1. GPCR/G Protein
  2. Leukotriene Receptor
  3. SM-15178

SM-15178 是一种强效、口服活性且选择性白三烯 B4(LTB4) 受体拮抗剂,其 IC50 为 0.30 μM。SM-15178 能显著减轻 LTB4 (HY-107608) 诱导的小鼠皮肤中性粒细胞浸润以及豚鼠的支气管收缩。SM-15178 在多种炎症动物模型中表现出显著的抗炎效果。SM-15178 可用于慢性炎症性疾病 (如炎症性肠病、银屑病和哮喘) 的研究。

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SM-15178

SM-15178 Chemical Structure

CAS No. : 146461-98-5

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查看 Leukotriene Receptor 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SM-15178 is a potent, orally active and selective leukotriene B4 (LTB4) receptor antagonist with an IC50 of 0.30 μM. SM-15178 attenuates LTB4 (HY-107608)-induced neutrophil accumulation in mouse skin and bronchoconstriction in guinea pigs. SM-15178 emonstrates significant anti-inflammatory efficacy across multiple animal models of inflammation. SM-15178 can be used for the research of chronic inflammatory diseases such as inflammatory bowel disease, psoriasis, and asthma[1][2][3].

IC50 & Target

LTB4

0.30 μM (IC50)

体外研究
(In Vitro)

SM-15178 (不同浓度;30 min) 可剂量依赖性地抑制 LTB₄ 与人中性粒细胞的结合 (IC₅₀ = 0.30 μM) [3]
SM-15178 (最高 30 μM;15-90 分钟) 可抑制 LTB4 诱导的多种细胞类型的趋化作用 (IC50 = 0.52-0.72 μM) [3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

SM-15178 (5 mg/kg;静脉注射;单次给药) 可减少小鼠皮肤中 LTB4诱导的中性粒细胞积聚[1]
SM-15178 (5 mg/kg;静脉注射;LTB4 前 2-30 min,或 40 mg/kg;口服;LTB4前 60 min) 可显著抑制豚鼠中 LTB4 诱导的支气管收缩[2]
SM-15178 (20-40 mg/kg;口服;单次给药) 可抑制豚鼠中 LTB4 诱导的短暂性白细胞减少症[3]
SM-15178 (5-100 mg/kg;口服;单次给药) 可抑小鼠中花生四烯酸诱导的中性粒细胞浸润 [3]
SM-15178 (10-100 mg/kg;口服;在 SRBC 前 1 天或前 1 小时) 可抑制小鼠由绵羊红细胞 (SRBC) 诱导的足肿胀[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6N mice induced by LTB4[1]
Dosage: 5 mg/kg
Administration: i.v.; single dose
Result: Significantly reduced LTB4-induced neutrophil accumulation by 70.3%.
Animal Model: Guinea pigs challenged with LTB₄[2]
Dosage: 5 mg/kg (i.v.); 40 mg/kg (p.o.)
Administration: i.v.; 2, 10, or 30 min pre-LTB₄; p.o.; 60 min pre-LTB₄
Result: Showed potent inhibitory activity against LTB₄-induced bronchoconstriction at all dosages.
Animal Model: Male Hartley Guinea pigs (400-450 g) intravenously injected with LTB₄[3]
Dosage: 20, 40 mg/kg
Administration: p.o.; single dose; 1 h pre-LTB4
Result: Significantly suppressed LTB₄-induced transient leukopenia and LTB₄-induced bronchoconstriction.
Animal Model: Male BALB/c (20-30 g) topically applied with Arachidonic Acid[3]
Dosage: 5, 25, 50, 100 mg/kg
Administration: p.o.; single dose
Result: Suppressed arachidonic acid-induced increases in myeloperoxidase (MPO) levels in a dose-dependent manner.
Animal Model: Male BALB/c (25-30 g) injected with SRBC[3]
Dosage: 10, 25, 50, 100 mg/kg
Administration: p.o.; one day or 1 hour before SRBC
Result: Inhibited Arthus reaction-induced paw edema in a dose-dependent manner with a minimum effective dose of 25 mg/kg.
分子量

414.46

Formula

C22H26N2O6

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
SM-15178
目录号:
HY-180411
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