2. Immunology/Inflammation Metabolic Enzyme/Protease
  3. PD-1/PD-L1 NAMPT
  4. PD-L1/Nampt-IN-1

PD-L1/Nampt-IN-1 是一种口服有效的抑制剂，同时靶向 PD-L1 和 NAMPT (烟酰胺磷酸核糖基转移酶)，其 IC50 值为 63 nM 和 582 nM。PD-L1/Nampt-IN-1 显示出跨物种亲和力，对 hPD-L1 和 mPD-L1 的 KD 值分别为 52.6 和 49.1 nM。PD-L1/Nampt-IN-1 通过激活肿瘤免疫微环境，有效抑制了肿瘤生长。PD-L1/Nampt-IN-1 可用于黑色素瘤的研究。

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PD-L1/Nampt-IN-1

PD-L1/Nampt-IN-1 Chemical Structure

CAS No. : 3054043-85-2

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PD-L1/Nampt-IN-1 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

PD-L1/Nampt-IN-1 is an orally active inhibitor that simultaneously target PD-L1 and NAMPT (nicotinamide phosphoribosyltransferase) with IC50s value of 63 nM and 582 nM. PD-L1/Nampt-IN-1 demonstrates cross-species affinity with comparable KD values for hPD-L1 (52.6 nM) and mPD-L1 (49.1 nM), respectively. PD-L1/Nampt-IN-1 effectively inhibits tumor growth by activating the tumor immune microenvironment. PD-L1/Nampt-IN-1 can be used for the study of melanoma[1].

体外研究
(In Vitro)

PD-L1/Nampt-IN-1 (Compound T8) (0.5-5 μM) 可以剂量依赖性抑制 PD-1/PD-L1 相互作用，在 5 μM 时抑制率达到了 76.3%[1]。

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

PD-L1/Nampt-IN-1 相关抗体:
体内研究
(In Vivo)

PD-L1/Nampt-IN-1 (Compound T8) (50 mg/kg, p.o., 共 14 天) 在 B16-F10 肿瘤小鼠模型中显著增强了肿瘤生长抑制效果，而这归因于肿瘤免疫微环境的激活[1]。
PD-L1/Nampt-IN-1 在肿瘤中富集 (1133.6 ng/mL, 8 h)，且穿透血脑屏障 (81.86 ng/mL, 1 h) [1]。

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

Animal Model: B16-F10 tumor model established in 6–8 weeks old male C57BL/6 mice[1]
Dosage: 50 mg/kg
Administration: Oral administration (p.o.), for 14 days
Result: Effectively inhibited melanoma tumor growth with a TGI of 40.1%.
Shows normal fluctuations in mouse body weight during treatment.
Increased the percentage of CD3+, CD3+CD4+, and CD3+CD8+.
No morphological aberration in organ tissues.
分子量

452.55

Formula

C28H28N4O2
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

PD-L1/Nampt-IN-1 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:

PD-L1/Nampt-IN-13054043-85-2PD-1/PD-L1NAMPTPD-1/Programmed death-ligand 1Nicotinamide phosphoribosyl transferasePBEFVisfatinpre-B cell-enhancing factorPre-B cell colony enhancing factorB16-F10 cellsMelanomamice modelOral bioavailabilityDual inhibitorInhibitorinhibitorinhibit

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