2. GPCR/G Protein Neuronal Signaling
  3. Neurotensin Receptor
  4. JMV 7490

JMV 7490 是一种高效和高亲水性的神经降压素受体 NTS1 探针，可被 68Ga、111In 成功标记。JMV 7490 可作为外排抑制剂，降低其在 NTS1 阳性癌细胞中的外排；同时也是一种内化诱导剂，可高效且持续地被 NTS1 阳性癌细胞内化。经 111In 放射性标记的 JMV 7490 在裸鼠的 NTS1 阳性异种移植物中表现出持续摄取，而在 NTS1 阴性异种移植物中无显著摄取。JMV 7490 可用于 NTS1 阳性肿瘤的体内示踪应用，并支持结直肠癌的相关研究。

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JMV 7490

JMV 7490 Chemical Structure

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JMV 7490 相关抗体

Top Publications Citing Use of Products

查看 Neurotensin Receptor 亚型特异性产品:

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NTR1 NTR2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JMV 7490 is a highly potent and highly hydrophilic neurotensin receptor NTS1 probe that can be successfully labeled with 68Ga and 111In. JMV 7490 acts as an efflux inhibitor to reduce its efflux in NTS1-positive cancer cells; it also serves as an internalization inducer and is efficiently and continuously internalized by NTS1-positive cancer cells. 111In-radiolabeled JMV 7490 shows persistent uptake in NTS1-positive xenografts in nude mice, but no significant uptake in NTS1-negative xenografts. JMV 7490 can be used for in vivo tracer applications of NTS1-positive tumors and supports related research on colorectal cancer[1].

IC50 & Target

NTR1

 

体外研究
(In Vitro)

[68Ga]Ga-JMV 7490 (0.1-500 nM；4°C 孵育 2 小时) 可与 HT-29 细胞上的 NTS1 结合，其 Kd 为 14.61 nM，NTS1/NTS2 选择性为 44.4；[111In]In-JMV 7490 对 NTS1 的 Kd 值为 77.47 nM，选择性为 6.5[1]。
[68Ga]Ga-JMV 7490 在人血浆中具有完全的离体稳定性，而 [111In]In-JMV 7490 在离体培养 2 小时和 4 小时时，只分别保留 76% 和 61% 的完整肽段[1]。

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

JMV 7490 相关抗体:

Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell Invasion AssayCell Migration Assay Real Time qPCRELISA Assay[1]

Cell Line: HT-29 cells
Concentration: 0.1、1、10、100、500 nM
Incubation Time: 2 h
Result: [68Ga]Ga-JMV 7490 exhibited a Kd value of 14.61 nM for NTS1 and a NTS1/NTS2 selectivity of 44.4. [111In]In-JMV 7490 showed a lower affinity for NTS1 with a Kd value of 77.47 nM and a NTS1/NTS2 selectivity of 6.5.
The nat/68Ga-labeled JMV 7490 had an affinity value of 19.20 nM for NTS1.
体内研究
(In Vivo)

[111In]In-JMV 7490 (12 MBq/200 pmol；静脉注射) 在雄性 NMRI-Foxn1 nu/nu 小鼠的 NTS1 阴性 HEK 293T 异种移植瘤中的摄取量极低；而在 HT-29 异种移植模型的 SPECT/CT 成像中，可有效显示肿瘤位置 [1]。

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

Animal Model: NMRI-Foxn1 nu/nu (male, 7 weeks old)[1]
Dosage: 12 MBq/200 pmol
Administration: i.v.
Result: Reached tumor uptake of 5.86 ± 0.86 %ID/g tissue at 1 h post-injection; reached tumor uptake of 3.65 ± 0.29 %ID/g tissue at 4 h post-injection; showed high kidney uptake of 65.29 ± 3.08 %ID/g tissue at 1 h and 77.07 ± 7.97 %ID/g tissue at 4 h post-injection.
分子量

1362.73

Formula

C63H111N15O16Si
Sequence

{DOTA}-{β-Ala}-Lys-Lys-Lys-Pro-Tyr-Ile-{TMSAla}
Sequence Shortening

{DOTA}-{β-Ala}-KKKPYI-{TMSAla}
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

JMV 7490 相关分类

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

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× = ×
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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.

Keywords:

JMV 7490JMV7490JMV-7490Neurotensin Receptornude miceNeurotensin-receptor-1NTS?-positive cancer cellsHEK 293T xenograftshuman blood plasmaNTS?colorectal cancerNTS?-negative xenograftsHT-29 cellsInhibitorinhibitorinhibit

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