2. Protein Tyrosine Kinase/RTK Others
  3. IGF-1R VEGFR Drug Derivative
  4. JB-1

JB-1, an IGF-I analog, is a selective IGF-I receptor inhibitor that does not interact with IGF-II. JB-1 competes with IGF-I for binding to IGF-1R and blocks receptor autophosphorylation. JB-1 increases the level of sVEGFR-1. JB-1 normalizes retinal abnormalities, including reducing retinal neovascularization. JB-1 is applicable to studies related to oxygen-induced retinopathy.

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Custom Peptide Synthesis

JB-1

JB-1 Chemical Structure

CAS No. : 147819-32-7

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JB-1 Related Antibodies

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Description

JB-1, an IGF-I analog, is a selective IGF-I receptor inhibitor that does not interact with IGF-II. JB-1 competes with IGF-I for binding to IGF-1R and blocks receptor autophosphorylation. JB-1 increases the level of sVEGFR-1. JB-1 normalizes retinal abnormalities, including reducing retinal neovascularization. JB-1 is applicable to studies related to oxygen-induced retinopathy[1].

IC50 & Target[1]

VEGFR-1

 

In Vivo

Early short-term JB-1 (1 μg/day; s.c.; P1-P3) normalizes retinal abnormalities in H/H-exposed rats, reducing retinal neovascularization area to 1.4 × 105 μm2 (p < 0.01 vs saline H/H) and preventing severe OIR, while long-term JB-1 (1 μg/day; s.c.; alternate days P1-P13) leads to severe OIR in 90% of retinas by P21[1].

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

Animal Model: Sprague Dawley (newborn, pooled from timed-pregnant dams, assigned to expanded litters of 17 pups/litter, hyperoxia/hypoxia cycling exposed)[1]
Dosage: 1 μg/day (JB1x3: P1, P2, P3); 1 μg/day (JB1x7: P1, P3, P5, P7, P9, P11, P13)
Administration: s.c.
Result: Increased body weight to 22.1 ± 0.51 g and linear growth to 6.0 ± 0.12 cm at P14 compared to saline-treated H/H littermates (JB1x3).
Increased serum sVEGFR-1 to 3562.5 ± 439.7 pg/mL at P14 compared to saline H/H (JB1x3).
Increased retinal VEGF and sVEGFR-1 levels at P14 compared to saline H/H (JB1x3).
Decreased retinal neovascularization area to 1.4 × 105 μm2 at P14 compared to saline H/H (2.0 × 105 μm2, p < 0.01) and JB1x7 H/H (1.7 × 105 μm2, p < 0.05) (JB1x3).
Resulted in all retinal flatmounts scoring <12 (no severe OIR) at P14 (JB1x3).
Sustained increased serum sVEGFR-1 to 6011.8 ± 800.2 pg/mL at P21 compared to saline H/H; downregulated VEGFA mRNA compared to saline H/H (JB1x3).
Decreased body weight to 17.5 ± 0.45 g and linear growth to 5.3 ± 0.10 cm at P14 compared to JB1x3 H/H (JB1x7).
Increased serum sVEGFR-1 to 5834.40 ± 903.5 pg/mL at P14 compared to saline H/H (JB1x7).
Decreased retinal sVEGFR-1 levels at P14 compared to saline H/H (JB1x7).
Decreased retinal neovascularization area to 1.7 × 105 μm2 at P14 compared to saline H/H (p < 0.05) (JB1x7).
Resulted in decreased body weight to 32.5 ± 1.00 g and linear growth to 6.4 ± 0.11 cm at P21 compared to saline H/H (JB1x7).
Suppressed serum sVEGFR-1 to 401.7 ± 31.7 pg/mL at P21 compared to saline H/H (JB1x7).
Resulted in extended retinal vascular overgrowth area to 2.6 × 105 μm2 (p < 0.01) similar to saline H/H, and 90% of retinal flatmounts scoring >12 (severe OIR) at P21 (JB1x7).
Upregulated VEGFA mRNA at P21 compared to JB1x3 H/H (JB1x7).
Clinical Trial
Molecular Weight

1249.50

Formula

C55H88N14O15S2
CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Cys-Tyr-Ala-Ala-Pro-Leu-Lys-Pro-Ala-Lys-Ser-Cys (Disulfide bridge: Cys1-Cys12)
Sequence Shortening

CYAAPLKPAKSC (Disulfide bridge: Cys1-Cys12)
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

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

Solvent & Solubility
In Vitro: 

H2O : ≥ 100 mg/mL (80.03 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8003 mL 4.0016 mL 8.0032 mL
5 mM 0.1601 mL 0.8003 mL 1.6006 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). 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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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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

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g

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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). 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
H2O 1 mM 0.8003 mL 4.0016 mL 8.0032 mL 20.0080 mL
5 mM 0.1601 mL 0.8003 mL 1.6006 mL 4.0016 mL
10 mM 0.0800 mL 0.4002 mL 0.8003 mL 2.0008 mL
15 mM 0.0534 mL 0.2668 mL 0.5335 mL 1.3339 mL
20 mM 0.0400 mL 0.2001 mL 0.4002 mL 1.0004 mL
25 mM 0.0320 mL 0.1601 mL 0.3201 mL 0.8003 mL
30 mM 0.0267 mL 0.1334 mL 0.2668 mL 0.6669 mL
40 mM 0.0200 mL 0.1000 mL 0.2001 mL 0.5002 mL
50 mM 0.0160 mL 0.0800 mL 0.1601 mL 0.4002 mL
60 mM 0.0133 mL 0.0667 mL 0.1334 mL 0.3335 mL
80 mM 0.0100 mL 0.0500 mL 0.1000 mL 0.2501 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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JB-1 Related Classifications

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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.

Keywords:

JB-1147819-32-7JB1JB 1IGF-1RVEGFRDrug DerivativeInsulin-like growth factor-1 receptorVascular endothelial growth factor receptorDrug derivativeIGF-IIretinal neovascularizationretinaoxygen-induced retinopathyvascular endothelial growth factor receptor 1IGF-I receptorratsIGF-IInhibitorinhibitorinhibit

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