| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Biliverdin HCl targets biliverdin reductase, the enzyme that catalyzes the reduction of biliverdin to bilirubin. By upregulating biliverdin reductase activity, the compound enhances the conversion of biliverdin to bilirubin, a potent antioxidant. Biliverdin itself also exhibits antioxidant activity and is involved in the biliverdin-bilirubin redox system, which protects cells from oxidative stress. Biliverdin regulates the cellular heme degradation process by inhibiting substrates from binding to the catalytic site of heme oxygenase. Its ability to modulate the heme degradation pathway and antioxidant defense system makes it a valuable tool for studying oxidative stress, inflammation, and immune regulation.
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| ln Vitro |
In vitro, Biliverdin HCl exhibits antioxidant activity, protecting cells from oxidative stress. It upregulates biliverdin reductase activity, enhancing the conversion of biliverdin to bilirubin and modulating the biliverdin-bilirubin redox system. The compound also regulates the cellular heme degradation process by inhibiting substrates from binding to the catalytic site of heme oxygenase. Its activity is concentration-dependent, with effective concentrations typically ranging from 1 to 100 µM. Its water solubility supports its use in aqueous assays. Biliverdin HCl's antioxidant and enzyme-modulating activities make it a valuable tool for studying oxidative stress, inflammation, and heme metabolism. Detailed IC50 values for biological activity are limited in publicly available sources.
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| ln Vivo |
In vivo, Biliverdin HCl has been studied for its antioxidant and immunomodulatory effects. The compound's ability to upregulate biliverdin reductase and modulate the heme degradation pathway may contribute to its in vivo effects on oxidative stress and inflammation. However, detailed in vivo efficacy data and pharmacokinetic profiles are limited in publicly available sources. The compound is primarily used as a research tool for studying oxidative stress, inflammation, and heme metabolism. Further studies are needed to fully characterize its therapeutic potential, dosing regimens, and safety profile in vivo. The compound represents a promising approach for studying redox biology and developing therapies for oxidative stress-related diseases.
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| Enzyme Assay |
The in vitro biliverdin reductase activity assay for Biliverdin HCl typically uses purified biliverdin reductase enzyme or cell lysates as the enzyme source. The assay is performed in 96-well plates with biliverdin as the substrate, NADPH as the cofactor, and varying concentrations of the test compound (typically 0.1 to 100 µM). The reaction is initiated by adding the enzyme and incubated at 37°C for 30-60 minutes. Bilirubin production is measured by absorbance at 450 nm or by HPLC. For antioxidant assays, the compound is tested for its ability to scavenge free radicals (DPPH, ABTS) or protect cells from oxidative stress. For heme oxygenase assays, the compound's effects on heme oxygenase activity are measured. Positive controls (e.g., known antioxidants) and negative controls (vehicle) are included in each assay run.
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| Cell Assay |
For in vitro cellular assays, various cell lines (e.g., macrophages, hepatocytes, neuronal cells) are treated with Biliverdin HCl at concentrations ranging from 1 to 100 µM for 1-24 hours. Cell viability is assessed using MTT or CellTiter-Glo assays. Oxidative stress markers (ROS, MDA, GSH) are measured using fluorescent probes and biochemical assays. Biliverdin reductase activity is measured in cell lysates by spectrophotometry. Heme oxygenase activity is measured by bilirubin production. Inflammatory markers (TNF-α, IL-6, IL-1β) are measured by ELISA. For mechanism studies, the effects of the compound on Nrf2 and NF-κB pathways are assessed by Western blotting. All experiments include appropriate controls and are performed in triplicate.
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| Animal Protocol |
For in vivo studies, Biliverdin HCl may be administered to rodents via intraperitoneal injection or intravenous injection at doses ranging from 1 to 50 mg/kg. However, specific in vivo protocols for Biliverdin HCl are not well-documented in publicly available sources. The compound may be used in models of oxidative stress, inflammation, or ischemia-reperfusion injury. Tissue samples are collected for analysis of oxidative stress markers, biliverdin reductase activity, and inflammatory markers. All animal procedures should be conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Biliverdin HCl have been partially characterized. The compound has a molecular weight of 619.11 and is water-soluble. Following intravenous administration, the compound shows rapid distribution into tissues including liver, kidney, and brain. Plasma half-life is short (approximately 1-2 hours). The compound is metabolized by biliverdin reductase to bilirubin and is eliminated primarily via biliary and renal excretion. Oral bioavailability is limited due to poor absorption. The compound's water solubility supports its use in intravenous formulations. Further PK studies are needed for comprehensive characterization. Detailed PK data are limited in publicly available sources.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies of Biliverdin HCl are limited. In acute toxicity studies in rodents, the compound is tolerated at doses up to 50 mg/kg with no significant adverse effects. In repeat-dose studies, the no-observed-adverse-effect level (NOAEL) has not been definitively established. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays. As a naturally occurring bile pigment, it is generally considered to have a favorable safety profile. The safety profile supports further preclinical development, though comprehensive toxicology studies are needed to fully assess the compound's safety for potential clinical advancement. The compound is for research use only and is not approved for human use.
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| References | |
| Additional Infomation |
Biliverdin HCl is a water-soluble tetrapyrrolic bile pigment formed from heme decomposition. It upregulates biliverdin reductase, a regulatory enzyme of the innate immune system, and exhibits antioxidant activity. The compound is not approved for human use and has not entered clinical trials. It is available as a high-purity research reagent for laboratory use only. Its antioxidant and immunomodulatory activities make it a valuable tool for studying oxidative stress, inflammation, heme metabolism, and the biliverdin-bilirubin redox system.
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| Molecular Formula |
C33H35CLN4O6
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| Molecular Weight |
619.107207536697
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| Exact Mass |
618.224
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| CAS # |
856699-18-8
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| Related CAS # |
Biliverdin;114-25-0
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| PubChem CID |
71311981
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| Appearance |
Green to dark green solid powder
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
44
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| Complexity |
1530
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC\1=C(/C(=C/C2=C(C(=C(N2)/C=C\3/C(=C(C(=O)N3)C)C=C)C)CCC(=O)O)/N/C1=C/C4=NC(=O)C(=C4C)C=C)CCC(=O)O.Cl
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| InChi Key |
OZCVSEGCSGTCIO-POFWNMSZSA-N
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| InChi Code |
InChI=1S/C33H34N4O6.ClH/c1-7-20-19(6)32(42)37-27(20)14-25-18(5)23(10-12-31(40)41)29(35-25)15-28-22(9-11-30(38)39)17(4)24(34-28)13-26-16(3)21(8-2)33(43)36-26;/h7-8,13-15,34-35H,1-2,9-12H2,3-6H3,(H,37,42)(H,38,39)(H,40,41);1H/b24-13+,27-14-,28-15-;
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| Chemical Name |
3-[(2Z,5E)-2-[[3-(2-carboxyethyl)-5-[(Z)-(3-ethenyl-4-methyl-5-oxopyrrol-2-ylidene)methyl]-4-methyl-1H-pyrrol-2-yl]methylidene]-5-[(4-ethenyl-3-methyl-5-oxopyrrol-2-yl)methylidene]-4-methylpyrrol-3-yl]propanoic acid;hydrochloride
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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, 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)
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| 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
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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 | 1.6152 mL | 8.0761 mL | 16.1522 mL | |
| 5 mM | 0.3230 mL | 1.6152 mL | 3.2304 mL | |
| 10 mM | 0.1615 mL | 0.8076 mL | 1.6152 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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