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• 產(chǎn)品描述： SB290157 trifluoroacetate (SB 290157 TFA) 是一種有效的 C3a receptor (C3aR) 的競(jìng)爭(zhēng)性、選擇性的拮抗劑，對(duì)RBL-C3aR的IC50值為200 nM

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

• 體外研究：
  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.

• 體內(nèi)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.

• 細(xì)胞實(shí)驗(yàn)： 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.

• 動(dòng)物實(shí)驗(yàn)： 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

• 參考文獻(xiàn)：
  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

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	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

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號(hào)：

本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

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