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| Targets |
LPA5-IN-4 targets the LPA5 receptor (also known as GPR92). It acts as a specific non-lipid antagonist of this receptor.
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| ln Vitro |
The proliferation of pancreatic islets CGTH-W3, TPC-1, B-CAPAP, and BHT101 was strongly suppressed by TC LPA5 4; the IC50 values were 103.0 μM, 84.9 μM, 55.9 μM, and 57.17 μM, respectively. TC LPA5 4 (5 μM; 24 hours) dramatically reduced LPA-stimulated TPC-1 and CGTH-W3 cell migration by approximately 30%. Higher levels of LPAR5 mRNA were expressed by B-CPAP and BHT101 cells. TC LPA5 4 reduces the proliferation of both cell lines with an IC50 of 55.9. Lower levels of LPAR5 mRNA are expressed by CGTH-W3 and TPC-1 cells. The anti-tumor effects of TC LPA5 4 are distinct, with IC50 values of 103.0 μM and 84.9 μM [2].
In vitro, TC LPA5 4 inhibits LPA-induced aggregation of isolated human platelets with an IC50 of 800 nM. It suppresses the proliferation and migration of thyroid cancer cells. It inhibits proliferation of thyroid cancer cell lines with IC50 values ranging from 55.9 to 103.0 μM. |
| ln Vivo |
For two weeks, TC LPA5 4 (10 mg/kg; i.p.; five days/week) inhibits the growth of CGTH-W3 xenografts in nude mice [2].
In vivo, TC LPA5 4 (10 mg/kg; i.p.; five days/week for two weeks) inhibits the growth of CGTH-W3 xenografts in nude mice with an inhibition rate of 46.7%. |
| Enzyme Assay |
In vitro receptor binding assays measure the displacement of a radiolabeled LPA5 ligand from membrane preparations. LPA5-IN-4 is incubated with membranes and a radioactive tracer, and the IC50 is determined. Functional assays measure the inhibition of LPA-induced platelet aggregation.
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| Cell Assay |
In vitro cellular assays evaluate the effects of LPA5-IN-4 on cell proliferation and migration. Thyroid cancer cell lines are treated with the compound, and proliferation is measured using MTT or similar assays. Migration is assessed using transwell assays.
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| Animal Protocol |
Animal/Disease Models: BALB/C nu/nu (nude) mice, 4 years and 5 weeks (CGTH-W3 xenograft) [2]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip) injection; 5 days per week for 2 weeks Experimental Results: Dramatically inhibited the growth of CGTH-W3 xenografts, with an inhibition rate of 46.7%. In vivo animal experiments are conducted in nude mice bearing CGTH-W3 xenografts. LPA5-IN-4 is administered intraperitoneally at 10 mg/kg, five days per week for two weeks. Tumor growth inhibition is measured. |
| ADME/Pharmacokinetics |
LPA5-IN-4 has a molecular formula of C17H12ClF3N2O4S and a molecular weight of 410.14. It has a CAS number of 1393814-38-4. The compound is a specific LPA5 antagonist. It should be protected from light.
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| Toxicity/Toxicokinetics |
The toxicity profile of LPA5-IN-4 is not well documented. As an LPA5 antagonist, its effects are related to modulation of lysophosphatidic acid signaling. Standard toxicological studies would be required for therapeutic development.
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| References | |
| Additional Infomation |
LPA5-IN-4 is a research tool used to study the role of LPA5 in platelet aggregation, cancer cell proliferation, and migration. It is a selective non-lipid modulator of LPA5 activity. It is also known as TC-LPA5-4.
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| Molecular Formula |
C23H23CLN2O3
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|---|---|
| Molecular Weight |
410.898
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| Exact Mass |
410.14
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| CAS # |
1393814-38-4
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| PubChem CID |
66552906
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
5.947
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
556
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC=CC(=C1)N2C(=CC(=N2)C(=O)O)C3=CC(=C(C=C3)C4CCCCC4)Cl
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| InChi Key |
BNALUYKEGYUHQC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H23ClN2O3/c1-29-18-9-5-8-17(13-18)26-22(14-21(25-26)23(27)28)16-10-11-19(20(24)12-16)15-6-3-2-4-7-15/h5,8-15H,2-4,6-7H2,1H3,(H,27,28)
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| Chemical Name |
5-(3-chloro-4-cyclohexylphenyl)-1-(3-methoxyphenyl)pyrazole-3-carboxylic acid
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| Synonyms |
LPA5IN4, TC-LPA5-4; LPA5-IN4; LPA5-IN-4
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~62.5 mg/mL (~152.11 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.06 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.06 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4337 mL | 12.1684 mL | 24.3368 mL | |
| 5 mM | 0.4867 mL | 2.4337 mL | 4.8674 mL | |
| 10 mM | 0.2434 mL | 1.2168 mL | 2.4337 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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