| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
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| 50mg | |||
| 100mg |
| Targets |
HYNIC-PSMA targets prostate-specific membrane antigen (PSMA). PSMA is a transmembrane protein that is significantly overexpressed on the surface of prostate cancer cells. The HYNIC moiety serves as a chelator to attach radioactive isotopes, such as ⁹⁹ᵐTc or ¹⁸⁸Re, to the PSMA-targeting peptide. This allows for the targeted delivery of radioisotopes to PSMA-expressing tumors for imaging or therapy.
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|---|---|
| ln Vitro |
In nuclear medicine, drag isotopes combined with HYNIC-PSMA ligands can produce non-invasive effects on the standoff gun response (PSMA). Moreover, over-expressed PSMA on zombie corpses may be dragged to identify and emphasize malignant lesions [1].
In vitro, HYNIC-PSMA is used to study the binding and internalization of PSMA-targeted ligands in prostate cancer cells. The compound's specificity for PSMA is confirmed by competitive binding assays using PSMA-expressing cells. Cellular uptake experiments demonstrate the compound's ability to bind to PSMA and be internalized by the cells. These in vitro activities support its use in prostate cancer research and radiopharmaceutical development. |
| ln Vivo |
In vivo, HYNIC-PSMA can be used for the synthesis and research of Radionuclide-Drug Conjugates (RDCs). When labeled with a radioisotope such as ⁹⁹ᵐTc, it can be used for SPECT imaging of prostate cancer. ¹⁸⁸Re-labeled HYNIC-PSMA has been used for targeted radiotherapy. However, specific published in vivo studies for HYNIC-PSMA are not detailed in the current literature.
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| Enzyme Assay |
The in vitro binding assay for HYNIC-PSMA is conducted using PSMA-positive prostate cancer cell lines (e.g., LNCaP). Cells are incubated with varying concentrations of radiolabeled HYNIC-PSMA. The bound radioactivity is measured using a gamma counter. Non-specific binding is determined in the presence of an excess of unlabeled PSMA ligand. The binding affinity (Kd) and the number of binding sites (Bmax) are calculated from saturation binding curves.
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| Cell Assay |
In vitro cellular uptake assays are performed using PSMA-positive cells. Cells are incubated with radiolabeled HYNIC-PSMA at 37°C for various time points. The cells are then washed, and the internalized radioactivity is measured. The specificity of uptake is confirmed by blocking with an excess of unlabeled ligand. The internalization rate and the amount of internalized compound are determined.
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| Animal Protocol |
In vivo imaging studies for HYNIC-PSMA are conducted in mouse models bearing PSMA-positive tumor xenografts. The radiolabeled compound (e.g., ⁹⁹ᵐTc-HYNIC-PSMA) is administered via intravenous injection. SPECT/CT imaging is performed at various time points post-injection to visualize the biodistribution and tumor uptake of the tracer. The tumor-to-background ratio is calculated to assess the imaging contrast.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for HYNIC-PSMA is not extensively reported in publicly available sources. The compound has a CAS number of 2213408-17-2. The pharmacokinetic properties would depend on the specific radioisotope and the formulation used. For radiolabeled compounds, the biodistribution and clearance are typically evaluated in animal models. Detailed PK parameters are not available in the current literature.
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| Toxicity/Toxicokinetics |
Toxicity data for HYNIC-PSMA is not extensively reported. As a research compound, HYNIC-PSMA is intended for research use only and not for human therapeutic applications. The toxicity would depend on the specific radioisotope used for labeling. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment.
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| References | |
| Additional Infomation |
HYNIC-PSMA (CAS 2213408-17-2) is a synthetic peptide conjugate that targets prostate-specific membrane antigen (PSMA). It consists of a PSMA-targeting peptide linked to HYNIC, a chelator for radioactive isotopes. PSMA is specifically expressed on prostate cancer cells. HYNIC-PSMA is used in prostate cancer research and for the development of radionuclide-drug conjugates (RDCs) for imaging and therapy. It is for research use only.
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| Exact Mass |
567.265
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|---|---|
| CAS # |
2213408-17-2
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| PubChem CID |
168432170
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
9
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
20
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| Heavy Atom Count |
40
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| Complexity |
859
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1=CC(=NC=C1C(=O)NCCCCCC(=O)NCCCC[C@@H](C(=O)O)NC(=O)N[C@@H](CCC(=O)O)C(=O)O)NN
|
| InChi Key |
FZSZRXIUKIJFEN-IRXDYDNUSA-N
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| InChi Code |
InChI=1S/C24H37N7O9/c25-31-18-10-8-15(14-28-18)21(35)27-13-4-1-2-7-19(32)26-12-5-3-6-16(22(36)37)29-24(40)30-17(23(38)39)9-11-20(33)34/h8,10,14,16-17H,1-7,9,11-13,25H2,(H,26,32)(H,27,35)(H,28,31)(H,33,34)(H,36,37)(H,38,39)(H2,29,30,40)/t16-,17-/m0/s1
|
| Chemical Name |
(2S)-2-[[(1S)-1-carboxy-5-[6-[(6-hydrazinylpyridine-3-carbonyl)amino]hexanoylamino]pentyl]carbamoylamino]pentanedioic acid
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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.) |
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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