Ro67-7476 | CAS#298690-60-5 | PAM mGlu1 receptor

MedKoo Cat#: 532571 | Name: Ro67-7476

Description:

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

Ro67-7476 is a positive allosteric modulator of mGlu1 receptors. It potentiates glutamate-induced calcium release (EC50 = 60.1 nM at rat mGluR1a). Ro67-7476 displays no activity at human mGlu1 receptors.

Chemical Structure

Ro67-7476

CAS#298690-60-5

Theoretical Analysis

MedKoo Cat#: 532571

Name: Ro67-7476

CAS#: 298690-60-5

Chemical Formula: C17H18FNO2S

Exact Mass: 319.1042

Molecular Weight: 319.39

Elemental Analysis: C, 63.93; H, 5.68; F, 5.95; N, 4.39; O, 10.02; S, 10.04

Price and Availability

Size	Price	Availability
10mg	USD 120.00	Ready to ship
25mg	USD 250.00	Ready to ship
50mg	USD 450.00	Ready to ship
100mg	USD 750.00	Ready to ship
200mg	USD 1,250.00	Ready to ship
500mg	USD 1,950.00	Ready to ship
1g	USD 2,950.00	2 weeks
2g	USD 5,250.00	2 weeks

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Related CAS #

No Data

Synonym

Ro67-7476; Ro-67-7476; Ro 67-7476.

IUPAC/Chemical Name

(2S)-2-(4-Fluorophenyl)-1-[(4-methylphenyl)sulfonyl]pyrrolidine

InChi Key

DAEHFYNGSSBGSS-KRWDZBQOSA-N

InChi Code

InChI=1S/C17H18FNO2S/c1-13-4-10-16(11-5-13)22(20,21)19-12-2-3-17(19)14-6-8-15(18)9-7-14/h4-11,17H,2-3,12H2,1H3/t17-/m0/s1

SMILES Code

O=S(N1[C@H](C2=CC=C(F)C=C2)CCC1)(C3=CC=C(C)C=C3)=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

>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#C20R12B04

QC Data

View QC data: current batch, Lot#C20R12B04

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

Ro 67-7476 is a positive allosteric modulator of mGluR1 and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC50 of 60.1 nM.

In vitro activity:

Figure 5 shows the effect of 100 nM R214127 on 1 µM Ro 01-6128, Ro 67-4853, or Ro 67-7476 induced P-ERK1/2. R214127 completely inhibits the activity of these compounds but does not effect basal ERK1/2 phosphorylation, demonstrating that noncompetitive antagonists of mGluR1 can block the ability of the mGluR1 PAMs to cause P-ERK1/2 induction. The EC50 values P-ERK1/2 activation for the mGluR1 PAMs were all in the low to mid nanomolar range with a values of 247.9 ± 50.6 nM (Ro 01-6128), 9.2 ± 6.2 nM (Ro 67-4853), or 163.3 ± 44.8 nM (Ro 67-7476). Notably, the EC50s for full P-ERK1/2 activation are nearly identical to the EC50s for calcium mobilization potentiation. Together, these data demonstrate that Ro 01-6128, Ro 67-4853, and Ro 67-7476 activate mGluR1-induced ERK1/2 phosphorylation in the absence of exogenously added agonist, showing that these PAMs of mGluR1 have fundamentally different effects on mGluR1 coupling to calcium mobilization versus ERK1/2 phosphorylation. Reference: Neuropharmacology. 2008 Sep; 55(4): 419–427. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2600811/

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	DMSO	30.0	93.90

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 319.39 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. Sheffler DJ, Conn PJ. Allosteric potentiators of metabotropic glutamate receptor subtype 1a differentially modulate independent signaling pathways in baby hamster kidney cells. Neuropharmacology. 2008 Sep;55(4):419-27. doi: 10.1016/j.neuropharm.2008.06.047. Epub 2008 Jul 2. PMID: 18625258; PMCID: PMC2600811.

In vitro protocol:

In vivo protocol:

TBD

1: Sheffler DJ, Conn PJ. Allosteric potentiators of metabotropic glutamate receptor subtype 1a differentially modulate independent signaling pathways in baby hamster kidney cells. Neuropharmacology. 2008 Sep;55(4):419-27. doi: 10.1016/j.neuropharm.2008.06.047. Epub 2008 Jul 2. PubMed PMID: 18625258; PubMed Central PMCID: PMC2600811. 2: Chen Y, Goudet C, Pin JP, Conn PJ. N-{4-Chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl}-2-hydroxybe nzamide (CPPHA) acts through a novel site as a positive allosteric modulator of group 1 metabotropic glutamate receptors. Mol Pharmacol. 2008 Mar;73(3):909-18. Epub 2007 Dec 4. PubMed PMID: 18056795. 3: Hemstapat K, de Paulis T, Chen Y, Brady AE, Grover VK, Alagille D, Tamagnan GD, Conn PJ. A novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulators. Mol Pharmacol. 2006 Aug;70(2):616-26. Epub 2006 Apr 27. PubMed PMID: 16645124. 4: Xie J, Xu J, Chen H. Regulatory mechanisms of miR-212-3p on the secretion of inflammatory factors in monocyte-macrophages and the directed differentiation into osteoclasts in ankylosing spondylitis. Aging (Albany NY). 2023 Nov 28;15(22):13411-13421. doi: 10.18632/aging.205249. Epub 2023 Nov 28. PMID: 38019469; PMCID: PMC10713416.