| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
C3a (70-77) TFA targets the complement C3a receptor (C3aR), a G protein-coupled receptor expressed on mast cells, smooth muscle cells, and leukocytes. It mimics the full C3a protein by binding to cellular C3a binding sites, exhibiting 1-2% of the biologic activity. The octapeptide induces histamine release and degranulation of rat mast cells, promotes contraction of guinea pig ileal tissue, and enhances vascular permeability in human skin.
|
|---|---|
| ln Vitro |
Human mononuclear leukocytes in culture that are directly interacting with C3a(70–77) exhibit concentration-dependent suppression of the synthesis of LIF elicited by mitogens and the antigen SK-SD[1]. C3a(70–77) increases vascular permeability in human skin, stimulates contraction of guinea pig ileal tissue, and causes histamine release and degranulation of rat mast cells. Ileal smooth muscle is desensitized to C3a(70–77) but not to human C5a, a similar anaphylatoxin. Cross-desensitization suggests that C3a(70–77) interacts with cellular C3a binding sites in a particular way[2].
In vitro, C3a (70-77) TFA induces histamine release and degranulation of rat mast cells, promotes contraction of guinea pig ileal tissue, and enhances vascular permeability in human skin. The direct interaction of C3a (70-77) with human mononuclear leukocytes in culture results in a concentration-dependent inhibition of the generation of LIF evoked by mitogens and by the antigen SK-SD. It selectively desensitizes ileal smooth muscle to C3a but not to human C5a. |
| ln Vivo |
C3a (70-77) TFA induces histamine release and degranulation of rat mast cells, promotes contraction of guinea pig ileal tissue, and enhances vascular permeability in human skin. It is used to study complement-mediated inflammatory responses in various ex vivo and in vivo models. The cross-desensitization indicating specific interaction of C3a (70-77) with cellular C3a binding sites is also observed in functional assays. Further in vivo activity is described in the literature.
|
| Enzyme Assay |
Binding of C3a (70-77) TFA to the C3a receptor is assessed using radioligand binding assays on membrane preparations from cells expressing recombinant C3aR or from RBL-2H3 cells. Various concentrations of the peptide are incubated with a labeled C3a tracer. After incubation, bound and free radioligands are separated by filtration, and radioactivity is measured to calculate IC₅0 or Ki values. The specificity of binding can be confirmed by cross-desensitization assays, showing that C3a (70-77) desensitizes responses to C3a but not to C5a.
|
| Cell Assay |
Functional cellular assays for C3a (70-77) TFA utilize rat peritoneal mast cells, guinea pig ileal strips, or human mononuclear leukocytes. Mast cells are treated with various concentrations of the peptide, and histamine release is measured in the supernatant by ELISA or fluorometric assay. For ileal contraction assays, guinea pig ileum segments are mounted in an organ bath, and contraction force is measured upon peptide addition. For vascular permeability studies, the peptide is injected intradermally into human skin or animal models, and extravasation of Evans blue dye is measured.
|
| Animal Protocol |
In vivo animal studies for C3a (70-77) TFA are performed in guinea pigs and rats. For the contraction assay, guinea pig ileal tissue is mounted in an organ bath, and the peptide is added to measure contraction. For vascular permeability, the peptide is administered intradermally into guinea pig or rat skin, and Evans blue dye is injected intravenously. The extent of dye extravasation into the skin (blue spot area and intensity) is quantified as a measure of increased vascular permeability. Cross-desensitization experiments can be performed by pre-exposing tissues to the peptide and then challenging with C3a to assess desensitization.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for C3a (70-77) TFA are not detailed in standard product literature. As an 8-amino acid peptide (octapeptide), its half-life in vivo is extremely short (minutes) due to rapid degradation by serum peptidases. It is not orally bioavailable and is typically administered intradermally, intraperitoneally, or used in ex vivo tissue bath experiments. The TFA salt form enhances solubility for biochemical and pharmacological assays. Comprehensive PK studies would be required for in vivo applications.
|
| Toxicity/Toxicokinetics |
Comprehensive toxicological data for C3a (70-77) TFA are not provided in standard product literature. As an octapeptide mimicking a fragment of the complement protein C3a, it is generally well-tolerated at research-use concentrations. Potential effects at high doses include excessive histamine release leading to hypotensive responses, and increased vascular permeability. For laboratory use, standard chemical safety precautions for handling peptides should be followed.
|
| References | |
| Additional Infomation |
C3a (70-77) TFA (Complement 3a (70-77) TFA) has the molecular formula C3₇H₆2F3N13O12 and a molecular weight of 937.96. The peptide sequence is Ala-Ser-His-Leu-Gly-Leu-Ala-Arg (ASHLGLAR). It appears as a white to off-white solid powder. The compound is stored at -20degC or -80degC, sealed, and away from moisture. It is soluble in water at 100 mg/mL and in PBS. It exhibits 1-2% of the biologic activity of full C3a. The product is for research use only.
|
| Molecular Formula |
C37H62F3N13O12
|
|---|---|
| Molecular Weight |
937.96
|
| Related CAS # |
C3a (70-77);63555-63-5
|
| Appearance |
Solid powder
|
| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O :~100 mg/mL (~106.61 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (106.61 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0661 mL | 5.3307 mL | 10.6614 mL | |
| 5 mM | 0.2132 mL | 1.0661 mL | 2.1323 mL | |
| 10 mM | 0.1066 mL | 0.5331 mL | 1.0661 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
