MRS-1477
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MedKoo CAT#: 563521

CAS#: 212200-21-0

Description: MRS-1477 is a TRPV1 positive allosteric modulator (PAM). Withdrawal responses of the capsaicin-only or MRS1477-only treated paws were not significantly different from the untreated, contralateral paws. However, rats treated with the combination of capsaicin and MRS1477 exhibited increased withdrawal latency and decreased response intensity consistent with agonist potentiation and inactivation or lesion of TRPV1-containing nerve terminals.


Chemical Structure

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MRS-1477
CAS# 212200-21-0

Theoretical Analysis

MedKoo Cat#: 563521
Name: MRS-1477
CAS#: 212200-21-0
Chemical Formula: C21H27NO4S
Exact Mass: 389.17
Molecular Weight: 389.510
Elemental Analysis: Chemical Formula: C21H27NO4S Exact Mass: 389.1661 Molecular Weight: 389.5100 Elemental Analysis: C, 64.76; H, 6.99; N, 3.60; O, 16.43; S, 8.23

Price and Availability

Size Price Availability Quantity
50mg USD 250 2 Weeks
100mg USD 450 2 Weeks
200mg USD 750 2 Weeks
1g USD 2950 2 Weeks
Bulk inquiry

Synonym: MRS-1477; MRS 1477; MRS1477;

IUPAC/Chemical Name: 4-Ethyl-1,4-dihydro-5-[[(2-methoxyethyl)thio]carbonyl]-6-methyl-2-phenyl-3-pyridinecarboxylic acid ethyl ester

InChi Key: DMVMFYWYJCPZGS-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H27NO4S/c1-5-16-17(21(24)27-13-12-25-4)14(3)22-19(15-10-8-7-9-11-15)18(16)20(23)26-6-2/h7-11,16,22H,5-6,12-13H2,1-4H3

SMILES Code: O=C(C1=C(C2=CC=CC=C2)NC(C)=C(C(SCCOC)=O)C1CC)OCC

Appearance: Solid powder

Purity: >95% (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: There is convincing epidemiological and experimental evidence that capsaicin, a potent natural transient receptor potential cation channel vanilloid member 1 (TRPV1) agonist, has anticancer activity. However, capsaicin cannot be given systemically in large doses, because of its induction of acute pain and neurological inflammation. MRS1477, a dihydropyridine derivative acts as a positive allosteric modulator of TRPV1, if added together with capsaicin, but is ineffective, if given alone. Addition of MRS1477 evoked Ca2+ signals in MCF7 breast cancer cells, but not in primary breast epithelial cells. This indicates that MCF7 cells not only express functional TRPV1 channels, but also produce endogenous TRPV1 agonists. https://pubmed.ncbi.nlm.nih.gov/28640864/

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 389.51 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:
In vitro protocol:
In vivo protocol:

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1: Nazıroğlu M, Çiğ B, Blum W, Vizler C, Buhala A, Marton A, Katona R, Jósvay K, Schwaller B, Oláh Z, Pecze L. Targeting breast cancer cells by MRS1477, a positive allosteric modulator of TRPV1 channels. PLoS One. 2017 Jun 22;12(6):e0179950. doi: 10.1371/journal.pone.0179950. eCollection 2017. PubMed PMID: 28640864; PubMed Central PMCID: PMC5481018.

2: Lebovitz EE, Keller JM, Kominsky H, Kaszas K, Maric D, Iadarola MJ. Positive allosteric modulation of TRPV1 as a novel analgesic mechanism. Mol Pain. 2012 Sep 21;8:70. doi: 10.1186/1744-8069-8-70. PubMed PMID: 22998799; PubMed Central PMCID: PMC3556054.

3: Kaszas K, Keller JM, Coddou C, Mishra SK, Hoon MA, Stojilkovic S, Jacobson KA, Iadarola MJ. Small molecule positive allosteric modulation of TRPV1 activation by vanilloids and acidic pH. J Pharmacol Exp Ther. 2012 Jan;340(1):152-60. doi: 10.1124/jpet.111.183053. Epub 2011 Oct 17. PubMed PMID: 22005042; PubMed Central PMCID: PMC3251023.