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  4. Certepetide

Certepetide  (Synonyms: CEND-1; iRGD; LSTA1)

Cat. No.: HY-P3448 Purity: 99.40%
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Certepetide (CEND-1) is a bifunctional cyclic peptide (a.k.a. iRGD). Certepetide is a tumor-penetrating enhancer via RGD motif interaction with alphav-integrins and via activating NRP-1, and transforms the solid tumor microenvironment into a temporary agent conduit. Certepetide accumulates in tumors, and is used in the research of pancreatic cancer and other solid tumors.

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

Custom Peptide Synthesis

Certepetide Chemical Structure

Certepetide Chemical Structure

CAS No. : 2580154-02-3

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5 mg USD 250 In-stock
10 mg USD 400 In-stock
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Based on 1 publication(s) in Google Scholar

Certepetide Related Antibodies

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View All Integrin Isoform Specific Products:

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αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

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Description

Certepetide (CEND-1) is a bifunctional cyclic peptide (a.k.a. iRGD). Certepetide is a tumor-penetrating enhancer via RGD motif interaction with alphav-integrins and via activating NRP-1, and transforms the solid tumor microenvironment into a temporary agent conduit. Certepetide accumulates in tumors, and is used in the research of pancreatic cancer and other solid tumors[1][2][3].

IC50 & Target

Alphav-integrins, NRP-1[3].
In Vivo

CEND-1 (iRGD) can modulate the solid tumour microenvironment, enhancing the delivery and therapeutic index of co-administered anti-cancer agents[4].
CEND-1 enhances the penetration of anticancer therapeutics specifically into tumours, but not into normal tissues, it also holds the potential for dose reductions, which can attenuate side effects[4].
CEND-1 (intravenously injected) increases the levels of co-administered Evans blue approximately threefold[5].

Table 1. Derived mean pharmacokinetic parameters for CEND-1 in mouse, rat, dog and monkey plasma after a single intravenous infusion of CEND-1 (±SD) [5].
Number of Animals (Sex) CEND-1 Dose (mg/kg) t1/2 (h) C0 (ng/mL) V (mL/kg) Cl_obs (mL/hr/kg) AUC0-inf (h*ng/mL)
Mouse *
3 (M) 1.5 0.306 10,343 449 1016 1476
3 (M) 13.5 0.547 68,358 1007 1277 10,569
Rat*
6 (M) 75 0.341 469,000 171 348 215,476
6 (F) 75 0.391 436,333 254 451 166,331
Dog*
3 (M) 1 0.665 (0.0448) 6010 (1985) 241 (27) 253 (40.1) 4030 (686)
3 (F) 5 0.648 (0.0486) 25,133 (3635) 230 (14.6) 247 (32.9) 20,443 (2530)
Monkey*
3 (M) 5 0.888 (0.0963) 55,082 (19,905) 204 (14.1) 179 (23.4) 28,230 (3865)
3 (M) 50 0.956 (0.0869) 602,161 (211,386) 162 (32.1) 178 (51.9) 421,119 (171,418)
Note:* Because of volume limitations in the mice and rats, each animal was used for one time point sampling, limiting the statistical analysis of the data. M, male; F, female.

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

989.09

Formula

C37H60N14O14S2
CAS No.
Appearance

Solid

Color

White to off-white

Sequence Shortening

Ac-CRGDKGPDC-NH2 (Disulfide bridge: Cys1-Cys9)
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Sealed storage, away from moisture and light, under nitrogen

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

Solvent & Solubility
In Vitro: 

H2O : ≥ 50 mg/mL (50.55 mM)

DMSO : 2.33 mg/mL (2.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0110 mL 5.0552 mL 10.1103 mL
5 mM 0.2022 mL 1.0110 mL 2.0221 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 (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
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 (sealed storage, away from moisture and light, under nitrogen). 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 / H2O 1 mM 1.0110 mL 5.0552 mL 10.1103 mL 25.2758 mL
H2O 5 mM 0.2022 mL 1.0110 mL 2.0221 mL 5.0552 mL
10 mM 0.1011 mL 0.5055 mL 1.0110 mL 2.5276 mL
15 mM 0.0674 mL 0.3370 mL 0.6740 mL 1.6851 mL
20 mM 0.0506 mL 0.2528 mL 0.5055 mL 1.2638 mL
25 mM 0.0404 mL 0.2022 mL 0.4044 mL 1.0110 mL
30 mM 0.0337 mL 0.1685 mL 0.3370 mL 0.8425 mL
40 mM 0.0253 mL 0.1264 mL 0.2528 mL 0.6319 mL
50 mM 0.0202 mL 0.1011 mL 0.2022 mL 0.5055 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Certepetide Related Classifications

Help & FAQs
  • 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.

Keywords:

Certepetide2580154-02-3CEND-1 iRGD LSTA1CEND1CEND 1LSTA1LSTA 1LSTA-1IntegrinComplement Systemcyclic peptideantitumorsolid cancerintegrinInhibitorinhibitorinhibit

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