TC LPA5 4
Based on 1 Customer Validation
TC LPA5 4 is a LPA5 (GPR92)-specific non-lipid antagonist. TC LPA5 4 inhibits LPA-induced aggregation of isolated human platelet (LPA5-RH7777 cell line) with an IC50 of 800 nM. TC LPA5 4 displays selectivity for LPA5 over 80 other screened agent targets. TC LPA5 4 inhibits cell proliferation and migration of thyroid cancer cells.
For research use only. We do not sell to patients.
- Purity: 99.69%
- CAS No.: 1393814-38-4
- Formula: C23H23ClN2O3
- Molecular Weight:410.89
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RH7777 | IC50 |
0.8 μM
Compound: 4
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Antagonist activity at human recombinant LPA5 receptor expressed in rat RH7777 cells assessed as inhibition of hexadecyl-LPA-induced effect
Antagonist activity at human recombinant LPA5 receptor expressed in rat RH7777 cells assessed as inhibition of hexadecyl-LPA-induced effect
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[PMID: 22801643] |
TC LPA5 4 inhibits the proliferation on thyroid cancer cells CGTH-W3, TPC-1, B-CAPAP, and BHT101 significantly with IC50 at 103.0 μM, 84.9 μM, 55.9μM, and 57.17 μM. TC LPA5 4 (5 μM; 24 hours) significantly inhibits LPA-stimulated migration of CGTH-W3 and TPC-1 cells, with an inhibitory rate of ~ 30%.? B-CPAP and BHT101 cells expressed higher LPAR5 mRNA. TC LPA5 4 inhibits these two cell lines’ proliferations with IC50 at 55.9μM and 57.17 μM. CGTH-W3 and TPC-1 cells expressed lower LPAR5 mRNA. TC LPA5 4 displays differential antitumor activity with IC50 at 103.0 μM and 84.9 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/C nu/nu mice, aged 4 5 weeks (CGTH-W3 xenografts) [2]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection; 5 days/week for 2 weeks
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Result:Significantly inhibits CGTH-W3 xenograft growth with inhibitory rates of 46.7%.
Chemical Information
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CAS No. 1393814-38-4
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Appearance Solid
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Molecular Weight 410.89
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Formula C23H23ClN2O3
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Color Light yellow to yellow
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SMILES
O=C(C1=NN(C2=CC=CC(OC)=C2)C(C3=CC=C(C4CCCCC4)C(Cl)=C3)=C1)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 62.5 mg/mL (152.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.06 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Kozian DH, et al. Selective non-lipid modulator of LPA5 activity in human platelets. Bioorg Med Chem Lett. 2012;22(16):5239-5243. [Content Brief]
[2]. Zhao WJ, et al. LPAR5 promotes thyroid carcinoma cell proliferation and migration by activating class IA PI3K catalytic subunit p110β. Cancer Sci. 2021;112(4):1624-1632. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4337 mL | 12.1687 mL | 24.3374 mL | 60.8435 mL |
| 5 mM | 0.4867 mL | 2.4337 mL | 4.8675 mL | 12.1687 mL | |
| 10 mM | 0.2434 mL | 1.2169 mL | 2.4337 mL | 6.0844 mL | |
| 15 mM | 0.1622 mL | 0.8112 mL | 1.6225 mL | 4.0562 mL | |
| 20 mM | 0.1217 mL | 0.6084 mL | 1.2169 mL | 3.0422 mL | |
| 25 mM | 0.0973 mL | 0.4867 mL | 0.9735 mL | 2.4337 mL | |
| 30 mM | 0.0811 mL | 0.4056 mL | 0.8112 mL | 2.0281 mL | |
| 40 mM | 0.0608 mL | 0.3042 mL | 0.6084 mL | 1.5211 mL | |
| 50 mM | 0.0487 mL | 0.2434 mL | 0.4867 mL | 1.2169 mL | |
| 60 mM | 0.0406 mL | 0.2028 mL | 0.4056 mL | 1.0141 mL | |
| 80 mM | 0.0304 mL | 0.1521 mL | 0.3042 mL | 0.7605 mL | |
| 100 mM | 0.0243 mL | 0.1217 mL | 0.2434 mL | 0.6084 mL |
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