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LPA5-IN-4

Alias: LPA5IN4, TC-LPA5-4; LPA5-IN4; LPA5-IN-4
Cat No.:V24437 Purity: ≥98%
TC LPA5 4 is a specific non-lipid LPA5 (GPR92) antagonist.
LPA5-IN-4
LPA5-IN-4 Chemical Structure CAS No.: 1393814-38-4
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
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5mg
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Product Description
TC LPA5 4 is a specific non-lipid LPA5 (GPR92) antagonist. TC LPA5 4 inhibits LPA-induced aggregation of isolated human platelets (LPA5-RH7777 cell line) with IC50 of 800 nM. TC LPA5 4 is selective for LPA5 over 80 other screened active molecular targets. TC LPA5 4 suppresses the proliferation/growth and migration of thyroid cancer/tumor cells.
Biological Activity I Assay Protocols (From Reference)
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].
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].
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%.
References

[1]. Selective non-lipid modulator of LPA5 activity in human platelets. Bioorg Med Chem Lett. 2012;22(16):5239-5243.

[2]. LPAR5 promotes thyroid carcinoma cell proliferation and migration by activating class IA PI3K catalytic subunit p110β. Cancer Sci. 2021;112(4):1624-1632.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H23CLN2O3
Molecular Weight
410.898
Exact Mass
410.14
CAS #
1393814-38-4
PubChem CID
66552906
Appearance
Light yellow to yellow solid powder
LogP
5.947
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
5
Heavy Atom Count
29
Complexity
556
Defined Atom Stereocenter Count
0
InChi Key
BNALUYKEGYUHQC-UHFFFAOYSA-N
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)
Chemical Name
5-(3-chloro-4-cyclohexylphenyl)-1-(3-methoxyphenyl)pyrazole-3-carboxylic acid
Synonyms
LPA5IN4, TC-LPA5-4; LPA5-IN4; LPA5-IN-4
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO : ~62.5 mg/mL (~152.11 mM)
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.

Calculator

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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