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  3. Lys(CO-C3-p-I-Ph)-O-tBu

Lys(CO-C3-p-I-Ph)-O-tBu is a pharmacokinetic modifier (PK modifier) that can improve the PK properties of PSMA ligand molecules. Lys(CO-C3-p-I-Ph)-O-tBu can increase the residence time of PSMA ligand in plasma by increasing its binding capacity to albumin. Lys(CO-C3-p-I-Ph)-O-tBu also reduces salivary gland absorption, possibly extending the half-life of the active compound. Ac-PSMA-trillium is a suitable PSMA-targeting compound that has different biological applications after modification with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or labeled with 225Ac as a Macropa chelator for targeted radionuclide therapy (TRT) in the study of metastatic castration-resistant prostate cancer (mCRPC).

For research use only. We do not sell to patients.

Lys(CO-C3-p-I-Ph)-O-tBu Chemical Structure

Lys(CO-C3-p-I-Ph)-O-tBu Chemical Structure

CAS No. : 2703051-80-1

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5 mg USD 150 In-stock
10 mg USD 250 In-stock
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50 mg USD 900 In-stock
100 mg USD 1450 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Lys(CO-C3-p-I-Ph)-O-tBu is a pharmacokinetic modifier (PK modifier) that can improve the PK properties of PSMA ligand molecules. Lys(CO-C3-p-I-Ph)-O-tBu can increase the residence time of PSMA ligand in plasma by increasing its binding capacity to albumin. Lys(CO-C3-p-I-Ph)-O-tBu also reduces salivary gland absorption, possibly extending the half-life of the active compound. Ac-PSMA-trillium is a suitable PSMA-targeting compound that has different biological applications after modification with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or labeled with 225Ac as a Macropa chelator for targeted radionuclide therapy (TRT) in the study of metastatic castration-resistant prostate cancer (mCRPC)[1][2].

Molecular Weight

474.38

Formula

C20H31IN2O3

CAS No.
Appearance

Oil

Color

Light yellow to yellow

SMILES

IC1=CC=C(CCCC(NCCCC[C@@H](C(OC(C)(C)C)=O)N)=O)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (210.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1080 mL 10.5401 mL 21.0801 mL
5 mM 0.4216 mL 2.1080 mL 4.2160 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1080 mL 10.5401 mL 21.0801 mL 52.7004 mL
5 mM 0.4216 mL 2.1080 mL 4.2160 mL 10.5401 mL
10 mM 0.2108 mL 1.0540 mL 2.1080 mL 5.2700 mL
15 mM 0.1405 mL 0.7027 mL 1.4053 mL 3.5134 mL
20 mM 0.1054 mL 0.5270 mL 1.0540 mL 2.6350 mL
25 mM 0.0843 mL 0.4216 mL 0.8432 mL 2.1080 mL
30 mM 0.0703 mL 0.3513 mL 0.7027 mL 1.7567 mL
40 mM 0.0527 mL 0.2635 mL 0.5270 mL 1.3175 mL
50 mM 0.0422 mL 0.2108 mL 0.4216 mL 1.0540 mL
60 mM 0.0351 mL 0.1757 mL 0.3513 mL 0.8783 mL
80 mM 0.0264 mL 0.1318 mL 0.2635 mL 0.6588 mL
100 mM 0.0211 mL 0.1054 mL 0.2108 mL 0.5270 mL
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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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Lys(CO-C3-p-I-Ph)-O-tBu
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