| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Targets the bradykinin B2 receptor (B2R) with high affinity (pKi = 10.3). It acts as a competitive antagonist, blocking the binding of the natural ligand bradykinin. MEN 11270 is highly selective, displaying a pIC50 of less than 5.5 for 29 other receptors and ion channels.
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| ln Vitro |
As a potent B2 receptor antagonist, MEN 11270 effectively inhibits bradykinin-induced signaling pathways. By blocking B2R activation, it prevents downstream effects such as G-protein coupling, phospholipase C activation, and subsequent calcium mobilization. It acts as a pure antagonist with no detectable agonist activity, making it a standard tool for B2R pharmacology.
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| ln Vivo |
MEN 11270 has been shown to block bradykinin-induced hypotension and bronchoconstriction in vivo in preclinical models such as anesthetized guinea pigs. These effects are mediated by the B2 bradykinin receptor, and its antagonism by MEN 11270 confirms the receptor‘s role in these physiological responses, making it a valuable tool for in vivo pharmacology.
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| Enzyme Assay |
Non-cell radioligand binding assays are performed using membranes from WI38 human fibroblasts, which constitutively express the B2 kinin receptor. Membranes are incubated with [3H]-bradykinin (BK) and increasing concentrations of MEN 11270. Bound radioactivity is separated by filtration and counted. The pKi of 10.3 is derived from competition binding experiments.
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| Cell Assay |
Functional antagonism is typically assessed in cell lines endogenously expressing the B2 receptor, such as WI38 fibroblasts or A431 cells. Cells are loaded with a fluorescent calcium indicator dye. After a pre-incubation with MEN 11270, the cells are stimulated with bradykinin. The inhibition of bradykinin-induced calcium flux by MEN 11270 is measured to confirm its antagonist activity and calculate its functional pA2/pKi.
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| Animal Protocol |
In anesthetized guinea pig models, animals are surgically prepared for monitoring blood pressure and airway function. MEN 11270 is administered intravenously prior to a challenge with bradykinin. The ability of the compound to block bradykinin-induced hypotension and bronchoconstriction is measured as the primary endpoint, establishing the in vivo efficacy of the B2 receptor blockade.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for MEN 11270 is limited. As a cyclic decapeptide with a molecular weight of 1299.56 g/mol, it is not likely to be orally bioavailable and is typically administered by injection for in vivo studies. Its stability and half-life in vivo would be key parameters for its use as an experimental tool.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available for MEN 11270. As a research tool, no safety studies have been published. Given its high specificity for the B2 receptor, off-target toxicities are considered low, but its pharmacological effect of blocking bradykinin could potentially impact cardiovascular and inflammatory homeostasis at high doses.
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| References | |
| Additional Infomation |
MEN 11270 is a research-grade reagent and is not approved for clinical use. It is a second-generation, conformationally constrained cyclic peptide derived from Icatibant (HOE 140), designed for greater stability and affinity. It is an essential tool for investigating the biology of the bradykinin B2 receptor in inflammation, pain, and cardiovascular function.
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| Molecular Formula |
C60H90N20O11S
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|---|---|
| Molecular Weight |
1299.55
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| Exact Mass |
1298.681
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| CAS # |
235082-52-7
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| PubChem CID |
90488898
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Index of Refraction |
1.755
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| LogP |
-5.38
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| Hydrogen Bond Donor Count |
14
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
24
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| Heavy Atom Count |
92
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| Complexity |
2750
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| Defined Atom Stereocenter Count |
10
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| SMILES |
C1CCC2C(C1)C[C@@H]3N2C(=O)[C@H]4CC5=CC=CC=C5CN4C(=O)[C@H](CCNC(=O)[C@@H](NC3=O)CCCN=C(N)N)NC(=O)[C@@H](CC6=CC=CS6)NC(=O)CNC(=O)[C@@H]7C[C@H](CN7C(=O)[C@@H]8CCCN8C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)N)O
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| InChi Key |
LPLBKEKLEUYDEJ-UUHVOKIZSA-N
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| InChi Code |
InChI=1S/C60H90N20O11S/c61-38(14-5-20-69-58(62)63)49(83)75-40(16-7-22-71-60(66)67)54(88)77-24-8-18-44(77)56(90)79-32-36(81)28-45(79)52(86)72-30-48(82)73-42(29-37-13-9-25-92-37)51(85)76-41-19-23-68-50(84)39(15-6-21-70-59(64)65)74-53(87)46-27-34-11-3-4-17-43(34)80(46)57(91)47-26-33-10-1-2-12-35(33)31-78(47)55(41)89/h1-2,9-10,12-13,25,34,36,38-47,81H,3-8,11,14-24,26-32,61H2,(H,68,84)(H,72,86)(H,73,82)(H,74,87)(H,75,83)(H,76,85)(H4,62,63,69)(H4,64,65,70)(H4,66,67,71)/t34?,36-,38-,39+,40+,41+,42-,43?,44+,45+,46+,47-/m1/s1
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| Chemical Name |
(2S,4R)-1-[(2S)-1-[(2S)-2-[[(2R)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]-N-[2-[[(2R)-1-[[(1R,11S,14S,19S)-14-[3-(diaminomethylideneamino)propyl]-2,12,15,20-tetraoxo-3,13,16,21-tetrazapentacyclo[19.8.0.03,11.04,9.023,28]nonacosa-23,25,27-trien-19-yl]amino]-1-oxo-3-thiophen-2-ylpropan-2-yl]amino]-2-oxoethyl]-4-hydroxypyrrolidine-2-carboxamide
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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) |
DMSO: 100 mg/mL (76.95 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.92 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (1.92 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7695 mL | 3.8475 mL | 7.6950 mL | |
| 5 mM | 0.1539 mL | 0.7695 mL | 1.5390 mL | |
| 10 mM | 0.0769 mL | 0.3847 mL | 0.7695 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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