2. Immunology/Inflammation Stem Cell/Wnt MAPK/ERK Pathway Membrane Transporter/Ion Channel
  3. FAP ERK GLUT
  4. BR103354

BR103354 是一种口服有效的、选择性的成纤维细胞活化蛋白 (FAP) 抑制剂，对 hFAP 的 IC50 值为 14 nM。BR103354 恢复 hFGF21 与 FAP 共处理降低的磷酸化 ERK 和 Glut1 水平，降低非空腹血糖浓度，改善葡萄糖耐量，并减少肝脏甘油三酯含量。BR103354 可改善肝脂肪变性和肝纤维化。BR103354 可用于 2 型糖尿病和非酒精性脂肪性肝炎的研究。

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BR103354

BR103354 Chemical Structure

CAS No. : 2505339-87-5

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BR103354 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BR103354 is an orally active, selective fibroblast activation protein (FAP) inhibitor with an IC50 value of 14 nM against hFAP. BR103354 restores the levels of phosphorylated ERK and Glut1 that are reduced by co-treatment with hFGF21 and FAP, decreases non-fasting blood glucose concentrations, improves glucose tolerance, and reduces hepatic triglyceride content. BR103354 ameliorates hepatic steatosis and hepatic fibrosis. BR103354 can be used in the research of type 2 diabetes and non-alcoholic steatohepatitis[1].

IC50 & Target[1]

GLUT1

 

体外研究
(In Vitro)

BR103354 (0.03 nM-100 μM; 60 min) 可强效且选择性地抑制纯化的 hFAP，其 IC50 为 14 nM[1]。
BR103354 在小鼠、食蟹猴和人源样本中以相近效力抑制血清 FAP 活性，其 IC50 值约为 27 至 31 nM[1]。

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

BR103354 相关抗体:

Western Blot Analysis[1]

Cell Line: Differentiated 3T3/L1 adipocytes
Concentration: 5 μM
Incubation Time: 2 h (pre-incubation of hFGF21 with FAP; then added to cells)
Result: Restored phosphorylated ERK and Glut1 levels that had been reduced by co-treatment of hFGF21 with FAP, matching levels observed with hFGF21 treatment alone.
药代动力学
(Parmacokinetics)
Species Dose Route Tmax Cmax T1/2 Bioavailability
Mice[1] 1 mg/kg p.o. 0.5 h 2.3 μg/mL 1.2 h 48.4 %
Mice[1] 5 mg/kg p.o. 0.5 h 7.2 μg/mL 1.1 h 48.4 %
Mice[1] 10 mg/kg p.o. 0.5 h 19.2 μg/mL 1.2 h 48.4 %
Mice[1] 100 mg/kg p.o. 1 h 66.0 μg/mL 4.0 h 48.4 %
Mice[1] 200 mg/kg p.o. 1 h 122.5 μg/mL 3.8 h 48.4 %
Rat[1] 10 mg/kg p.o. 1.1 h 4.4 μg/mL 3.5 h /
Monkey[1] 10 mg/kg i.n. 2.3 h 0.42 μg/mL 1.3 h /
Monkey[1] 30 mg/kg i.n. 2.3 h 2.0 μg/mL 2.8 h /
体内研究
(In Vivo)

BR103354 (20-50 mg/kg；口服) 可使 ob/ob 小鼠的非空腹血糖 AUC 降低 40%-45%，并能在长达 9 小时内抑制 FAP 活性超过 70%[1]。
BR103354 (20-50 mg/kg；口服；每日 1 次；连续 4 周) 可降低 ob/ob 小鼠的非空腹血糖，抑制 FAP 活性达 ≥80%，使血清 FGF21 水平升高约 1.4 倍，同时改善其胰岛素抵抗、葡萄糖耐量及肝脏脂肪变性[1]。
BR103354 (50 mg/kg；鼻内给予) 可抑制 FAP 活性达 65%-83%，并使正常食蟹猴体内完整 FGF21 水平升高 1.5-3.5 倍[1]。
BR103354 (10-30 mg/kg；口服；每日 1 次；连续 10 周) 可抑制 FAP 活性，使血清 FGF21 水平升高 1.5-1.9 倍，降低肝酶及代谢生物标志物水平，并改善 CDAHFD 诱导的 NASH 小鼠的肝脂肪变性与纤维化[1]。

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

Animal Model: ob/ob (8-week-old male; spontaneous obese, diabetic model)[1]
Dosage: 20 mg/kg; 50 mg/kg
Administration: p.o.; single dose
Result: Reduced average nonfasting blood glucose to 178 mg/dL (20 mg/kg group) and 154 mg/dL (50 mg/kg group) at 3 hours post-administration.
Decreased blood glucose AUC by 40-45% relative to control.
Inhibited FAP activity by more than 70% at 1 hour post-administration, with inhibition maintained up to 9 hours.
Elevated plasma intact hFGF21 levels until 3 hours post-administration, then dropped below 10 ng/mL by 6 hours.
Animal Model: ob/ob (8-week-old male; spontaneous obese, diabetic model)[1]
Dosage: 20 mg/kg; 50 mg/kg
Administration: p.o.; once daily; 4 weeks
Result: Significantly reduced nonfasting blood glucose levels starting at week 2 (P<0.01) and further reduced at week 3 (P<0.001) relative to vehicle.
Inhibited FAP activity by at least 80% at week 4 relative to vehicle.
Increased serum total FGF21 levels by approximately 1.4-fold at week 4.
Showed significantly improved glucose tolerance (reduced OGTT AUC) in the 50 mg/kg group.
Significantly reduced fasting body weight, liver weight, fasting blood glucose, insulin levels, and HOMA-IR relative to vehicle.
Significantly reduced serum ALT, AST, and total cholesterol levels; serum TG and NEFA levels were unaltered.
Decreased liver TG content, with reduced Oil Red O stained area relative to vehicle.
Reduced mRNA expression of lipogenesis/steatosis-related genes, and increased fatty acid oxidation-related genes (MCAD, PPARα) in liver.
Elevated white adipose tissue adiponectin mRNA expression.
Increased ERK phosphorylation in white adipose tissue relative to vehicle.
Animal Model: C57BL/6J (5-week-old male; NASH induced by CDAHFD feeding for 4 weeks prior to treatment)[1]
Dosage: 10 mg/kg; 30 mg/kg
Administration: p.o.; once daily; 10 weeks
Result: Inhibited FAP activity in a dose-dependent manner relative to vehicle.
Increased serum FGF21 levels by 1.5-1.9-fold in treatment groups.
Reduced plasma ALT, AST, total cholesterol, TG, and glucose levels relative to vehicle.
Significantly reduced steatosis scores and Picrosirius red staining (fibrosis) relative to vehicle.
分子量

415.42

Formula

C19H15F2N5O2S
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

BR103354 相关分类

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  • 稀释计算器

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  • 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.

Keywords:

BR1033542505339-87-5BR 103354BR-103354FAPERKGLUTFibroblast activation protein Extracellular signal regulated kinasesGlucose transporterprolyl oligopeptidasehuman FAPfibroblast activation proteinhERGdipeptidyl peptidase-related enzymesnon-alcoholic steatohepatitishuman fibroblast growth factor 21type 2 diabetesmouse FAPmonkey FAPInhibitorinhibitorinhibit

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