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

GRI977143
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 531862

CAS#: 325850-81-5

Description: 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

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 531862
Name: GRI977143
CAS#: 325850-81-5
Chemical Formula: C22H17NO3S
Exact Mass: 375.09
Molecular Weight: 375.442
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 295	2 Weeks
10mg	USD 500	2 Weeks
25mg	USD 950	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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

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Product Data:

Product Data

Instruction:

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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/

Solubility Data

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

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:	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.
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.

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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.

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