| 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 |
ASP6432 targets the lysophosphatidic acid receptor 1 (LPA1). It is a potent antagonist with IC50 values of 11 nM for the human LPA1 receptor and 30 nM for the rat LPA1 receptor.
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|---|---|
| ln Vitro |
LPA-induced proliferation of human prostate stromal cells is inhibited by ASP6432 [1].
In vitro, ASP6432 inhibits the LPA-induced proliferation of human prostate stromal cells. This demonstrates its functional antagonism of the LPA1 receptor in a cell-based model. |
| ln Vivo |
In vivo activity data for ASP6432 is not detailed in the available literature. As a potent and selective LPA1 antagonist, its in vivo effects would be related to the physiological and pathological roles of the LPA1 receptor, which is involved in various processes including fibrosis, cancer, and pain.
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| Enzyme Assay |
The binding affinity and potency of ASP6432 are determined using radioligand binding or functional assays. The IC50 values of 11 nM (human) and 30 nM (rat) were established in such assays, demonstrating its high potency.
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| Cell Assay |
The functional activity of ASP6432 is assessed in cell-based assays. One such assay measures the compound's ability to inhibit LPA-induced proliferation of human prostate stromal cells. This confirms its role as a functional antagonist at the LPA1 receptor.
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| Animal Protocol |
Specific in vivo animal models are not detailed. Given its antagonism of LPA1, relevant models would include those for fibrosis (e.g., pulmonary or renal fibrosis), cancer metastasis, and neuropathic pain, where the LPA1 receptor is known to play a significant role.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties for ASP6432 are not detailed in the available literature. As a small molecule antagonist, its properties would typically be characterized by standard ADME studies to determine its suitability for in vivo use.
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| Toxicity/Toxicokinetics |
Specific toxicity data for ASP6432 is not provided. As a research compound, its safety profile would be assessed in the context of its intended use, with standard toxicological evaluations being conducted if it were to be developed further.
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| References | |
| Additional Infomation |
A novel LPA1 antagonist
ASP6432 is a valuable research tool for studying the LPA1 receptor. Its high potency and selectivity make it useful for investigating the role of LPA1 signaling in various diseases, including cancer, fibrosis, and inflammation, and for validating LPA1 as a therapeutic target. |
| Molecular Formula |
C26H32KN4O6S2
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|---|---|
| Molecular Weight |
599.783784866333
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| Exact Mass |
598.132
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| CAS # |
1282549-08-9
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| PubChem CID |
138454774
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
39
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| Complexity |
857
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[K].S1C=C(C(NS(NCC)(=O)=O)=O)N=C1CN(C(C1C=C(C(C)=C(C=1)OC)OC)=O)CCCC1C=CC=CC=1
|
| InChi Key |
WKYBXXHNGOTYDD-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C26H32N4O6S2.K/c1-5-27-38(33,34)29-25(31)21-17-37-24(28-21)16-30(13-9-12-19-10-7-6-8-11-19)26(32)20-14-22(35-3)18(2)23(15-20)36-4;/h6-8,10-11,14-15,17,27H,5,9,12-13,16H2,1-4H3,(H,29,31);/q;+1/p-1
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| Chemical Name |
potassium;[2-[[(3,5-dimethoxy-4-methylbenzoyl)-(3-phenylpropyl)amino]methyl]-1,3-thiazole-4-carbonyl]-(ethylsulfamoyl)azanide
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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 : ~250 mg/mL (~417.52 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 4.17 mg/mL (6.96 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 41.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 4.17 mg/mL (6.96 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 41.7 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6673 mL | 8.3364 mL | 16.6728 mL | |
| 5 mM | 0.3335 mL | 1.6673 mL | 3.3346 mL | |
| 10 mM | 0.1667 mL | 0.8336 mL | 1.6673 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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