GRI977143 | CAS#325850-81-5 |LPA2 receptor Agonist

MedKoo Cat#: 531862 | Name: GRI977143

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

GRI977143 is a selective lysophosphatidic acid 2 (LPA2) receptor non-lipid agonist (EC50 = 3.3 μM). GRI977143 does not activate other LPA GPCRs at concentrations up to 10 μM.

Chemical Structure

GRI977143

CAS#325850-81-5

Theoretical Analysis

MedKoo Cat#: 531862

Name: GRI977143

CAS#: 325850-81-5

Chemical Formula: C22H17NO3S

Exact Mass: 375.0929

Molecular Weight: 375.44

Elemental Analysis: C, 70.38; H, 4.56; N, 3.73; O, 12.78; S, 8.54

Price and Availability

Size	Price	Availability
5mg	USD 350.00	2 Weeks
10mg	USD 600.00	2 Weeks
25mg	USD 1,050.00	2 Weeks

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Synonym

GRI977143; GRI-977143; GRI 977143.

IUPAC/Chemical Name

2-[3-(1,3-dioxobenzo[de]isoquinolin-2-yl)propylsulfanyl]benzaldehyde

InChi Key

IYUOFUODBWFCBK-UHFFFAOYSA-N

InChi Code

InChI=1S/C22H17NO3S/c24-14-16-6-1-2-11-19(16)27-13-5-12-23-21(25)17-9-3-7-15-8-4-10-18(20(15)17)22(23)26/h1-4,6-11,14H,5,12-13H2

SMILES Code

O=CC1=CC=CC=C1SCCCN(C(C2=CC=CC3=CC=CC4=C23)=O)C4=O

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

GRI977143 is a specific LPA2 receptor agonist, with an EC50 of 3.3 μM.

In vitro activity:

GRI (GRI977143) selectively protected LPA2 MEF cells and reduced caspase 9 activation by 37% ± 1% but was without any effect in the vector-transduced MEF cells. Reference: Biochim Biophys Acta. 2013 Jan;1831(1):117-25. https://pubmed.ncbi.nlm.nih.gov/23127512/

In vivo activity:

On the contrary, GRI977143 also inhibited inhibition of β-hexosaminidase release at 100 µM concentration, which was ten-fold higher than the effective concentration of H2L5186303 (10 µM) (Figure 2A). This may imply a non-specific off-target effect of the LPA2 agonist, GRI977143 (Figure 2A). Reference: Int J Mol Sci. 2022 Aug 28;23(17):9745. https://pubmed.ncbi.nlm.nih.gov/36077141/

	Solvent	mg/mL	mM
Solubility
	DMF	10.0	26.64
	DMSO	24.6	65.44
	DMSO:PBS (pH 7.2) (1:40)	0.0	0.07

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 375.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Kiss GN, Lee SC, Fells JI, Liu J, Valentine WJ, Fujiwara Y, Thompson KE, Yates CR, Sümegi B, Tigyi G. Mitigation of radiation injury by selective stimulation of the LPA(2) receptor. Biochim Biophys Acta. 2013 Jan;1831(1):117-25. doi: 10.1016/j.bbalip.2012.08.020. PMID: 23127512; PMCID: PMC3491361. 2. Kiss GN, Fells JI, Gupte R, Lee SC, Liu J, Nusser N, Lim KG, Ray RM, Lin FT, Parrill AL, Sümegi B, Miller DD, Tigyi G. Virtual screening for LPA2-specific agonists identifies a nonlipid compound with antiapoptotic actions. Mol Pharmacol. 2012 Dec;82(6):1162-73. doi: 10.1124/mol.112.079699. Epub 2012 Sep 11. PMID: 22968304; PMCID: PMC3502618. 3. Lee YJ, Im DS. Efficacy Comparison of LPA2 Antagonist H2L5186303 and Agonist GRI977143 on Ovalbumin-Induced Allergic Asthma in BALB/c Mice. Int J Mol Sci. 2022 Aug 28;23(17):9745. doi: 10.3390/ijms23179745. PMID: 36077141; PMCID: PMC9456302. 4. Kaji I, Roland JT, Watanabe M, Engevik AC, Goldstein AE, Hodges CA, Goldenring JR. Lysophosphatidic Acid Increases Maturation of Brush Borders and SGLT1 Activity in MYO5B-deficient Mice, a Model of Microvillus Inclusion Disease. Gastroenterology. 2020 Oct;159(4):1390-1405.e20. doi: 10.1053/j.gastro.2020.06.008. Epub 2020 Jun 12. PMID: 32534933; PMCID: PMC8240502.

In vitro protocol:

In vivo protocol:

1. Lee YJ, Im DS. Efficacy Comparison of LPA2 Antagonist H2L5186303 and Agonist GRI977143 on Ovalbumin-Induced Allergic Asthma in BALB/c Mice. Int J Mol Sci. 2022 Aug 28;23(17):9745. doi: 10.3390/ijms23179745. PMID: 36077141; PMCID: PMC9456302. 2. Kaji I, Roland JT, Watanabe M, Engevik AC, Goldstein AE, Hodges CA, Goldenring JR. Lysophosphatidic Acid Increases Maturation of Brush Borders and SGLT1 Activity in MYO5B-deficient Mice, a Model of Microvillus Inclusion Disease. Gastroenterology. 2020 Oct;159(4):1390-1405.e20. doi: 10.1053/j.gastro.2020.06.008. Epub 2020 Jun 12. PMID: 32534933; PMCID: PMC8240502.

1: Lin KH, Ho YH, Chiang JC, Li MW, Lin SH, Chen WM, Chiang CL, Lin YN, Yang YJ, Chen CN, Lu J, Huang CJ, Tigyi G, Yao CL, Lee H. Pharmacological activation of lysophosphatidic acid receptors regulates erythropoiesis. Sci Rep. 2016 May 31;6:27050. doi: 10.1038/srep27050. PubMed PMID: 27244685; PubMed Central PMCID: PMC4886675. 2: Kiss GN, Lee SC, Fells JI, Liu J, Valentine WJ, Fujiwara Y, Thompson KE, Yates CR, Sümegi B, Tigyi G. Mitigation of radiation injury by selective stimulation of the LPA(2) receptor. Biochim Biophys Acta. 2013 Jan;1831(1):117-25. doi: 10.1016/j.bbalip.2012.08.020. PubMed PMID: 23127512; PubMed Central PMCID: PMC3491361. 3: Kiss GN, Fells JI, Gupte R, Lee SC, Liu J, Nusser N, Lim KG, Ray RM, Lin FT, Parrill AL, Sümegi B, Miller DD, Tigyi G. Virtual screening for LPA2-specific agonists identifies a nonlipid compound with antiapoptotic actions. Mol Pharmacol. 2012 Dec;82(6):1162-73. doi: 10.1124/mol.112.079699. PubMed PMID: 22968304; PubMed Central PMCID: PMC3502618.