Ro0711401 | CAS#714971-87-6 | mGlu1 receptor agonist

MedKoo Cat#: 532549 | Name: Ro0711401

Description:

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

Ro0711401 is a mGlu1 receptor agonist.

Chemical Structure

Ro0711401

CAS#714971-87-6

Theoretical Analysis

MedKoo Cat#: 532549

Name: Ro0711401

CAS#: 714971-87-6

Chemical Formula: C18H11F3N2O3

Exact Mass: 360.0722

Molecular Weight: 360.29

Elemental Analysis: C, 60.01; H, 3.08; F, 15.82; N, 7.78; O, 13.32

Price and Availability

Size	Price	Availability
10mg	USD 90.00	Ready to ship
25mg	USD 190.00	Ready to ship
50mg	USD 350.00	Ready to ship
100mg	USD 550.00	Ready to ship
200mg	USD 950.00	Ready to ship
500mg	USD 1,950.00	Ready to ship
1g	USD 3,450.00	Ready to ship
2g	USD 6,150.00	Ready to ship

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Related CAS #

No Data

Synonym

Ro0711401; Ro-0711401; Ro 0711401; RO07-11401; RO0711401; RO07 11401

IUPAC/Chemical Name

N-[4-(trifluoromethyl)-1,3-oxazol-2-yl]-9H-xanthene-9-carboxamide

InChi Key

GSGDLBUOSWGZER-UHFFFAOYSA-N

InChi Code

InChI=1S/C18H11F3N2O3/c19-18(20,21)14-9-25-17(22-14)23-16(24)15-10-5-1-3-7-12(10)26-13-8-4-2-6-11(13)15/h1-9,15H,(H,22,23,24)

SMILES Code

O=C(C1C2=C(OC3=C1C=CC=C3)C=CC=C2)NC4=NC(C(F)(F)F)=CO4

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

Certificate of Analysis

View CoA: current batch, Lot# B21B04C19

QC Data

View QC data: current batch, Lot# B21B04C19

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

RO0711401 is a selective and orally active positive allosteric modulator of mGlu1 receptor with an EC50 of 56 nM.

In vitro activity:

To be determined

In vivo activity:

mGlu5 receptor PAMs are potential candidates for the treatment of absence epilepsy in humans. Treatment with RO0711401 enhanced the expression of both mGlu1a and mGlu5 receptors in the thalamus and cortex of WAG/Rij rats. However, in non-epileptic rats, repeated injections of RO0711401 and VU0360172 down-regulated the expression of mGlu1a and mGlu5 receptors. Levels of RO0711401 were reduced in the cortex at day 8 of treatment. Reference: Neuropharmacology. 2014 Oct;85:91-103. https://pubmed.ncbi.nlm.nih.gov/24859611/

	Solvent	mg/mL	mM
Solubility
	DMSO	100.0	277.55

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 360.29 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. Liberatore F, Antenucci N, Tortolani D, Mascio G, Fanti F, Sergi M, Battaglia G, Bruno V, Nicoletti F, Maccarrone M, Notartomaso S. Targeting mGlu1 Receptors in the Treatment of Motor and Cognitive Dysfunctions in Mice Modeling Type 1 Spinocerebellar Ataxia. Cells. 2022 Dec 3;11(23):3916. doi: 10.3390/cells11233916. PMID: 36497172; PMCID: PMC9738505. 2. D'Amore V, Santolini I, Celli R, Lionetto L, De Fusco A, Simmaco M, van Rijn CM, Vieira E, Stauffer SR, Conn PJ, Bosco P, Nicoletti F, van Luijtelaar G, Ngomba RT. Head-to head comparison of mGlu1 and mGlu5 receptor activation in chronic treatment of absence epilepsy in WAG/Rij rats. Neuropharmacology. 2014 Oct;85:91-103. doi: 10.1016/j.neuropharm.2014.05.005. Epub 2014 May 20. PMID: 24859611; PMCID: PMC4356528.

In vitro protocol:

To be determined

In vivo protocol:

1: D'Amore V, Santolini I, Celli R, Lionetto L, De Fusco A, Simmaco M, van Rijn CM, Vieira E, Stauffer SR, Conn PJ, Bosco P, Nicoletti F, van Luijtelaar G, Ngomba RT. Head-to head comparison of mGlu1 and mGlu5 receptor activation in chronic treatment of absence epilepsy in WAG/Rij rats. Neuropharmacology. 2014 Oct;85:91-103. doi: 10.1016/j.neuropharm.2014.05.005. Epub 2014 May 20. PMID: 24859611; PMCID: PMC4356528. 2: Liberatore F, Antenucci N, Tortolani D, Mascio G, Fanti F, Sergi M, Battaglia G, Bruno V, Nicoletti F, Maccarrone M, Notartomaso S. Targeting mGlu1 Receptors in the Treatment of Motor and Cognitive Dysfunctions in Mice Modeling Type 1 Spinocerebellar Ataxia. Cells. 2022 Dec 3;11(23):3916. doi: 10.3390/cells11233916. PMID: 36497172; PMCID: PMC9738505. 3: Notartomaso S, Mascio G, Scarselli P, Martinello K, Fucile S, Gradini R, Bruno V, Battaglia G, Nicoletti F. Expression of the K+/Cl- cotransporter, KCC2, in cerebellar Purkinje cells is regulated by group-I metabotropic glutamate receptors. Neuropharmacology. 2017 Mar 15;115:51-59. doi: 10.1016/j.neuropharm.2016.07.032. Epub 2016 Aug 3. PMID: 27498071. 4: Notartomaso S, Zappulla C, Biagioni F, Cannella M, Bucci D, Mascio G, Scarselli P, Fazio F, Weisz F, Lionetto L, Simmaco M, Gradini R, Battaglia G, Signore M, Puliti A, Nicoletti F. Pharmacological enhancement of mGlu1 metabotropic glutamate receptors causes a prolonged symptomatic benefit in a mouse model of spinocerebellar ataxia type 1. Mol Brain. 2013 Nov 19;6:48. doi: 10.1186/1756-6606-6-48. PMID: 24252411; PMCID: PMC4225515. 5: D'Amore V, von Randow C, Nicoletti F, Ngomba RT, van Luijtelaar G. Anti- absence activity of mGlu1 and mGlu5 receptor enhancers and their interaction with a GABA reuptake inhibitor: Effect of local infusions in the somatosensory cortex and thalamus. Epilepsia. 2015 Jul;56(7):1141-51. doi: 10.1111/epi.13024. Epub 2015 Jun 3. PMID: 26040777. 6: Fazio F, Notartomaso S, Aronica E, Storto M, Battaglia G, Vieira E, Gatti S, Bruno V, Biagioni F, Gradini R, Nicoletti F, Di Marco R. Switch in the expression of mGlu1 and mGlu5 metabotropic glutamate receptors in the cerebellum of mice developing experimental autoimmune encephalomyelitis and in autoptic cerebellar samples from patients with multiple sclerosis. Neuropharmacology. 2008 Sep;55(4):491-9. doi: 10.1016/j.neuropharm.2008.06.066. Epub 2008 Jul 8. PMID: 18619983. 7: Ngomba RT, Santolini I, Biagioni F, Molinaro G, Simonyi A, van Rijn CM, D'Amore V, Mastroiacovo F, Olivieri G, Gradini R, Ferraguti F, Battaglia G, Bruno V, Puliti A, van Luijtelaar G, Nicoletti F. Protective role for type-1 metabotropic glutamate receptors against spike and wave discharges in the WAG/Rij rat model of absence epilepsy. Neuropharmacology. 2011 Jun;60(7-8):1281-91. doi: 10.1016/j.neuropharm.2011.01.007. Epub 2011 Jan 26. PMID: 21277877.