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SB290157 trifluoroacetate

Catalog No. T12851 CAS 1140525-25-2

SB290157 trifluoroacetate is a potent and selective antagonist of C3a receptor(IC50 of 200 nM).

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SB290157 trifluoroacetate Chemical Structure

SB290157 trifluoroacetate, CAS 1140525-25-2

Pack Size	Availability	Price/USD
5 mg	In stock	$ 43.00
10 mg	In stock	$ 74.00
25 mg	In stock	$ 163.00
50 mg	In stock	$ 278.00
100 mg	In stock	$ 488.00
1 mL * 10 mM (in DMSO)	In stock	$ 60.00

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Purity: 98.93%

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Storage & Solubility Information

Description	SB290157 trifluoroacetate is a potent and selective antagonist of C3a receptor(IC50 of 200 nM).
Targets&IC50	C3a:200 nM
In vitro	SB 290157 is a competitive antagonist of 125I-C3a radioligand binding to rat basophilic leukemia-2H3 cells expressing the human C3aR (RBL-C3aR, 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 (IC50s of 27.7 and 28 nM, respectively). SB 290157 is selective for the C3aR in that. 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 effectively inhibits neutrophil recruitment in a guinea pig model of LPS-induced airway neutrophilia and reduces paw edema in a rat model of adjuvant-induced arthritis. This antagonist demonstrates a capacity to decrease joint swelling, achieving approximately 50% inhibition at a concentration of 30 mg/kg, but only at the 3-hour mark. Additionally, it significantly lowers C3 levels at 3 hours post-administration, indicating complement consumption compared to naive mice. An increase in C3 activation correlates with the graded concentration of anti-OVA pAb, further showcasing its biological activity (1, 2).

Molecular Weight	526.51
Formula	C24H29F3N4O6
CAS No.	1140525-25-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (237.41 mM), Sonication is recommended.

References and Literature

1. Ames RS, et al. Identification of a selective nonpeptide antagonist of the anaphylatoxin C3areceptor that demonstrates antiinflammatory activity in animal models. J Immunol. 2001 May 15;166(10):6341-8. 2. Hutamekalin P, et al. Effect of the C3a-receptor antagonist SB 290157 on anti-OVA polyclonalantibody-induced arthritis. J Pharmacol Sci. 2010;112(1):56-63.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library NO PAINS Compound Library Immunology/Inflammation Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

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