![Sar-[D-Phe8]-des-Arg9-Bradykinin](/upload/1124/V75320.png)
| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg | |||
| Other Sizes |
| Targets |
Sar-[D-Phe8]-des-Arg9-Bradykinin specifically targets the bradykinin B1 receptor (B1R), a G protein-coupled receptor that is part of the kinin receptor family. Unlike the B2 receptor, which is constitutively expressed, the B1 receptor is typically induced by inflammatory stimuli such as cytokines (e.g., IL-1β) and plays a critical role in chronic inflammation and pain pathways. This compound acts as a potent agonist at this receptor.
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| ln Vitro |
In vitro, Sar-[D-Phe8]-des-Arg9-Bradykinin demonstrates exceptionally potent agonist activity at the bradykinin B1 receptor, with an EC50 value of 9.02 nM in functional assays using rabbit aortic rings. It selectively amplifies the contractile response in these tissues when they are pre-incubated with human recombinant interleukin-1β (IL-1β), which is known to upregulate B1 receptor expression. This selective activity profile confirms its high potency and specificity for the B1 receptor.
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| ln Vivo |
In vivo, Sar-[D-Phe8]-des-Arg9-Bradykinin exhibits hypotensive (blood pressure-lowering) and angiogenic (blood vessel-forming) activities. Its resistance to metabolic degradation by key enzymes allows it to maintain its activity in vivo for extended periods compared to native bradykinin peptides. This property makes it a critical pharmacological tool for investigating the role of the B1 receptor in various disease models where the receptor is upregulated, such as inflammation and vascular dysfunction.
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| Enzyme Assay |
For non-cellular in vitro enzyme/receptor binding assays, the affinity and selectivity of Sar-[D-Phe8]-des-Arg9-Bradykinin for the B1 receptor are typically characterized using radioligand binding displacement assays with membrane preparations from cells expressing the recombinant human B1 receptor. The compound's potency is also confirmed in cell-free systems by measuring its ability to stimulate GTPγS binding, a measure of G protein activation, in membranes prepared from B1 receptor-expressing cells.
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| Cell Assay |
For in vitro cellular assays, the activity of Sar-[D-Phe8]-des-Arg9-Bradykinin is commonly evaluated in cell lines that endogenously or heterologously express the bradykinin B1 receptor. A typical assay involves measuring the agonist-induced mobilization of intracellular calcium, a classic signaling readout for Gq-coupled GPCRs. Cells are loaded with a calcium-sensitive fluorescent dye, and the increase in fluorescence upon compound addition is measured to determine the EC50 for receptor activation.
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| Animal Protocol |
For in vivo animal studies, Sar-[D-Phe8]-des-Arg9-Bradykinin has been used to investigate the physiological and pathophysiological roles of the B1 receptor. For example, it has been evaluated for its hypotensive effects in animal models. In studies of inflammation and pain, the compound is often administered to rodents to assess its ability to modulate B1 receptor-mediated responses, such as hyperalgesia or edema formation, in models where the B1 receptor is upregulated.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Sar-[D-Phe8]-des-Arg9-Bradykinin are not extensively documented in the provided search results. However, its chemical design, which includes a sarcosine residue and D-amino acid substitutions, is specifically intended to confer resistance to metabolic degradation by aminopeptidases, kininase I and II (ACE), and neutral endopeptidase. This metabolic stability is a key feature that significantly prolongs its half-life and improves its bioavailability in vivo compared to native bradykinin and other less protected analogs.
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| Toxicity/Toxicokinetics |
Toxicological data for Sar-[D-Phe8]-des-Arg9-Bradykinin are limited. As a research compound, it is intended for laboratory use only and not for human therapeutic applications. Its safety profile has not been established for clinical use. However, given its mechanism as a potent vasoactive peptide agonist, potential toxicities could be related to its hypotensive and angiogenic activities. Comprehensive toxicology studies would be required before any therapeutic development could be considered.
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| References | |
| Additional Infomation |
Sar-[D-Phe8]-des-Arg9-Bradykinin is a potent, selective, and metabolically resistant agonist for the bradykinin B1 receptor. It is a synthetic peptide with the sequence H-Sar-Arg-Pro-Pro-Gly-Phe-Ser-Pro-D-Phe-OH. As a B1 receptor agonist, it is a critical research tool for studying the kinin system, inflammation, pain, and vascular biology. Its resistance to degradation makes it particularly useful for in vivo experiments where sustained receptor activation is required.
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| Molecular Formula |
C47H66N12O11
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| Molecular Weight |
975.10
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| Exact Mass |
974.497
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| CAS # |
126959-88-4
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| PubChem CID |
164234
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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 |
1.677
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| LogP |
0.44
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
24
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| Heavy Atom Count |
70
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| Complexity |
1870
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| Defined Atom Stereocenter Count |
7
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| SMILES |
CNCC(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N2CCC[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)O
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| InChi Key |
YIUBSFCQATYQJB-VCMDLEIESA-N
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| InChi Code |
InChI=1S/C47H66N12O11/c1-50-26-38(61)53-31(16-8-20-51-47(48)49)43(66)59-23-11-19-37(59)45(68)58-22-9-17-35(58)41(64)52-27-39(62)54-32(24-29-12-4-2-5-13-29)40(63)56-34(28-60)44(67)57-21-10-18-36(57)42(65)55-33(46(69)70)25-30-14-6-3-7-15-30/h2-7,12-15,31-37,50,60H,8-11,16-28H2,1H3,(H,52,64)(H,53,61)(H,54,62)(H,55,65)(H,56,63)(H,69,70)(H4,48,49,51)/t31-,32-,33+,34-,35-,36-,37-/m0/s1
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| Chemical Name |
(2R)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[2-[[(2S)-1-[(2S)-1-[(2S)-5-(diaminomethylideneamino)-2-[[2-(methylamino)acetyl]amino]pentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoic 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 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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0255 mL | 5.1277 mL | 10.2554 mL | |
| 5 mM | 0.2051 mL | 1.0255 mL | 2.0511 mL | |
| 10 mM | 0.1026 mL | 0.5128 mL | 1.0255 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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