| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
Targets lysophosphatidic acid receptor 1 (LPA1) as a potent agonist. LPA1 is a GPCR that plays critical roles in cell proliferation, migration, differentiation, and survival, and is involved in fibrosis, neuropathic pain, cancer progression, and embryonic development.
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| ln Vitro |
Activation of LPA1 by ONO-0740556 triggers Gi-dependent signaling pathways including inhibition of adenylate cyclase, activation of MAPK/ERK, PI3K/Akt, and Rho/ROCK pathways. At EC50=0.26 nM, it is one of the most potent synthetic LPA1 agonists reported, demonstrating high selectivity and efficacy in activating Gi-coupled signaling.
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| ln Vivo |
In vivo activity data for ONO-0740556 is not publicly available. The potency of this compound is demonstrated in vitro at EC50=0.26 nM. As an LPA1 agonist, it could be used in research models to investigate LPA1-mediated fibrotic, proliferative, or neuropathic pain processes, but no published animal studies are currently available.
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| Enzyme Assay |
Cell-free GTPgammaS binding assays are performed using membranes from CHO cells expressing human LPA1. Membranes (10 microg) are incubated in 20 mM HEPES buffer (pH 7.4) containing 100 mM NaCl, 5 mM MgCl2, 10 microM GDP, 0.1 nM [3⁵S]GTPgammaS, and increasing agonist concentrations (0.01 pM-1 microM) for 60 min at 30degC. Bound [3⁵S]GTPgammaS is separated by filtration through GF/B filters and counted.
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| Cell Assay |
Functional activity is assessed in CHO-K1 cells stably expressing human LPA1 using a calcium mobilization assay. Cells are loaded with Fluo-4 AM dye (4 microM) for 30 min at 37degC in HBSS buffer containing 20 mM HEPES. After washing, various concentrations of ONO-0740556 (0.001 pM-100 nM) are added, and fluorescence is measured. The EC50 is calculated from concentration-response curves. ONO-0740556 can also be evaluated in cell proliferation (MTT) and cell migration (Boyden chamber) assays.
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| Animal Protocol |
No specific animal studies have been reported for ONO-0740556. For an LPA1 agonist, potential in vivo models would include bleomycin-induced pulmonary fibrosis (to evaluate pro-fibrotic effects), spinal nerve ligation (for neuropathic pain studies), or cancer xenograft models. Standard routes of administration would be systemic (i.p. or s.c.) for small molecule agonists.
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| ADME/Pharmacokinetics |
Detailed PK data for ONO-0740556 is not publicly available. As a small molecule agonist (MW 415.46, purity ≥98%, white to off-white solid powder), it would be expected to have reasonable oral bioavailability and moderate clearance in preclinical species for a compound of this molecular weight.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available for ONO-0740556. As a potent LPA1 agonist, potential safety concerns may relate to off-target activation of LPA signaling pathways, which could promote cell proliferation, fibrosis, or cancer progression depending on the context. Standard safety pharmacology studies would be required for therapeutic development.
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| References | |
| Additional Infomation |
ONO-0740556 is a research chemical not approved for clinical use. It is a valuable tool compound for LPA1 receptor biology, particularly for studying the active conformation of LPA1 via its binding interactions with multiple extracellular loops and transmembrane domains. It may also have applications in research on fibrosis, neuropathic pain, and cancer, where LPA1 signaling is implicated.
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| Molecular Formula |
C20H34NO6P
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|---|---|
| Molecular Weight |
415.460827350616
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| Exact Mass |
415.212
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| CAS # |
2250210-69-4
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| PubChem CID |
141702624
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| Appearance |
White to off-white solid powder
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| LogP |
2.9
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
28
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| Complexity |
470
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1(CCCCC(N[C@H](CO)COP(O)(O)=O)=O)=CC=CC=C1CCCCCC
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| InChi Key |
LYWONSBDWRVEKO-LJQANCHMSA-N
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| InChi Code |
InChI=1S/C20H34NO6P/c1-2-3-4-5-10-17-11-6-7-12-18(17)13-8-9-14-20(23)21-19(15-22)16-27-28(24,25)26/h6-7,11-12,19,22H,2-5,8-10,13-16H2,1H3,(H,21,23)(H2,24,25,26)/t19-/m1/s1
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| Chemical Name |
[(2R)-2-[5-(2-hexylphenyl)pentanoylamino]-3-hydroxypropyl] dihydrogen phosphate
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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) |
DMSO: 75 mg/mL (180.52 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 | 2.4070 mL | 12.0349 mL | 24.0697 mL | |
| 5 mM | 0.4814 mL | 2.4070 mL | 4.8139 mL | |
| 10 mM | 0.2407 mL | 1.2035 mL | 2.4070 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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