| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Bradykinin B2 Receptor (B2R) Human Endogenous Metabolite
|
|---|---|
| ln Vitro |
Bradykinin acetate is a potent vasodilator peptide that exerts its vasodilatory effects by stimulating specific endothelial B2 receptors, leading to the release of prostacyclin, NO, and EDHF[1]. Bradykinin acetate is involved in the progression of multiple cancers. Bradykinin acetate treatment promotes the invasion and migration of colorectal cancer cells. Bradykinin acetate treatment stimulates ERK1/2 activation and IL-6 production[2]. Exogenous bradykinin acetate significantly inhibited LPS-induced TF expression at both mRNA and protein levels in a dose-dependent manner. NO synthase antagonist L-NAME and PI3K inhibitor LY294002 significantly abolished the inhibitory effect of bradykinin acetate on tissue factor expression[3].
|
| ln Vivo |
Application of 1 μM bradykinin acetate to the ovaries resulted in significant reductions in heart rate and mean arterial pressure. In vagotomized animals, application of 1 μM bradykinin acetate to the ovaries produced bradycardia and hypotension similar to responses induced when vagal innervation is intact [4]. Vascular bradykinin acetate improves pancreatic microcirculation and hemorheology in rats with severe acute pancreatitis. At 48 h, the pancreatic microcirculatory blood flow and flow rate in the bradykinin acetate-treated group gradually increased [5]. Activation of the PI3K/Akt signaling pathway induced by Bradykinin acetate administration reduced the activities of GSK-3β and MAPK, and reduced the NF-x03BA;B level in the nucleus, thereby inhibiting TF expression. Consistent with this, intraperitoneal injection of Bradykinin in C57/BL6 mice can also inhibit thrombosis caused by ligation of the inferior vena cava [3].
|
| References |
|
| Molecular Formula |
C50H73N15O11.XC2H4O2
|
|---|---|
| Molecular Weight |
1016.21 (free base)
|
| Exact Mass |
1059.561
|
| CAS # |
6846-03-3
|
| PubChem CID |
91886389
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.5±0.1 g/cm3
|
| Index of Refraction |
1.693
|
| LogP |
-0.82
|
| Hydrogen Bond Donor Count |
13
|
| Hydrogen Bond Acceptor Count |
16
|
| Rotatable Bond Count |
27
|
| Heavy Atom Count |
80
|
| Complexity |
2110
|
| Defined Atom Stereocenter Count |
8
|
| SMILES |
OC[C@@H](C(N1CCC[C@H]1C(N[C@H](C(N[C@H](C(O)=O)CCCNC(N)=N)=O)CC2=CC=CC=C2)=O)=O)NC([C@@H](NC(CNC([C@@H]3CCCN3C([C@@H]4CCCN4C([C@@H](N)CCCNC(N)=N)=O)=O)=O)=O)CC5=CC=CC=C5)=O.CC(O)=O
|
| InChi Key |
VIGBULRGBBKXHS-MIEKKPBHSA-N
|
| InChi Code |
InChI=1S/C50H73N15O11.C2H4O2/c51-32(16-7-21-56-49(52)53)45(72)65-25-11-20-39(65)47(74)64-24-9-18-37(64)43(70)58-28-40(67)59-34(26-30-12-3-1-4-13-30)41(68)62-36(29-66)46(73)63-23-10-19-38(63)44(71)61-35(27-31-14-5-2-6-15-31)42(69)60-33(48(75)76)17-8-22-57-50(54)55;1-2(3)4/h1-6,12-15,32-39,66H,7-11,16-29,51H2,(H,58,70)(H,59,67)(H,60,69)(H,61,71)(H,62,68)(H,75,76)(H4,52,53,56)(H4,54,55,57);1H3,(H,3,4)/t32-,33-,34-,35-,36-,37-,38-,39-;/m0./s1
|
| Chemical Name |
acetic acid;(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[2-[[(2S)-1-[(2S)-1-[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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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