SET2 | CAS#2313525-20-9 | TRPV2 antagonist

MedKoo Cat#: 463662 | Name: SET2

Featured

Description:

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

SET2 is a novel selective TRPV2 antagonist.

Chemical Structure

SET2

CAS#2313525-20-9

Theoretical Analysis

MedKoo Cat#: 463662

Name: SET2

CAS#: 2313525-20-9

Chemical Formula: C17H21F3N4O2S

Exact Mass: 402.1337

Molecular Weight: 402.44

Elemental Analysis: C, 50.74; H, 5.26; F, 14.16; N, 13.92; O, 7.95; S, 7.97

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 450.00	2 Weeks

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

No Data

Synonym

SET2; SET 2; SET-2;

IUPAC/Chemical Name

N-(furan-2-ylmethyl)-3-((4-(methyl(propyl)amino)-6-(trifluoromethyl)pyrimidin-2-yl)thio)propanamide

InChi Key

LZHSWRWIMQRTOP-UHFFFAOYSA-N

InChi Code

InChI=1S/C17H21F3N4O2S/c1-3-7-24(2)14-10-13(17(18,19)20)22-16(23-14)27-9-6-15(25)21-11-12-5-4-8-26-12/h4-5,8,10H,3,6-7,9,11H2,1-2H3,(H,21,25)

SMILES Code

FC(F)(F)C1=CC(N(C)CCC)=NC(SCCC(NCC2=CC=CO2)=O)=N1

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

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

SET2 is a selective TRPV2 antagonist (IC50=0.46 μM).

In vitro activity:

This study describes the discovery of SET2, which was then employed as a chemical probe. SET2 inhibited TRPV2, which reduced prostate cancer migration, highlighting TRPV2 as a potential antimetastasis therapeutic target. Functional assays indicated the coupling of TRPV2 to the metastasis mediator LPAR1. The discovery of this potent inhibitor opens new avenues for pharmacological applications and therapeutic development targeting the TRPV2 channel. Reference: J Med Chem. 2019 Feb 14;62(3):1373-1384. https://pubmed.ncbi.nlm.nih.gov/30620187/

In vivo activity:

To be determined

	Solvent	mg/mL	mM	comments
Solubility
	DMSO	100.0	248.29

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 402.44 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. Chai H, Cheng X, Zhou B, Zhao L, Lin X, Huang D, Lu W, Lv H, Tang F, Zhang Q, Huang W, Li Y, Yang H. Structure-Based Discovery of a Subtype-Selective Inhibitor Targeting a Transient Receptor Potential Vanilloid Channel. J Med Chem. 2019 Feb 14;62(3):1373-1384. doi: 10.1021/acs.jmedchem.8b01496. Epub 2019 Jan 16. PMID: 30620187.

In vitro protocol:

In vivo protocol: