| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
[68Ga]Ga-JMV 7490 (0.1-500 nM; incubation at 4°C for 2 hours) binds to NTS1 on HT-29 cells with a Kd value of 14.61 nM and an NTS1/NTS2 selectivity of 44.4; [111In]In-JMV 7490 has a Kd value of 77.47 nM and a selectivity of 6.5 for NTS1[1]. [68Ga]Ga-JMV 7490 has complete in vitro stability in human plasma, while [111In]In-JMV 7490 retains only 76% and 61% of the intact peptide after incubation for 2 hours and 4 hours, respectively[1].
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|---|---|
| ln Vivo |
[111In]In-JMV 7490 (12 MBq/200 pmol; intravenous injection) was taken up very low in NTS1-negative HEK 293T xenografts in male NMRI-Foxn1 nu/nu mice, but it was effective in displaying tumor sites in SPECT/CT imaging of the HT-29 xenograft model [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: HT-29 cells Tested Concentrations: 0.1, 1, 10, 100, 500 nM Incubation Duration: 2 hours Experimental Results: The Kd value of [68Ga]Ga-JMV 7490 for NTS1 was 14.61 nM, and the NTS1/NTS2 selectivity was 44.4. [111In]In-JMV 7490 had a lower affinity for NTS1, with a Kd value of 77.47 nM and an NTS1/NTS2 selectivity of 6.5. The affinity of nat/68Ga-labeled JMV 7490 for NTS1 was 19.20 nM. |
| Animal Protocol |
Animal/Disease Models:NMRI-Foxn1 nu/nu (male, 7 weeks old) [1]
Doses: 12 MBq/200 pmol Route of Administration: Intravenous Injection Experimental Results: Tumor uptake reached 5.86 ± 0.86 %ID/g tissue 1 hour after injection; tumor uptake reached 3.65 ± 0.29 %ID/g tissue 4 hours after injection; renal uptake was 65.29 ± 3.08 %ID/g tissue 1 hour after injection and 77.07 ± 7.97 %ID/g tissue 4 hours after injection. |
| References |
| Molecular Formula |
C63H111N15O16SI
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|---|---|
| Molecular Weight |
1362.73
|
| Sequence |
{DOTA}-{β-Ala}-Lys-Lys-Lys-Pro-Tyr-Ile-{TMSAla}{DOTA}-{β-Ala}-KKKPYI-{TMSAla}
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| SequenceShortening |
{DOTA}-{β-Ala}-KKKPYI-{TMSAla}
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| Appearance |
Typically exists as solids at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7338 mL | 3.6691 mL | 7.3382 mL | |
| 5 mM | 0.1468 mL | 0.7338 mL | 1.4676 mL | |
| 10 mM | 0.0734 mL | 0.3669 mL | 0.7338 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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