| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
Purity: ≥98%
| Targets |
Macropa is a macrocyclic chelator that binds radiometals, particularly actinium-225 (²²⁵Ac) and other radiometals, for targeted radionuclide therapy and imaging applications. It does not have a biological target itself but serves as a carrier for radioactive isotopes that are conjugated to targeting vectors such as antibodies or peptides.
|
|---|---|
| ln Vitro |
As a chelator, Macropa itself does not possess pharmacological activity. Its utility lies in its metal-binding properties: it forms highly stable complexes with radiometals, particularly actinium-225 (²²⁵Ac), with exceptional kinetic inertness and thermodynamic stability. This enables the delivery of radioactive isotopes to disease sites when conjugated to targeting moieties.
|
| ln Vivo |
As a chelator for radiometals, Macropa is used in preclinical imaging and therapy studies. When complexed with radiometals such as ²²⁵Ac and conjugated to tumor-targeting vectors, the Macropa-based probes enable targeted alpha therapy and imaging of soft tissue metastases. In vivo studies have demonstrated the utility of Macropa for radiolabeling and targeted delivery.
|
| Enzyme Assay |
Non-cell-based protocols for Macropa involve radiochemistry and chelation studies. A typical protocol includes: dissolving Macropa in appropriate buffer (e.g., 0.1 M MES buffer at pH 5.5–6.0), adding radiometal solution (e.g., ²²⁵Ac in dilute HCl), incubating at 37–80°C for 15–60 minutes, and assessing radiochemical purity by radio-TLC or radio-HPLC. Chelation efficiency and stability are evaluated under various conditions including competition with DTPA or EDTA.
|
| Cell Assay |
Cellular assays with Macropa-radiolabeled conjugates typically involve binding and internalization studies. A representative protocol includes: culturing target cells expressing the antigen of interest, incubating with the radiolabeled Macropa-conjugate (e.g., ²²⁵Ac-Macropa-antibody) for 1–4 hours at 37°C, washing, measuring cell-bound radioactivity using a gamma counter, and determining internalization by acid wash to remove surface-bound activity. Cytotoxicity of alpha-emitting conjugates can be assessed by clonogenic assays.
|
| Animal Protocol |
In vivo animal studies with Macropa-based radiopharmaceuticals typically involve xenograft mouse models. A representative protocol includes: subcutaneous or orthotopic implantation of tumor cells in immunodeficient mice, intravenous injection of the ²²⁵Ac-Macropa-conjugate (typically 5–50 μCi/kg), monitoring tumor growth and body weight, performing SPECT or PET imaging if using appropriate isotopes, collecting tissues for biodistribution analysis, and assessing therapeutic efficacy by tumor volume measurements.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Macropa-based radiopharmaceuticals depend on the targeting vector. Typical PK parameters for Macropa-antibody conjugates include slow clearance from circulation (t₁/₂ of days), tumor accumulation peaking at 24–72 hours post-injection, and excretion primarily via renal and hepatobiliary routes. The chelator itself provides favorable metal retention and stability in vivo.
|
| Toxicity/Toxicokinetics |
Toxicological data for Macropa are limited as it is a research-use chelator. Standard safety precautions should be followed when handling the compound and its radioactive conjugates. The compound is typically stored as a powder at -20°C for long-term preservation. Solubility is good in water and DMSO (~125 mg/mL).
|
| References | |
| Additional Infomation |
Macropa (CAS 1128304-86-8) is an advanced macrocyclic chelator for radiometal-based targeted imaging and therapy. Its exceptional complexation properties with actinium-225 make it particularly valuable for targeted alpha therapy (TAT) applications. The chelator's structure features two pyridinecarboxylic acid moieties linked by a diaza-crown ether, providing optimal coordination geometry for large radiometals. Macropa is widely used in the development of next-generation radiopharmaceuticals for cancer treatment.
|
| Molecular Formula |
C26H36N4O8.HCL
|
|---|---|
| Molecular Weight |
569.04
|
| Exact Mass |
532.253
|
| CAS # |
1128304-86-8
|
| Related CAS # |
2648154-46-3
|
| PubChem CID |
57329142
|
| Appearance |
White to off-white solid powder
|
| LogP |
-4.4
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
12
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
38
|
| Complexity |
612
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O1CCN(CC2N=C(C(O)=O)C=CC=2)CCOCCOCCN(CC2N=C(C(O)=O)C=CC=2)CCOCC1
|
| InChi Key |
AHJIXPVAMVLFOG-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C26H36N4O8/c31-25(32)23-5-1-3-21(27-23)19-29-7-11-35-15-17-37-13-9-30(10-14-38-18-16-36-12-8-29)20-22-4-2-6-24(28-22)26(33)34/h1-6H,7-20H2,(H,31,32)(H,33,34)
|
| Chemical Name |
6-[[16-[(6-carboxypyridin-2-yl)methyl]-1,4,10,13-tetraoxa-7,16-diazacyclooctadec-7-yl]methyl]pyridine-2-carboxylic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
H2O :~125 mg/mL (~234.70 mM; with sonication)
DMSO :~125 mg/mL (~234.70 mM; with sonication) |
|---|---|
| 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 | 1.7573 mL | 8.7867 mL | 17.5735 mL | |
| 5 mM | 0.3515 mL | 1.7573 mL | 3.5147 mL | |
| 10 mM | 0.1757 mL | 0.8787 mL | 1.7573 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA