SB290157 trifluoroacetate

製品コードS8931 バッチS893101

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
化学式

C24H29F3N4O6

分子量 526.51 CAS No. 1140525-25-2
Solubility (25°C)* 体外 DMSO 100 mg/mL (189.92 mM)
Ethanol 100 mg/mL (189.92 mM)
Water Insoluble
体内 (毎回新しく調製した物を用意してください)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml 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. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 SB290157 trifluoroacetate (SB 290157 TFA) is a potent, competitive and selective antagonist of C3a receptor (C3aR) with IC50 of 200 nM for RBL-C3aR.
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.[1]

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.[1]

生物活性

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

プロトコル(参考用のみ)

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

Cntnap4 partial deficiency exacerbates α-synuclein pathology through astrocyte-microglia C3-C3aR pathway [ Cell Death Dis, 2023, 14(4):285] PubMed: 37087484
Complement C3a receptor inactivation attenuates retinal degeneration induced by oxidative damage [ Front Neurosci, 2022, 16:951491] PubMed: 36110094
Astrocyte-microglia interaction through C3/C3aR pathway modulates neuropathic pain in rats model of chronic constriction injury [ Mol Pain, 2022, 18:17448069221140532] PubMed: 36341694

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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