MS0015203 | CAS#73912-52-4 | GPR171 agonist

MedKoo Cat#: 563739 | Name: MS0015203

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Description:

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

MS0015203 is a potent and selective agonist of the neuropeptide receptor GPR171.

Chemical Structure

MS0015203

CAS#73912-52-4

Theoretical Analysis

MedKoo Cat#: 563739

Name: MS0015203

CAS#: 73912-52-4

Chemical Formula: C12H11NO5

Exact Mass: 249.0637

Molecular Weight: 249.22

Elemental Analysis: C, 57.83; H, 4.45; N, 5.62; O, 32.10

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 250.00	2 Weeks
25mg	USD 575.00	2 Weeks

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Related CAS #

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Synonym

MS0015203; MS-0015203; MS 0015203;

IUPAC/Chemical Name

5-[(2-Methyl-1-oxo-2-propen-1-yl)amino]-1,3-benzenedicarboxylic acid

InChi Key

NVOBVSWSDYFEMR-UHFFFAOYSA-N

InChi Code

InChI=1S/C12H11NO5/c1-6(2)10(14)13-9-4-7(11(15)16)3-8(5-9)12(17)18/h3-5H,1H2,2H3,(H,13,14)(H,15,16)(H,17,18)

SMILES Code

O=C(C1=CC(NC(C(C)=C)=O)=CC(C(O)=O)=C1)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

>3 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

2934.99.03.00

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

MS15203 is a potent and selective GPR171 agonist.

In vitro activity:

This study identified MS0015203 as an agonist of GPR171 and demonstrated the selectivity of MS0015203 for GPR171 by testing the binding of this compound to 80 other membrane proteins, including family A GPCRs. Reducing the expression of GPR171 by shRNA (short hairpin RNA)-mediated knockdown blunted the cellular and tissue response to MS0015203. Reference: Sci Signal. 2016 May 31;9(430):ra55. https://pubmed.ncbi.nlm.nih.gov/27245612/

In vivo activity:

The therapeutic potential of the GPR171 agonist, MS15203, in its ability to alleviate chronic pain in male and female mice using a once-daily systemic dose (10 mg/kg, i.p.) of MS15203 over the course of 5 days. MS15203 treatment decreased the duration of thermal hypersensitivity in CFA-treated male mice following 3 days of once-daily administration. MS15203 treatment also produced an improvement in allodynia in male mice, but not female mice, in neuropathic pain after 5 days of treatment. Reference: Front Pain Res (Lausanne). 2021 Sep 10;2:695396. https://pubmed.ncbi.nlm.nih.gov/35295419/

	Solvent	mg/mL	mM
Solubility
	DMSO	62.5	250.62

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 249.22 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. Wardman JH, Gomes I, Bobeck EN, Stockert JA, Kapoor A, Bisignano P, Gupta A, Mezei M, Kumar S, Filizola M, Devi LA. Identification of a small-molecule ligand that activates the neuropeptide receptor GPR171 and increases food intake. Sci Signal. 2016 May 31;9(430):ra55. doi: 10.1126/scisignal.aac8035. PMID: 27245612; PMCID: PMC5150984.

In vitro protocol:

In vivo protocol:

1. Ram A, Edwards T, McCarty A, Afrose L, McDermott MV, Bobeck EN. GPR171 Agonist Reduces Chronic Neuropathic and Inflammatory Pain in Male, But Not Female Mice. Front Pain Res (Lausanne). 2021 Sep 10;2:695396. doi: 10.3389/fpain.2021.695396. PMID: 35295419; PMCID: PMC8915562. 2. Wardman JH, Gomes I, Bobeck EN, Stockert JA, Kapoor A, Bisignano P, Gupta A, Mezei M, Kumar S, Filizola M, Devi LA. Identification of a small-molecule ligand that activates the neuropeptide receptor GPR171 and increases food intake. Sci Signal. 2016 May 31;9(430):ra55. doi: 10.1126/scisignal.aac8035. PMID: 27245612; PMCID: PMC5150984.

1: Wardman JH, Gomes I, Bobeck EN, Stockert JA, Kapoor A, Bisignano P, Gupta A, Mezei M, Kumar S, Filizola M, Devi LA. Identification of a small-molecule ligand that activates the neuropeptide receptor GPR171 and increases food intake. Sci Signal. 2016 May 31;9(430):ra55. doi: 10.1126/scisignal.aac8035. PubMed PMID: 27245612; PubMed Central PMCID: PMC5150984.