| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Angiotensin-converting enzyme (ACE); Bradykinin inhibitory peptidase
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|---|---|
| ln Vitro |
The peptide exhibits strong bradykinin-potentiating activity on isolated guinea pig ileum. It distinctly increases the contractile effect of bradykinin on smooth muscles without causing contraction by itself. The effect persists even after washing the organ, suggesting it increases bradykinin's effect by inhibiting its enzymatic destruction.
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| ln Vivo |
Currently, no specific in vivo data is available for this compound. Similar snake venom peptides have been shown to induce hypotensive effects in animal models by enhancing the vasodilatory actions of bradykinin and inhibiting the renin-angiotensin system.
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| Enzyme Assay |
An in vitro assay for ACE inhibition typically uses a substrate like Hip-His-Leu. The peptide is incubated with ACE enzyme in a buffer at 37degC. Hippuric acid released from the substrate is extracted with ethyl acetate and its absorbance measured. For bradykinin potentiation, the contractile response to bradykinin is recorded using an isolated guinea pig ileum organ bath.
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| Cell Assay |
A typical protocol for studying bradykinin potentiation uses isolated guinea pig ileum segments. Tissues are suspended in an organ bath containing Tyrode's solution at 37degC, bubbled with 95% O2/5% CO2. Isometric contractions are recorded via a transducer. The peptide is added before bradykinin, and the augmentation of bradykinin-induced contraction is measured.
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| Animal Protocol |
General in vivo studies for bradykinin-potentiating peptides involve administering the compound intravenously to anesthetized rats. Blood pressure is continuously monitored via a carotid artery catheter. The compound is typically given as a bolus injection, and its effect on blood pressure in response to exogenous bradykinin is recorded.
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| ADME/Pharmacokinetics |
General PK properties for peptides are often characterized by poor oral bioavailability due to degradation in the gastrointestinal tract, a very short plasma half-life (often minutes), and rapid clearance via renal excretion and proteolytic degradation. For research purposes, they are typically administered intravenously.
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| Toxicity/Toxicokinetics |
General toxicity of snake venom peptides is dose-dependent, with potential effects including significant hypotension. At high doses, they may cause respiratory distress or anaphylactic reactions due to the introduction of a foreign protein. No specific LD50 or chronic toxicity data is available for this specific peptide.
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| References |
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| Additional Infomation |
This peptide originates from snake venom and functions as an ACE inhibitor. Its mechanism of action is to potentiate bradykinin-mediated vasodilation. It is used as a research tool to study the kinin-kallikrein system and blood pressure regulation. It has not been developed into a clinical drug.
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| Molecular Formula |
C56H91N15O13
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|---|---|
| Molecular Weight |
1182.41
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| Exact Mass |
1181.69
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| CAS # |
30892-86-5
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| PubChem CID |
3084520
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| Appearance |
White to off-white solid powder
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| Density |
1.48g/cm3
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| Index of Refraction |
1.684
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| LogP |
1.708
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
28
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| Heavy Atom Count |
84
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| Complexity |
2460
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCC(C)C(C(=O)N1CCCC1C(=O)N2CCCC2C(=O)O)NC(=O)C(CCCCN)NC(=O)C3CCCN3C(=O)C(CCCN=C(N)N)NC(=O)C4CCCN4C(=O)C5CCCN5C(=O)C(CC(C)C)NC(=O)CNC(=O)C6CCC(=O)N6
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| InChi Key |
JXGBFZMUUPNIBD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C56H91N15O13/c1-5-33(4)45(54(82)70-28-12-19-41(70)53(81)71-29-13-20-42(71)55(83)84)66-47(75)34(14-6-7-23-57)64-48(76)38-16-9-25-67(38)50(78)36(15-8-24-60-56(58)59)65-49(77)39-17-10-26-68(39)52(80)40-18-11-27-69(40)51(79)37(30-32(2)3)63-44(73)31-61-46(74)35-21-22-43(72)62-35/h32-42,45H,5-31,57H2,1-4H3,(H,61,74)(H,62,72)(H,63,73)(H,64,76)(H,65,77)(H,66,75)(H,83,84)(H4,58,59,60)
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| Chemical Name |
1-[1-[2-[[6-amino-2-[[1-[5-(diaminomethylideneamino)-2-[[1-[1-[4-methyl-2-[[2-[(5-oxopyrrolidine-2-carbonyl)amino]acetyl]amino]pentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxylic 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 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: 100 mg/mL (84.57 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 | 0.8457 mL | 4.2287 mL | 8.4573 mL | |
| 5 mM | 0.1691 mL | 0.8457 mL | 1.6915 mL | |
| 10 mM | 0.0846 mL | 0.4229 mL | 0.8457 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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