MS0015203
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 563739

CAS#: 73912-52-4

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


Chemical Structure

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MS0015203
CAS# 73912-52-4

Theoretical Analysis

MedKoo Cat#: 563739
Name: MS0015203
CAS#: 73912-52-4
Chemical Formula: C12H11NO5
Exact Mass: 249.06
Molecular Weight: 249.222
Elemental Analysis: C, 57.83; H, 4.45; N, 5.62; O, 32.10

Price and Availability

Size Price Availability Quantity
5mg USD 250 2 Weeks
25mg USD 575 2 Weeks
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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:
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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 62.5 250.62

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.

Recalculate based on batch purity %
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: 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 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.

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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.