| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| Other Sizes |
| Targets |
Girinimbine targets multiple pathways involved in inflammation, cancer, and infection. It induces apoptosis in cancer cells through mechanisms involving chromatin condensation and DNA damage. The compound exhibits anti-inflammatory activity by suppressing the production of inflammatory mediators. It also shows antibacterial activity, antiplatelet activity, and antitrypanosomal activity. Girinimbine has a molecular formula of C₁₈H₁₇NO and a molecular weight of 263.3 g/mol.
|
|---|---|
| ln Vitro |
Girinimbine (1-400 µM; 24-72 h) has IC50 values of 61 µM, 56 µM, and 40 µM, respectively, and reduces the viability of HepG2 cells in 24, 48, and 72 hours. Girinimbine (10–100 µM; 24-48 h) increases LDH leakage in HepG2 cells in a manner that is dependent on both concentration and time[1]. HepG2 cells treated with girinimbine (56 µM; 24-48 h) exhibit DNA fragmentation and increased caspase-3 levels[1]. Additionally, girinimbine (56 µM; 12-48 h) treatment induced G0/G1-phase arrest and showed a time-dependent buildup of the Sub-G0/G1 peak (hypodiploid)[1]. Girinimbine has a 10.16 µg/mL IC50 value, indicating strong antitrypanosomal activity[3].
In vitro, Girinimbine demonstrates potent anticancer activity by inducing apoptosis in cancer cells. It inhibits tumor growth in various cancer cell lines. The compound exhibits anti-inflammatory effects by suppressing the production of pro-inflammatory mediators such as IL-1β and TNF-α. It also shows antibacterial activity, antioxidant activity, and antiplatelet activity. These diverse in vitro activities support its potential as a multi-target therapeutic agent. |
| ln Vivo |
Girinimbine (10–100 mg/kg; orally gavage; once) is a pretreatment that reduces pro-inflammatory cytokine (TNF-α, IL-1β) levels in the peritoneal fluid and helps limit total leukocyte migration[2]. Girinimbine (20 μg/mL; 24 hours) significantly changes the location of apoptotic cells in zebrafish embryos in vivo[2].
In vivo, Girinimbine demonstrates significant anti-inflammatory activity. In mouse models, pretreatment with Girinimbine (10-100 mg/kg, oral gavage, once) limits total leukocyte migration and reduces pro-inflammatory cytokine (IL-1β, TNF-α) levels in peritoneal fluid. The compound also inhibits tumor growth in vivo. These results support its potential for treating inflammatory diseases and cancer. |
| Enzyme Assay |
The in vitro apoptosis assay for Girinimbine is conducted in cancer cell lines. Cells are treated with varying concentrations of the compound for 24-72 hours. Apoptosis is measured by flow cytometry using Annexin V/PI staining, caspase activity assays, and detection of DNA fragmentation. Anti-inflammatory activity is assessed in immune cells by measuring the production of pro-inflammatory cytokines such as IL-1β and TNF-α following stimulation. Antibacterial activity is evaluated using standard broth microdilution assays.
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: HepG2 cells Tested Concentrations: 1 µM, 10 µM, 50 µM, 100 µM, 200 µM Incubation Duration: 24 h, 48 h and 72 h Experimental Results: Inhibited the proliferation of HepG2 cells in vitro in a dose- and time-dependent manner. Apoptosis Analysis[1] Cell Types: HepG2 cells Tested Concentrations: 56 µM Incubation Duration: 24 h, 48 h Experimental Results: demonstrated typical morphological features of apoptosis. Cell Cycle Analysis[1] Cell Types: HepG2 cells Tested Concentrations: 56 µM Incubation Duration: 12 h, 24 h, 48 h Experimental Results: Induced G0/G1-phase arrest in HepG2 cells. Cellular assays for Girinimbine are conducted in cancer cell lines and immune cells. Cells are treated with varying concentrations of the compound for 24-72 hours. Cell viability and proliferation are measured using standard assays such as MTT or CellTiter-Glo. Apoptosis is assessed by flow cytometry, caspase activity, and DNA fragmentation. Cytokine production is measured by ELISA or Luminex in stimulated immune cells. Antibacterial activity is assessed by determining minimum inhibitory concentrations (MICs). |
| Animal Protocol |
Animal/Disease Models: Male ICR mice (25-35 g) treated with carrageenan[2]
Doses: 10 mg/kg, 30 mg/kg, and 100 mg/kg Route of Administration: Orally gavage; once Experimental Results: Helped limit total leukocyte migration, and diminished pro-inflammatory cytokine levels in the peritoneal fluid . In vivo studies for Girinimbine are conducted in mouse models of inflammation. The compound is administered orally at doses of 10-100 mg/kg as a single dose pretreatment. After stimulation (e.g., with inflammatory agents), leukocyte migration is quantified in peritoneal fluid, and pro-inflammatory cytokine levels (IL-1β, TNF-α) are measured by ELISA. For antitumor studies, xenograft models are used with tumor growth inhibition assessed over time. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for Girinimbine is not extensively reported in publicly available sources. The compound has a molecular weight of 263.3 g/mol and a molecular formula of C₁₈H₁₇NO. As a carbazole alkaloid, it is expected to have moderate oral bioavailability. Detailed PK parameters such as half-life, clearance, and volume of distribution are not available in the current literature for this natural product.
|
| Toxicity/Toxicokinetics |
Toxicity data for Girinimbine is limited in publicly available sources. In mouse studies, the compound was administered at doses up to 100 mg/kg without reported significant adverse effects. As with all research compounds, Girinimbine is intended for research use only and not for human therapeutic applications. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment.
|
| References |
|
| Additional Infomation |
Girinimbine belongs to the carbazole class of compounds and is a metabolite. It has been reported to exist in Murraya paniculata, Osmanthus fragrans, and other organisms with relevant data.
Girinimbine is a carbazole alkaloid isolated from Murraya and Clausena species that exhibits anti-inflammatory, analgesic, antibacterial, antioxidant, and antitumor activities. It induces apoptosis in cancer cells and inhibits tumor growth in vitro and in vivo. The compound shows anti-inflammatory effects by suppressing IL-1β and TNF-α production and reduces leukocyte migration in vivo. Girinimbine has a molecular formula of C₁₈H₁₇NO and a molecular weight of 263.3 g/mol. |
| Molecular Formula |
C18H17NO
|
|---|---|
| Molecular Weight |
263.33
|
| Exact Mass |
263.131
|
| CAS # |
23095-44-5
|
| PubChem CID |
96943
|
| Appearance |
Off-white to light yellow solid powder
|
| Density |
1.187g/cm3
|
| Boiling Point |
450ºC at 760mmHg
|
| Melting Point |
175 °C
|
| Flash Point |
161.5ºC
|
| Vapour Pressure |
7.27E-08mmHg at 25°C
|
| Index of Refraction |
1.68
|
| LogP |
4.813
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
1
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
20
|
| Complexity |
416
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
GAEQWKVGMHUUKO-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C18H17NO/c1-11-10-14-12-6-4-5-7-15(12)19-16(14)13-8-9-18(2,3)20-17(11)13/h4-10,19H,1-3H3
|
| Chemical Name |
3,3,5-trimethyl-11H-pyrano[3,2-a]carbazole
|
| 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 (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)
|
| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7975 mL | 18.9876 mL | 37.9752 mL | |
| 5 mM | 0.7595 mL | 3.7975 mL | 7.5950 mL | |
| 10 mM | 0.3798 mL | 1.8988 mL | 3.7975 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
