jan 1;10(1):74-90
Mice 4 T1 breast cancer model Intraperitoneal injection 10 mg/kg 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. J Exp Clin Cancer Res. 2020 Jan 13;39(1):11.
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. Int J Nanomedicine. 2019 Feb 26;14:1563-1573
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. Br J Pharmacol. 2020 Jun;177(11):2466-2477
Female Wistar rats Rat model of intestinal ischaemia/reperfusion injury Intravenous 0.1–1.0 mg/kg Single dose, 45 min or 120 min prior to reperfusion Evaluate the protective effects of PMX-53 on intestinal I/R injury. Results showed PMX-53 administered 45 min prior to reperfusion attenuated intestinal oedema, elevated ALT levels, and mucosal damage, but no protection was observed when administered 120 min prior to reperfusion. Br J Pharmacol. 2004 Jun;142(4):756-64.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.90mL

0.38mL

0.19mL

9.50mL

1.90mL

0.95mL

18.99mL

3.80mL

1.90mL

 

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