| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Other Sizes |
| Targets |
Lysophosphatidic acid 2 (LPA2) receptor. H2L5186303 is a potent and specific antagonist of this receptor. It also shows activity against LPA3 and LPA1, but with significantly lower potency.
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|---|---|
| ln Vitro |
H2L5186303 is a potent LPA2 receptor antagonist with an IC50 of 9 nM in a calcium mobilization assay. It is highly selective for LPA2 over LPA3 (IC50 = 1230 nM) and LPA1 (IC50 = 27354 nM).
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| ln Vivo |
Specific in vivo activity data for H2L5186303 are not detailed in the available literature. As an LPA2 antagonist, it could have effects on various physiological processes, including cell proliferation, migration, and survival. However, specific animal model studies are not described.
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| Enzyme Assay |
The in vitro assay for LPA receptor antagonism involves measuring the inhibition of LPA-induced calcium mobilization in cells expressing the LPA2 receptor. Cells are loaded with a calcium-sensitive fluorescent dye and treated with LPA in the presence or absence of H2L5186303. The calcium flux is measured, and the IC50 is determined.
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| Cell Assay |
Specific in vitro cell-based assay protocols for H2L5186303 are not detailed. Its activity can be assessed in cells expressing LPA2 by measuring the inhibition of LPA-induced calcium mobilization. This is a functional cell-based assay.
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| Animal Protocol |
Specific in vivo animal model protocols for H2L5186303 are not described. To evaluate its in vivo activity, H2L5186303 could be administered to animal models of diseases where LPA2 plays a role, such as cancer or fibrosis. Endpoints would depend on the specific model.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for H2L5186303 are not reported in the available literature. As a research compound, its absorption, distribution, metabolism, and excretion (ADME) properties have not been extensively characterized.
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| Toxicity/Toxicokinetics |
Specific toxicological data for H2L5186303 are not available. As a research compound, its safety profile has not been comprehensively characterized. Toxicity studies would be required to determine its safety margin.
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| References | |
| Additional Infomation |
H2L5186303 is a research tool for studying LPA2 receptor function and its role in various physiological and pathological processes. Its high potency and selectivity make it a valuable compound for investigating LPA2 signaling. It is not an approved therapeutic agent.
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| Molecular Formula |
C26H20N2O6
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|---|---|
| Molecular Weight |
456.45
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| Exact Mass |
488.121
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| Elemental Analysis |
C, 63.93; H, 4.13; N, 5.74; O, 26.20
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| CAS # |
139262-76-3
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| PubChem CID |
90488981
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
801.0±65.0 °C at 760 mmHg
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| Flash Point |
438.2±34.3 °C
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| Vapour Pressure |
0.0±3.0 mmHg at 25°C
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| Index of Refraction |
1.688
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| LogP |
4.46
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
36
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| Complexity |
760
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC(/C=C\C(NC1=CC=C(OC2C=CC=C(OC3=CC=C(NC(/C=C\C(=O)O)=O)C=C3)C=2)C=C1)=O)=O
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| InChi Key |
HZFPOTBCYPWQSH-DZDAAMPGSA-N
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| InChi Code |
InChI=1S/C26H20N2O8/c29-23(12-14-25(31)32)27-17-4-8-19(9-5-17)35-21-2-1-3-22(16-21)36-20-10-6-18(7-11-20)28-24(30)13-15-26(33)34/h1-16H,(H,27,29)(H,28,30)(H,31,32)(H,33,34)/b14-12-,15-13-
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| Chemical Name |
(Z)-4-[4-[3-[4-[[(Z)-3-carboxyprop-2-enoyl]amino]phenoxy]phenoxy]anilino]-4-oxobut-2-enoic acid
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| Synonyms |
H2L-5186303; H2L 5186303; H2L5186303
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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 : ~250 mg/mL (~511.82 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 | 2.1908 mL | 10.9541 mL | 21.9082 mL | |
| 5 mM | 0.4382 mL | 2.1908 mL | 4.3816 mL | |
| 10 mM | 0.2191 mL | 1.0954 mL | 2.1908 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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