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• 产品描述： SB290157 trifluoroacetate (SB 290157 TFA) 是一种有效的 C3a receptor (C3aR) 的竞争性、选择性的拮抗剂，对RBL-C3aR的IC50值为200 nM

• 靶点： RBL-C3aR(Cell-free assay):200 nM;ComplementSystem

• 体外研究：
  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.

• 体内研究：
  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.

• 细胞实验： 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.

• 动物实验： 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

• 参考文献：
  1. R S Ames, et al. Identification of a selective nonpeptide antagonist of the anaphylatoxin C3a receptor that demonstrates antiinflammatory activity in animal models. J Immunol. 2001 May 15;166(10):6341-8.

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.899 ml	9.497 ml	18.993 ml
  5 mM	0.38 ml	1.899 ml	3.799 ml
  10 mM	0.19 ml	0.95 ml	1.899 ml
  50 mM	0.038 ml	0.19 ml	0.38 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *