1. MAPK/ERK Pathway
  2. MAP3K
  3. CS17919

CS17919 是一种强效、选择性且具有口服活性的 ASK1 抑制剂,IC50 为 22.52 nM。CS17919 具有抗炎和抗纤维化作用。CS17919 可用于研究代谢相关的肾脏和肝脏疾病。

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CS17919 Chemical Structure

CS17919 Chemical Structure

CAS No. : 2379346-41-3

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  • 生物活性

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生物活性

CS17919 is a potent, selective and orally active ASK1 inhibitor with an IC50 of 22.52 nM. CS17919 shows anti-inflammatory and antifibrotic effects. CS17919 can be used for the study of metabolic-related kidney and liver diseases[1].

IC50 & Target[1]

ASK1

22.52 nM (IC50)

体外研究
(In Vitro)

CS17919 (0.32-10 μM;72 小时) 为棕榈酸处理的 LO2 细胞提供有效保护[1]

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

Apoptosis Analysis[1]

Cell Line: L02 cells stimulated with 50 μM Palmitic acid (HY-N0830)
Concentration: 0.32 μM, 0.63 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time: 72 h
Result: Significantly prevented apoptosis at all doses.
体内研究
(In Vivo)

CS17919(10-60 mg/kg;口服;每日两次;持续 11 天)可改善 UUO 模型中的肾损伤和纤维化[1]
CS17919(50 mg/kg;口服;每日两次;持续 70 天)可缓解 DKD 模型中的肾小球硬化[1]
CS17919(20 mg/kg;口服;每日两次;持续 4 周)可改善 NASH 模型中的肝脏炎症和纤维化[1]
口服后 CS17919 在 C57BL/6J 中的药代动力学参数[1]
1.19

Parameters 20 mg/kg. p.o. 50 mg/kg. p.o.
AUC0–∞ (h·ng/mL) 23 113 ± 5898.47 58 795 ± 23 199.32
AUC0–t (h·ng/mL) 23 078 ± 5892.78 57 239 ± 20 606.29
Cmax (ng/mL) 4039 ± 646.90 5741 ± 1835
MRT0–∞ (h) 3.96 ± 0.91 6.43 ± 1.44
T1/2 (h) 2.20 ± 0.74 3.50 ± 1.86
Tmax (h) 1.50 ± 0.87 2.00 ± 0

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

Animal Model: Male C57BL/6J mice (6-8 weeks old) bearing unilateral ureteral obstruction model (UUO)[1]
Dosage: 10 mg/kg, 60 mg/kg (0.2% CMC-Na + 0.1% Tween-80)
Administration: po; twice daily; for 11 days
Result: Preserved kidney function and showed a non-significant tendency to alleviate kidney fibrosis.
Animal Model: Male neonatal mice bearing chronic kidney disease (CKD)[1]
Dosage: 50 mg/kg
Administration: po; twice daily; for 70 days
Result: Significantly improved serum creatinine and glomerular sclerosis.
Animal Model: Male C57BL/6J mice (6-8 weeks) bearing non-alcoholic steatohepatitis (NASH)[1]
Dosage: 20 mg/kg
Administration: po; twice daily; for 4 weeks
Result: Significantly improved liver inflammation and substantially reduced liver fibrosis.
分子量

476.43

Formula

C22H20F4N6O2

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

The molarity calculator equation

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

质量   浓度   体积   分子量 *
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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)
× = ×
C1   V1   C2   V2
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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CS17919
目录号:
HY-163752
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