Ro 60-0175 fumarate
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MedKoo CAT#: 532566

CAS#: 169675-09-6 (fumarate)

Description: Ro60-0175 is a potent and selective SR-2 agonist. It shows selectivity for the 5-HT2C subtype (pKi values are 9, 7.5, 5.4, 5.2 and 5.6 for human 5-HT2C, 2A, 1A, 6 and 7 receptors respectively). Ro60-0175 acts as a potent and selective agonist for both the 5-HT2B and 5-HT2C serotonin receptor subtypes, with good selectivity over the closely related 5-HT2A subtype, and little or no affinity at other receptors.


Chemical Structure

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Ro 60-0175 fumarate
CAS# 169675-09-6 (fumarate)

Theoretical Analysis

MedKoo Cat#: 532566
Name: Ro 60-0175 fumarate
CAS#: 169675-09-6 (fumarate)
Chemical Formula: C15H16ClFN2O4
Exact Mass: 0.00
Molecular Weight: 342.750
Elemental Analysis: C, 52.56; H, 4.71; Cl, 10.34; F, 5.54; N, 8.17; O, 18.67

Price and Availability

Size Price Availability Quantity
5mg USD 350 2 Weeks
10mg USD 550 2 Weeks
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Related CAS #: 169675-09-6 (fumarate)   169675-08-5 (free base)    

Synonym: Ro 60-0175 fumarate; Ro60-0175; Ro-60-0175; Ro 60-0175; Ro600175; Ro-600175; Ro 600175;

IUPAC/Chemical Name: (S)-1-(6-chloro-5-fluoro-1H-indol-1-yl)propan-2-amine fumarate

InChi Key: CEPHEXXZGQBXGT-XZTIXWOLSA-N

InChi Code: InChI=1S/C11H12ClFN2.C4H4O4/c1-7(14)6-15-3-2-8-4-10(13)9(12)5-11(8)15;5-3(6)1-2-4(7)8/h2-5,7H,6,14H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1+/t7-;/m0./s1

SMILES Code: C[C@@H](CN1C=CC2=CC(=C(C=C21)Cl)F)N.C(=C/C(=O)O)\C(=O)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 and water

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:
Biological target: Ro 60-0175 fumarate is a potent, selective 5-HT2 receptor agonist. It shows selectivity for the 5-HT2C subtype (pKi values are 9, 7.5, 5.4, 5.2 and 5.6 for human 5-HT2C, 2A, 1A, 6 and 7 receptors respectively). Ro 60-0175 fumarate is centrally active following oral or systemic administration in vivo.
In vitro activity: To be determined
In vivo activity: In squirrel monkeys, Ro 60-0175 attenuated the reinforcing effects of cocaine during ongoing cocaine self-administration. Ro 60-0175 exhibited behavioral specificity because it did not significantly alter nondrug-maintained responding. In vivo microdialysis studies revealed that Ro 60-0175 pretreatment caused a reduction of cocaine-induced dopamine increases within the nucleus accumbens, but not the caudate nucleus. Reference: J Pharmacol Exp Ther. 2012 May;341(2):424-34. https://pubmed.ncbi.nlm.nih.gov/22328576/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 6.9 20.00
Water 1.7 5.00

Preparing Stock Solutions

The following data is based on the product molecular weight 342.75 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: 1. Mbaki Y, Gardiner J, McMurray G, Ramage AG. 5-HT 2A receptor activation of the external urethral sphincter and 5-HT 2C receptor inhibition of micturition: a study based on pharmacokinetics in the anaesthetized female rat. Eur J Pharmacol. 2012 May 5;682(1-3):142-52. doi: 10.1016/j.ejphar.2012.02.010. Epub 2012 Feb 21. PMID: 22374259. 2. Manvich DF, Kimmel HL, Howell LL. Effects of serotonin 2C receptor agonists on the behavioral and neurochemical effects of cocaine in squirrel monkeys. J Pharmacol Exp Ther. 2012 May;341(2):424-34. doi: 10.1124/jpet.111.186981. Epub 2012 Feb 10. PMID: 22328576; PMCID: PMC3336818.
In vitro protocol: To be determined
In vivo protocol: 1. Mbaki Y, Gardiner J, McMurray G, Ramage AG. 5-HT 2A receptor activation of the external urethral sphincter and 5-HT 2C receptor inhibition of micturition: a study based on pharmacokinetics in the anaesthetized female rat. Eur J Pharmacol. 2012 May 5;682(1-3):142-52. doi: 10.1016/j.ejphar.2012.02.010. Epub 2012 Feb 21. PMID: 22374259. 2. Manvich DF, Kimmel HL, Howell LL. Effects of serotonin 2C receptor agonists on the behavioral and neurochemical effects of cocaine in squirrel monkeys. J Pharmacol Exp Ther. 2012 May;341(2):424-34. doi: 10.1124/jpet.111.186981. Epub 2012 Feb 10. PMID: 22328576; PMCID: PMC3336818.

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