2. Neuronal Signaling Immunology/Inflammation
  3. Amyloid-β CD47
  4. CL121

CL121 是一种 Glutaminyl Cyclase 抑制剂，对人 sQC 的 IC50 为 0.07 μM，对人 gQC 的 IC50 为 0.54 μM。CL121 可降低癌细胞表面焦谷氨酸 (pE) 修饰的 CD47 水平。CL121 对三阴性乳腺癌显示出抗肿瘤活性。

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CL121

CL121 Chemical Structure

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2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

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CL121 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CL121 is a Glutaminyl Cyclase inhibitor with an IC50 of 0.07 μM against human sQC and an IC50 of 0.54 μM against human gQC. CL121 reduces the level of pyroglutamate (pE)-modified CD47 on the surface of cancer cells. CL121 exhibits anti-tumor activity against triple-negative breast cancer[1].

体外研究
(In Vitro)

CL121 可强效抑制纯化的人源 sQC，其 IC50 为 0.07 μM；同时可抑制人源 gQC，其 IC50 为 0.54 μM[1]。
CL121 (10-40 μM; 72 h) 可呈剂量依赖性降低 MDA-MB-231 细胞表面的 pE-CD47 修饰水平，且不影响 CD47 的总表达量[1]。
CL121 (10-40 μM) 可增强巨噬细胞介导的 KYSE30 细胞吞噬作用[1]。

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

CL121 相关抗体:

Cell Viability Assay[1]

Cell Line: MDA-MB-231, KYSE30, MCF-10A, Het1A
Concentration: 50 μM
Incubation Time: 72 h
Result: Resulted in cell viability above 75% across all tested cell lines.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Tmax T1/2 CLz/F Vz/F AUC0-∞
Rat[1] 10 mg/kg i.p. 4976 ± 889 μg/L 0.25 h 2.48 ± 2.15 h 1.9 ± 0.4 L/h/kg 6 ± 3.84 L/kg 5431 ± 1253 μg/L·h
体内研究
(In Vivo)

CL121 (10-20 mg/kg；腹腔注射；每日一次；连续 3 周) 在小鼠 MDA-MB-231 异种移植模型中表现出显著的抗肿瘤活性[1]。

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

Animal Model: BALB/c nude (female)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: i.p.; daily; 3 weeks
Result: Reduced average tumor volume to 154 mm3 (from 227 mm3 in controls) and average tumor weight to 129.05 mg (from 191.49 mg in controls) at 10 mg/kg, with statistically significant tumor weight reduction (P < 0.01).
Reduced average tumor volume to 195 mm3 and average tumor weight to 173.69 mg at 20 mg/kg, with no statistically significant difference compared to controls.
Significantly reduced intratumoral pE-CD47 expression relative to controls at both doses, with 10 mg/kg showing statistically significant reduction (P < 0.05) and 20 mg/kg showing stronger statistically significant reduction (P < 0.01).
Showed no significant differences in body weight between treatment groups and controls, indicating low systemic toxicity.
分子量

351.40

Formula

C20H21N3O3
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

CL121 相关分类

  • 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 *
= × ×

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.

Keywords:

CL121CL 121CL-121Amyloid-βCD47β-amyloid peptideAβAbetaCluster of Differentiation 47MER6OA3human sQCmouse xenograft tumor modelspyroglutamate (pE)-CD47glutaminyl cyclaseHet1AKYSE30 cellsmacrophage-mediated phagocytosishuman gQCMCF-10AMDA-MB-231 cellsInhibitorinhibitorinhibit

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