SB 290157 (trifluoroacetate salt)
目录号 : GC11800
SB 290157（三氟乙酸盐）用作选择性非肽类 C3aR 拮抗剂。
Cas No.:1140525-25-2
Sample solution is provided at 25 µL, 10mM.
SB 290157 (trifluoroacetate salt) is used as a selective nonpeptide C3aR antagonist. SB 290157 was a selective antagonist for rat basophilic leukemia cells expressing the human C3aR (IC50 of 200 nM). Antagonism by SB 290157 was not only limited to the human C3aR (IC50 of 12 nM), it also inhibited C3a-induced Ca2+ mobilization of cells expressing the mouse and guinea-pig C3aR (IC50 of 7 and 30 nM, respectively). [1].
SB 290157 (trifluoroacetate salt) (0.1 μM) significantly increased the abundance of SM22α mRNA and decreased the abundance of osteopontin mRNA in VSMCs from SHR rats, but these did not occur in cells from WKY rats [2]. C3a overexpression markedly altered the distribution of vinculin in human podocyte line cells, C3aR inhibition with 1 μM SB 290157 blocked this alteration [3]. SB 290157(0.1-10μM) inhibited C3aR internalization induced by 10 nM C3a in a concentration-dependent manner. In the presence of >1 μM concentrations of SB 290157 the internalization of the C3aR induced by C3a was reduced by ～50% [4].
SB 290157 (trifluoroacetate salt) (1 mg/kg) treatment reduced microglial activation and cognitive deficits in lipopolysaccharide (LPS) induced mice. SB 290157 (trifluoroacetate salt) attenuated LPS-induced hippocampal neuroinflammation and inhibitory synapse related protein loss, contributing to improved cognitive function of mice [5]. SB 290157 (trifluoroacetate salt) was involved in the suppression of anti-OVA pAb-induced arthritis, injection of SB 290157 at concentrations of 30 mg/kg, SB 290157 was able to reduce joint swelling at 3 h, and inhibit about 50% inhibition of joint swelling [6].
References:
[1]. Ames R S, Lee D, Foley J J, et al. Identification of a selective nonpeptide antagonist of the anaphylatoxin C3a receptor that demonstrates antiinflammatory activity in animal models[J]. The Journal of Immunology, 2001, 166(10): 6341-6348.
[2]. Han Y, Fukuda N, Ueno T, et al. Role of complement 3a in the synthetic phenotype and angiotensin II-production in vascular smooth muscle cells from spontaneously hypertensive rats[J]. American journal of hypertension, 2012, 25(3): 284-289.
[3]. Zheng J M, Wang S S, Tian X, et al. Sustained activation of C3aR in a human podocyte line impairs the morphological maturation of the cells[J]. Molecular medicine reports, 2020, 22(6): 5326-5338.
[4]. Ames R S, Lee D, Foley J J, et al. Identification of a selective nonpeptide antagonist of the anaphylatoxin C3a receptor that demonstrates antiinflammatory activity in animal models[J]. The Journal of Immunology, 2001, 166(10): 6341-6348.
[5]. Li S, Li B, Zhang L, et al. A complement-microglial axis driving inhibitory synapse related protein loss might contribute to systemic inflammation-induced cognitive impairment[J]. International Immunopharmacology, 2020, 87: 106814.
[6]. Hutamekalin P, Takeda K, Tani M, et al. Effect of the C3a-receptor antagonist SB 290157 on anti-OVA polyclonal antibody-induced arthritis[J]. Journal of pharmacological sciences, 2010, 112(1): 56-63.
SB 290157（三氟乙酸盐）用作选择性非肽类 C3aR 拮抗剂。 SB 290157 是表达人 C3aR 的大鼠嗜碱性白血病细胞的选择性拮抗剂（IC50 为 200 nM）。 SB 290157 的拮抗作用不仅限于人 C3aR（IC50 为 12 nM）,它还抑制 C3a 诱导的表达小鼠和豚鼠 C3aR 的细胞的 Ca2+ 动员（IC50 分别为 7 和 30 nM）。 [1].
SB 290157（三氟乙酸盐）(0.1 μM) 可显着增加 SHR 大鼠 VSMC 中 SM22α mRNA 的丰度并降低骨桥蛋白 mRNA 的丰度,但这些并未发生在 WKY 大鼠的细胞中 [2]。 C3a 过表达显着改变了人足细胞系细胞中纽蛋白的分布,用 1 μM SB 290157 抑制 C3aR 可阻断这种改变[3]。 SB 290157(0.1-10μM) 以浓度依赖性方式抑制由 10 nM C3a 诱导的 C3aR 内化。在 >1 μM 浓度的 SB 290157 存在下,C3a 诱导的 C3aR 内化减少了 ~ 50% [4]。
SB 290157（三氟乙酸盐）(1 mg/kg) 处理可减少脂多糖 (LPS) 诱导的小鼠的小胶质细胞活化和认知缺陷。 SB 290157（三氟乙酸盐）可减轻 LPS 诱导的海马神经炎症和抑制性突触相关蛋白丢失,有助于改善小鼠的认知功能[5]。 SB 290157（三氟乙酸盐）参与抗OVA pAb诱导的关节炎的抑制,注射浓度为30 mg/kg的SB 290157,SB 290157能够在3 h时减轻关节肿胀,并抑制约50%的抑制作用关节肿胀 [6].
| Cell experiment [1]: | |
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Cell lines |
Vascular smooth muscle cells (VSMCs) from SHR and WKY rats |
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Preparation Method |
VSMCs were inoculated and grown into DMEM containing 5% calf serum in the absence or presence of 0.1µmol/l SB 290157 (trifluoroacetate salt) in 24-well culture dishes at a density of 105 cells/cm3. Cells were trypsinized with 0.05% trypsin at 24, 48, and 72 h after inoculation, and cell numbers were counted in a Coulter counter. |
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Reaction Conditions |
0.1µmol/l for 24, 28, 72 hours |
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Applications |
SB290157 significantly inhibited the increase in the number of VSMCs in SHR rats, whereas SB 290157 (trifluoroacetate salt) did not affect the increase in the number of cells in WKY rats. |
| Animal experiment [2]: | |
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Animal models |
C57BL/6JNarl (B6) mice |
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Preparation Method |
Stock solution of SB 290157 was prepared by dissolving the compound in a minimal volume of sterile DMSO (100 mg.ml-1). SB 290157 (trifluoroacetate salt) was further diluted with 1× sterile PBS for injection to a final dose of 20 mg.kg-1 body weight in 100 µl volume. In the photothrombotic stroke model, SB 290157 (trifluoroacetate salt) or vehicle was injected intraperitoneally 1 hr after stroke while in the embolic clot middle cerebral artery occlusion model, it was intravenously injected 2 hr post-stroke. |
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Dosage form |
Intraperitoneal or intravenous injection, 20 mg.kg-1 |
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Applications |
SB 290157 (trifluoroacetate salt) treatment 1 hr after photothrombotic stroke significantly improved neurofunctional outcome assessed by the adhesive tape removal and corner turn tests. SB 290157 (trifluoroacetate salt) significantly reduced the infarct volume relative to vehicle-treated animals at 48 hr post-photothrombotic. |
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References: [1]: Han Y, Fukuda N, Ueno T, et al. Role of complement 3a in the synthetic phenotype and angiotensin II-production in vascular smooth muscle cells from spontaneously hypertensive rats[J]. American journal of hypertension, 2012, 25(3): 284-289. | |
| Cas No. | 1140525-25-2 | SDF | |
| 化学名 | N2-[2-(2,2-diphenylethoxy)acetyl]-L-arginine, 2,2,2-trifluoroacetate | ||
| Canonical SMILES | O=C(N[C@H](C(O)=O)CCCNC(N)=N)COCC(C1=CC=CC=C1)C2=CC=CC=C2.FC(F)(C(O)=O)F | ||
| 分子式 | C22H28N4O4 • CF3COOH | 分子量 | 526.5 |
| 溶解度 | ≤30mg/ml in ethanol;20mg/ml in DMSO;25mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8993 mL | 9.4967 mL | 18.9934 mL |
| 5 mM | 0.3799 mL | 1.8993 mL | 3.7987 mL |
| 10 mM | 0.1899 mL | 0.9497 mL | 1.8993 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
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2.
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