| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
LPA2 (lysophosphatidic acid receptor 2). EC50 = 100 nM.
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| ln Vitro |
DBIBB is a specific non-lipid agonist of LPA2. It activates LPA2 signaling with an EC50 of 100 nM. Activation of LPA2 mitigates gastrointestinal radiation syndrome, increases intestinal crypt survival and enterocyte proliferation, and reduces apoptosis. It dose-dependently attenuates radiation-induced DNA damage in mouse embryo fibroblasts (MEFs) expressing LPA2.
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| ln Vivo |
In vivo, DBIBB mitigates gastrointestinal and hematopoietic acute radiation syndrome. It increases intestinal crypt survival and enterocyte proliferation, and reduces apoptosis. It is a candidate active molecule for alleviating acute radiation syndrome induced by high-dose gamma rays.
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| Enzyme Assay |
DBIBB is evaluated in cell-free receptor binding assays using membrane preparations expressing LPA2. Radioligand binding displacement assays are performed to determine the affinity (EC50) of DBIBB for LPA2. Competition binding experiments are conducted with increasing concentrations of DBIBB and a fixed concentration of a labeled reference ligand.
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| Cell Assay |
DBIBB is assessed in cell-based functional assays using cells expressing LPA2. Calcium mobilization or other signaling assays are performed to measure receptor activation. Cells are treated with DBIBB, and LPA2-mediated signaling is measured. Radiation-induced DNA damage is assessed in MEFs expressing LPA2.
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| Animal Protocol |
DBIBB is administered in animal models of acute radiation syndrome to evaluate its protective effects. Efficacy is assessed by measuring intestinal crypt survival, enterocyte proliferation, apoptosis, and survival rates after radiation exposure. Pharmacokinetic studies are conducted to assess bioavailability and tissue distribution.
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| ADME/Pharmacokinetics |
No detailed PK data available. DBIBB has a molecular weight of 452.48. Soluble in DMSO.
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| Toxicity/Toxicokinetics |
No detailed toxicity data available. For research use only.
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| Additional Infomation |
DBIBB is a potent LPA2 agonist. Molecular formula: C23H20N2O6S; MW: 452.48. For research use only.
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| Molecular Formula |
C23H20N2O6S
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|---|---|
| Molecular Weight |
452.479704856873
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| Exact Mass |
452.104
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| CAS # |
1569309-92-7
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| PubChem CID |
73296092
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
710.4±70.0 °C at 760 mmHg
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| Flash Point |
383.5±35.7 °C
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| Vapour Pressure |
0.0±2.4 mmHg at 25°C
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| Index of Refraction |
1.670
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| LogP |
2.44
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
32
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| Complexity |
808
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1C=CC=CC=1C(=O)O)(NCCCCN1C(C2=CC=CC3=CC=CC(C1=O)=C23)=O)(=O)=O
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| InChi Key |
POLJNARIJSROOS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H20N2O6S/c26-21-17-10-5-7-15-8-6-11-18(20(15)17)22(27)25(21)14-4-3-13-24-32(30,31)19-12-2-1-9-16(19)23(28)29/h1-2,5-12,24H,3-4,13-14H2,(H,28,29)
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| Chemical Name |
2-[4-(1,3-dioxobenzo[de]isoquinolin-2-yl)butylsulfamoyl]benzoic 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 |
| 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) |
DMSO : ≥ 100 mg/mL (~221.00 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 | 2.2100 mL | 11.0502 mL | 22.1004 mL | |
| 5 mM | 0.4420 mL | 2.2100 mL | 4.4201 mL | |
| 10 mM | 0.2210 mL | 1.1050 mL | 2.2100 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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