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SB290157 trifluoroacetate Complement System antagonist

Name: SB290157 trifluoroacetate
Brand: Selleck Chemicals
SKU: S8931
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S8931

SB290157 trifluoroacetate (SB 290157 TFA) is a potent, competitive and selective antagonist of C3a receptor (C3aR) with IC50 of 200 nM for RBL-C3aR.

Chemical Structure

Molecular Weight: 526.51

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Quality Control

Batch: S893101 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 99.69%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.69

Related Targets	PD-1/PD-L1 CXCR STING AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX
Other Complement System Products	Compstatin C5b-9 + C5b-8 Antibody [P24G22] C9 Antibody [F9K1] Phaseoloidin Lendalizumab (Anti-Complement C5) JR14a Pegcetacoplan acetate Danicopan Mannan Binding Lectin/MBL Antibody [M19P7] C1q Antibody [G8H3]

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (189.92 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
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.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	526.51	Formula	C₂₄H₂₉F₃N₄O₆	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1140525-25-2	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC=C(C=C1)C(COCC(=O)NC(CCCN=C(N)N)C(=O)O)C2=CC=CC=C2.C(=O)(C(F)(F)F)O

Mechanism of Action

Targets/IC₅₀/Ki	RBL-C3aR (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.
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/11342658/

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