| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg | |||
| 50mg | |||
| Other Sizes |
| Targets |
(Hyp3)-Bradykinin targets bradykinin receptors, specifically the bradykinin B2 receptor (BDKRB2) and to a lesser extent the B1 receptor (BDKRB1). These are G protein-coupled receptors (GPCRs) that mediate the biological effects of bradykinin. The hydroxyproline substitution at position 3 may alter receptor binding affinity, selectivity, or metabolic stability compared to native bradykinin, making it useful for structure-activity studies.
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| ln Vitro |
[Hyp3]-Bradykinin is potent in isolated rat uterus and has the same ability to bind to bovine myometrium as native bradykinin [1].
In vitro, (Hyp3)-Bradykinin is used in receptor binding and functional assays to study bradykinin receptor pharmacology. The peptide may act as an agonist or antagonist at bradykinin receptors. It is used in calcium mobilization assays, inositol phosphate accumulation, or nitric oxide production assays in cells expressing B2 or B1 receptors. The hydroxyproline substitution allows investigation of how this residue contributes to receptor recognition and activation. |
| ln Vivo |
In vivo, (Hyp3)-Bradykinin is used to study the physiological effects of bradykinin receptor activation. As a bradykinin analog, it may have vasodilatory, hypotensive, or pro-inflammatory effects. The peptide is used in cardiovascular and inflammatory research to investigate blood pressure regulation, vascular permeability, and pain signaling. Detailed in vivo data depend on the experimental model and dosing regimen.
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| Enzyme Assay |
In vitro receptor binding assays for (Hyp3)-Bradykinin involve incubating the peptide with membrane preparations expressing bradykinin receptors (B2 or B1). Radiolabeled bradykinin is used as a tracer. Competition binding experiments determine binding affinity (IC50, Ki) for each receptor subtype. Assays are performed in buffer systems at physiological pH with protease inhibitors. The hydroxyproline substitution allows assessment of how proline hydroxylation affects receptor binding.
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| Cell Assay |
In vitro cell-based assays for (Hyp3)-Bradykinin use cells expressing bradykinin receptors, such as endothelial cells, smooth muscle cells, or transfected HEK-293 cells. Cells are treated with the peptide at various concentrations. Functional responses measured include intracellular calcium mobilization (Fluo-4 or Fura-2), inositol phosphate accumulation, nitric oxide production, or ERK phosphorylation. Dose-response curves determine EC50 or IC50 values for agonism or antagonism.
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| Animal Protocol |
In vivo animal studies for (Hyp3)-Bradykinin use rodent models for cardiovascular and inflammatory research. The peptide is administered via intravenous or intraperitoneal injection. Blood pressure is monitored by telemetry or tail-cuff methods. Vascular permeability is assessed by Evans blue dye extravasation. Pain responses may be evaluated in nociception assays. The peptide's effects are compared to native bradykinin and other analogs to determine structure-activity relationships.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of (Hyp3)-Bradykinin are typical of peptide analogs. Bradykinin and its analogs have very short half-lives in circulation due to rapid degradation by kininases (e.g., angiotensin-converting enzyme, ACE). The hydroxyproline substitution may confer some resistance to enzymatic degradation. As a peptide, it has limited oral bioavailability and is typically administered by injection. Detailed PK parameters require experimental determination.
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| Toxicity/Toxicokinetics |
Toxicity data for (Hyp3)-Bradykinin are limited as it is a research peptide. Bradykinin analogs may cause hypotension, increased vascular permeability, and pain due to their vasoactive and pro-inflammatory properties. The compound is for research use only and not for human therapeutic use. Cardiovascular effects should be considered when designing in vivo experiments. Standard laboratory safety precautions apply.
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| References | |
| Additional Infomation |
[Hyp(3)]-bradykinin is an oligopeptide and an analogue of bradykinin, in which the third amino acid, proline, is replaced by hydroxyproline. It is a human urinary metabolite and a bradykinin receptor agonist. It is an oligopeptide and peptide hormone that is functionally related to bradykinin and is the conjugate base of [Hyp(3)]-bradykinin(2+).
(Hyp3)-Bradykinin is a synthetic peptide analog of bradykinin with hydroxyproline at position 3. It is used to study bradykinin receptor pharmacology, structure-activity relationships, and signaling. The hydroxyproline substitution allows investigation of how proline hydroxylation affects receptor recognition, activation, and metabolic stability. It is for research use only. |
| Molecular Formula |
C28H30NO2CL
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|---|---|
| Molecular Weight |
447.9963
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| Exact Mass |
1075.556
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| CAS # |
37642-65-2
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| PubChem CID |
169947
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.700
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| LogP |
-1.09
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| Hydrogen Bond Donor Count |
13
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
27
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| Heavy Atom Count |
77
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| Complexity |
2110
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| Defined Atom Stereocenter Count |
9
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| SMILES |
C1C[C@H](N(C1)C(=O)[C@H](CCCN=C(N)N)N)C(=O)N2C[C@@H](C[C@H]2C(=O)NCC(=O)N[C@@H](CC3=CC=CC=C3)C(=O)N[C@@H](CO)C(=O)N4CCC[C@H]4C(=O)N[C@@H](CC5=CC=CC=C5)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)O
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| InChi Key |
JXRLHZCEMXTCBN-DIBGMJQNSA-N
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| InChi Code |
InChI=1S/C50H73N15O12/c51-32(15-7-19-56-49(52)53)45(73)64-22-10-18-38(64)47(75)65-27-31(67)25-39(65)43(71)58-26-40(68)59-34(23-29-11-3-1-4-12-29)41(69)62-36(28-66)46(74)63-21-9-17-37(63)44(72)61-35(24-30-13-5-2-6-14-30)42(70)60-33(48(76)77)16-8-20-57-50(54)55/h1-6,11-14,31-39,66-67H,7-10,15-28,51H2,(H,58,71)(H,59,68)(H,60,70)(H,61,72)(H,62,69)(H,76,77)(H4,52,53,56)(H4,54,55,57)/t31-,32+,33+,34+,35+,36+,37+,38+,39+/m1/s1
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| Chemical Name |
(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[2-[[(2S,4R)-1-[(2S)-1-[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]-4-hydroxypyrrolidine-2-carbonyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoic acid
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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 |
| 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) |
DMSO : ~100 mg/mL (~92.92 mM)
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2321 mL | 11.1607 mL | 22.3214 mL | |
| 5 mM | 0.4464 mL | 2.2321 mL | 4.4643 mL | |
| 10 mM | 0.2232 mL | 1.1161 mL | 2.2321 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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