1. GPCR/G Protein
  2. Bradykinin Receptor
  3. Lys-[Des-Arg9]Bradykinin TFA

Lys-[Des-Arg9]Bradykinin TFA, a naturally occurring kinin, is a potent and highly selective bradykinin B1 receptor agonist with a Ki of 0.12 nM, 1.7 nM and 0.23 nM for human, mouse and rabbit B1 receptors, respectively. Lys-[Des-Arg9]Bradykinin TFA has low inhibitory activity on B2 receptors.

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Lys-[Des-Arg9]Bradykinin TFA Chemical Structure

Lys-[Des-Arg9]Bradykinin TFA Chemical Structure

CAS No. : 2763588-90-3

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Description

Lys-[Des-Arg9]Bradykinin TFA, a naturally occurring kinin, is a potent and highly selective bradykinin B1 receptor agonist with a Ki of 0.12 nM, 1.7 nM and 0.23 nM for human, mouse and rabbit B1 receptors, respectively. Lys-[Des-Arg9]Bradykinin TFA has low inhibitory activity on B2 receptors[1][2].

IC50 & Target

Bradykinin B1 Receptor (B1R)

 

In Vitro

Lys-[Des-Arg9]Bradykinin is formed by the proteolytic cleavage of bradykinin, exerts its effects through bradykinin B1 receptor (B1R)[1].
Lys-[Des-Arg9]Bradykinin (Lda-BK; 10 μM) enhances the secretion of IL-12p70 and inhibits the secretion of IL-12p40 by mature hMo-DCs. Pretreatment with Lys-[Des-Arg9]Bradykinin treatment reduces the migration of mature hMo-DCs toward medium alone, suggesting that Lys-[Des-Arg9]Bradykinin may inhibit the chemokinesis of mature hMo-DCs[1].

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

In Vivo

Lys-[Des-Arg9]Bradykinin (1 μg; intra-artenal injection; New Zealand White rabbits) treatment reduces peripheral vascular resistance in LPS-induced rabbits, but the effect is brief (T1/2 is 118-195 s)[3].

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

Molecular Weight

1146.22

Formula

C52H74F3N13O13

CAS No.
Appearance

Solid

Color

White to off-white

Sequence Shortening

KRPPGFSPF

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture and light

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)

Solvent & Solubility
In Vitro: 

DMSO : 110 mg/mL (95.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 50 mg/mL (43.62 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8724 mL 4.3622 mL 8.7243 mL
5 mM 0.1745 mL 0.8724 mL 1.7449 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). 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.75 mg/mL (2.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.75 mg/mL (2.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (87.24 mM); Clear solution; Need ultrasonic

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). 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 / DMSO 1 mM 0.8724 mL 4.3622 mL 8.7243 mL 21.8108 mL
5 mM 0.1745 mL 0.8724 mL 1.7449 mL 4.3622 mL
10 mM 0.0872 mL 0.4362 mL 0.8724 mL 2.1811 mL
15 mM 0.0582 mL 0.2908 mL 0.5816 mL 1.4541 mL
20 mM 0.0436 mL 0.2181 mL 0.4362 mL 1.0905 mL
25 mM 0.0349 mL 0.1745 mL 0.3490 mL 0.8724 mL
30 mM 0.0291 mL 0.1454 mL 0.2908 mL 0.7270 mL
40 mM 0.0218 mL 0.1091 mL 0.2181 mL 0.5453 mL
DMSO 50 mM 0.0174 mL 0.0872 mL 0.1745 mL 0.4362 mL
60 mM 0.0145 mL 0.0727 mL 0.1454 mL 0.3635 mL
80 mM 0.0109 mL 0.0545 mL 0.1091 mL 0.2726 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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Lys-[Des-Arg9]Bradykinin TFA 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.

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Lys-[Des-Arg9]Bradykinin TFA
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