Grassofermata | NAV-2729 | CAS#419547-11-8

MedKoo Cat#: 407413 | Name: Grassofermata

Description:

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

Grassofermata, also known as NAV-2729, is a selective ARF6 inhibitor (IC50 = 1.0 μM). Blocking ARF6 with a small-molecule inhibitor reduces uveal melanoma cell proliferation and tumorigenesis in a mouse model, confirming the functional relevance of this pathway and suggesting a therapeutic strategy for Gα-mediated diseases.

Chemical Structure

Grassofermata

CAS#419547-11-8

Theoretical Analysis

MedKoo Cat#: 407413

Name: Grassofermata

CAS#: 419547-11-8

Chemical Formula: C25H17ClN4O3

Exact Mass: 456.0989

Molecular Weight: 456.89

Elemental Analysis: C, 65.72; H, 3.75; Cl, 7.76; N, 12.26; O, 10.51

Price and Availability

Size	Price	Availability
10mg	USD 350.00	2 Weeks
25mg	USD 650.00	2 Weeks
50mg	USD 950.00	2 Weeks
100mg	USD 1,650.00	2 Weeks

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Related CAS #

419547-11-8

Synonym

NAV-2729; NAV 2729; NAV2729; Grassofermata;

IUPAC/Chemical Name

3-(4-Chlorophenyl)-5-(4-nitrophenyl)-2-(phenylmethyl)pyrazolo[1,5-a]pyrimidin-7(4H)-one

InChi Key

GUUWHOSUKOCRHG-UHFFFAOYSA-N

InChi Code

InChI=1S/C25H17ClN4O3/c26-19-10-6-18(7-11-19)24-22(14-16-4-2-1-3-5-16)28-29-23(31)15-21(27-25(24)29)17-8-12-20(13-9-17)30(32)33/h1-13,15,27H,14H2

SMILES Code

O=C1C=C(C2=CC=C([N+]([O-])=O)C=C2)NC3=C(C4=CC=C(Cl)C=C4)C(CC5=CC=CC=C5)=NN13

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

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

NAV-2729 is a dual Arf1/Arf6 activation inhibitor.

In vitro activity:

Grassofermata was effective in inhibiting the uptake of FA analog C1-BODIPY-C12 in C2C12 and INS-1E cells with IC50 of 10.6 and 8.3 μM respectively (Fig. 1C and 1D). By comparison, the IC50 was higher in human adipocytes (58.2 μM; Fig. 1E). As expected, Grassofermata exhibited a non-competitive mechanism of inhibition (Fig. 1F). Reference: Biochem Biophys Res Commun. 2015 Sep 25;465(3):534-41. https://pubmed.ncbi.nlm.nih.gov/26284975/

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	DMSO	47.2	103.25

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 456.89 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. Black PN, Ahowesso C, Montefusco D, Saini N, DiRusso CC. Fatty Acid Transport Proteins: Targeting FATP2 as a Gatekeeper Involved in the Transport of Exogenous Fatty Acids. Medchemcomm. 2016 Apr 1;7(4):612-622. doi: 10.1039/C6MD00043F. Epub 2016 Feb 19. PMID: 27446528; PMCID: PMC4948302. 2. Saini N, Black PN, Montefusco D, DiRusso CC. Fatty acid transport protein-2 inhibitor Grassofermata/CB5 protects cells against lipid accumulation and toxicity. Biochem Biophys Res Commun. 2015 Sep 25;465(3):534-41. doi: 10.1016/j.bbrc.2015.08.055. Epub 2015 Aug 15. PMID: 26284975; PMCID: PMC4589248.

In vitro protocol:

In vivo protocol:

TBD

1: Yoo JH, Shi DS, Grossmann AH, Sorensen LK, Tong Z, Mleynek TM, Rogers A, Zhu W, Richards JR, Winter JM, Zhu J, Dunn C, Bajji A, Shenderovich M, Mueller AL, Woodman SE, Harbour JW, Thomas KR, Odelberg SJ, Ostanin K, Li DY. ARF6 Is an Actionable Node that Orchestrates Oncogenic GNAQ Signaling in Uveal Melanoma. Cancer Cell. 2016 Jun 13;29(6):889-904. doi: 10.1016/j.ccell.2016.04.015. PubMed PMID: 27265506; PubMed Central PMCID: PMC5027844.