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

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.

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JMV 7490

JMV 7490 Chemical Structure

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Description

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

 

In Vitro

[68Ga]Ga-JMV 7490 (0.1-500 nM; incubated at 4°C for 2 hours) binds to NTS1 on HT-29 cells, with a Kd of 14.61 nM and an NTS1/NTS2 selectivity of 44.4; [111In]In-JMV 7490 has a Kd of 77.47 nM against NTS1 and a selectivity of 6.5[1].
[68Ga]Ga-JMV 7490 exhibits complete ex vivo stability in human plasma, while [111In]In-JMV 7490 retains only 76% and 61% of intact peptide after 2 h and 4 h of ex vivo incubation, respectively[1].

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

Cell Viability 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.
In Vivo

[111In]In-JMV 7490 (12 MBq/200 pmol; intravenous injection) shows extremely low uptake in NTS1 -negative HEK 293T xenografts in male NMRI-Foxn1 nu/nu mice, whereas it effectively visualizes tumor sites in SPECT/CT imaging of HT-29 xenograft models [1].

MedChemExpress (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.
Molecular Weight

1362.73

Formula

C63H111N15O16Si

Sequence

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

Sequence Shortening

{DOTA}-{β-Ala}-KKKPYI-{TMSAla}

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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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.

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Product Name:
JMV 7490
Cat. No.:
HY-P11594
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