| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Lys‑Bradykinin TFA targets the bradykinin B2 receptor (B2R), a G protein‑coupled receptor (GPCR) that is constitutively expressed in many tissues, including smooth muscle, endothelium, and neurons. Activation of B2R by bradykinin or kallidin triggers phospholipase C (PLC) activation, leading to increased intracellular calcium, release of nitric oxide (NO), and vasodilation. It also increases vascular permeability and causes pain (hyperalgesia). Lys‑Bradykinin is a full agonist of the B2 receptor with slightly lower potency than bradykinin itself.
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| ln Vitro |
Lys‑Bradykinin TFA is a naturally occurring bioactive peptide and an agonist of the bradykinin B2 receptor (B2R). It potently activates the B2 receptor, leading to the release of intracellular calcium, nitric oxide (NO), and prostaglandins. In isolated rat uterus and guinea pig ileum preparations, Lys‑Bradykinin induces concentration‑dependent contractions, with potencies similar to or slightly less than bradykinin. The compound is used in research on inflammation, pain, and cardiovascular function. No specific EC₅0 values are reported in the search results.
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| ln Vivo |
Lys‑Bradykinin TFA (kallidin) is a potent mediator of inflammation and pain in vivo. Intradermal injection of Lys‑Bradykinin in humans causes vasodilation (wheal) and increased vascular permeability (flare), leading to edema. In animal models, intravenous administration of Lys‑Bradykinin causes hypotension due to vasodilation. It also induces hyperalgesia (increased sensitivity to pain) when injected into tissues. These effects are mediated by the B2 receptor and are blocked by B2 receptor antagonists (e.g., icatibant). Lys‑Bradykinin is used to study the role of the kallikrein‑kinin system in inflammatory diseases.
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| Enzyme Assay |
The binding of Lys‑Bradykinin TFA to the B2 receptor is measured by competitive radioligand binding assays using cell membranes expressing the human B2 receptor. A radiolabeled B2 antagonist (e.g., [3H]‑icatibant or [3H]‑bradykinin) is used as a tracer. Lys‑Bradykinin is added at graded concentrations (0.1‑10,000 nM) to compete for binding, and the Ki or IC₅0 is calculated. For functional assays, the ability of Lys‑Bradykinin to induce calcium flux or inositol phosphate (IP) accumulation is measured.
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| Cell Assay |
For cellular assays, cells expressing the B2 receptor (e.g., HEK293‑B2R cells, or primary human fibroblasts) are seeded in 96‑well plates. Cells are loaded with Fluo‑4 AM, and Lys‑Bradykinin is added at graded concentrations (0.1‑10,000 nM). The increase in intracellular calcium is measured by fluorescence. The EC₅0 is calculated from dose‑response curves. For isolated tissue assays, rat uterus or guinea pig ileum strips are mounted in organ baths. Lys‑Bradykinin is added cumulatively (0.1‑1000 nM), and isotonic contractions are measured. The EC₅0 is calculated.
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| Animal Protocol |
For in vivo evaluation of hypotensive activity, male Sprague‑Dawley rats (250‑300 g) are anesthetized, and a carotid artery catheter is inserted for blood pressure monitoring. Lys‑Bradykinin is administered intravenously (IV) at doses of 1‑100 microg/kg. The decrease in mean arterial pressure (MAP) is recorded. For pain studies, Lys‑Bradykinin is injected intradermally into the hind paw of rats, and paw withdrawal latency (hyperalgesia) is measured using a pressure application device. These effects are blocked by pre‑treatment with a B2 antagonist (e.g., icatibant).
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| ADME/Pharmacokinetics |
Lys‑Bradykinin TFA (C₅₆H₈₅N1₇O12·xC2HF3O2, MW = 1188.39 (free base), purity ≥97%, CAS 71800‑36‑7 (free base)) is a lyophilized powder. For storage, the powder should be kept at -20degC or -80degC, sealed and protected from light. For in vitro use, stock solutions in water (10 mg/mL) or DMSO (10 mg/mL) can be prepared and stored at -80degC for up to 6 months or at -20degC for 1 month. The TFA salt form improves solubility and stability. No detailed PK parameters are reported.
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| Toxicity/Toxicokinetics |
Lys‑Bradykinin is a naturally occurring peptide that is a potent mediator of inflammation and pain. At high doses, it can cause severe hypotension and edema. As a research‑grade compound, it is not intended for human or veterinary use. Standard laboratory safety precautions for handling peptides should be followed. No LD₅0 or formal toxicology studies are available.
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| Additional Infomation |
Lys‑Bradykinin (kallidin) is a naturally occurring peptide of the kallikrein‑kinin system. It is derived from low‑molecular‑weight kininogen by the action of tissue kallikrein. Lys‑Bradykinin is a bradykinin analog with an additional N‑terminal lysine residue. It is a potent B2 receptor agonist and is more resistant to degradation by kininases than bradykinin. Lys‑Bradykinin has been studied for its roles in inflammation, pain, vasodilation, and cardiovascular regulation. The TFA salt is the industry standard for synthetic peptides. The compound is for research use only and has no clinical applications.
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| Molecular Formula |
C56H85N17O12.XC2HF3O2
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| Molecular Weight |
1188.38 (free base)
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| Appearance |
Solid powder
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| Synonyms |
Kallidin (380-389) (human, porcine, bovine) TFA
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : 33.3 mg/mL (with sonication and heat)
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| 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.) |
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.
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