(AS)-6-CHLORO-5-FLUORO-ALPHA-METHYL-1H-INDOLE-1-ETHANAMINE FUMARATE
- Product Name
- (AS)-6-CHLORO-5-FLUORO-ALPHA-METHYL-1H-INDOLE-1-ETHANAMINE FUMARATE
- CAS No.
- 169675-09-6
- Chemical Name
- (AS)-6-CHLORO-5-FLUORO-ALPHA-METHYL-1H-INDOLE-1-ETHANAMINE FUMARATE
- Synonyms
- RO 60-0175 FUMARATE;Ro 600175 fumarate,Ro 60 0175 fumarate;(S)-1-(6-Chloro-5-fluoro-1H-indol-1-yl)propan-2-amine fumarate;(αS)-6-Chloro-5-fluoro-α-methyl-1H-indole-1-ethanaminefumarate;(S)-2-(Chloro-5-fluoro-indol-L-yl)-1-methylethylamine fumarate;(AS)-6-CHLORO-5-FLUORO-ALPHA-METHYL-1H-INDOLE-1-ETHANAMINE FUMARATE;(alpha-S)-6-Chloro-5-fluoro-alpha-methyl-(1H)-indole-1-ethaneaminefumarate;1H-Indole-1-ethanaMine, 6-chloro-5-fluoro-a-Methyl-, (aS)-, (2E)-2-butenedioate;1H-Indole-1-ethanamine, 6-chloro-5-fluoro-alpha-methyl-, (S)-, (E)-2-butenedioate (1:1);1H-Indole-1-ethanamine, 6-chloro-5-fluoro-alpha-methyl-, (alphas)-, (2E)-2-butenedioate (1:1)
- CBNumber
- CB9664058
- Molecular Formula
- C15H16ClFN2O4
- Formula Weight
- 342.75
- MOL File
- 169675-09-6.mol
(AS)-6-CHLORO-5-FLUORO-ALPHA-METHYL-1H-INDOLE-1-ETHANAMINE FUMARATE Property
- storage temp.
- Desiccate at RT
- solubility
- Soluble to 5 mM in water and to 20 mM in DMSO
- form
- Powder
- color
- White to off-white
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P321Specific treatment (see … on this label).
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
N-Bromosuccinimide Price
- Product number
- 29520
- Product name
- Ro 60-0175
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 29520
- Product name
- Ro 60-0175
- Packaging
- 5mg
- Price
- $86
- Updated
- 2024/03/01
- Product number
- 29520
- Product name
- Ro 60-0175
- Packaging
- 10mg
- Price
- $138
- Updated
- 2021/12/16
- Product number
- 1854
- Product name
- Ro60-0175fumarate
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $159
- Updated
- 2021/12/16
- Product number
- 1854
- Product name
- Ro60-0175fumarate
- Purity
- ≥98%(HPLC)
- Packaging
- 50
- Price
- $658
- Updated
- 2021/12/16
(AS)-6-CHLORO-5-FLUORO-ALPHA-METHYL-1H-INDOLE-1-ETHANAMINE FUMARATE Chemical Properties,Usage,Production
Description
Ro 60-0175 is an agonist of the serotonin (5-HT) receptor subtype 5-HT2 that stimulates increases in intracellular calcium levels in CHO-K1 cells expressing human 5-HT2A, 5-HT2B, and 5-HT2C receptors (EC50s = 447, 0.9, and 32 nM, respectively). It is selective for human 5-HT2A and 5-HT2C (Kis = 32 and 1 nM, respectively) over human 5-HT1A, 5-HT1D, 5-HT6, and 5-HT7, rat 5-HT1B and 5-HT3, and guinea pig 5-HT4 receptors (Kis = ≥1,995 nM), as well as adenosine A1 and A2, histamine H1-3, dopamine D1-5, α1-, α2-, and β1-adrenergic, M1-5 muscarinic, nicotinic, kainate, AMPA, and μ-, δ-, and κ-opioid receptors (IC50s = >1,000 nM), but does bind to β2-adrenergic receptors (IC50 = 251 nM). In vivo, Ro 60-0175 increases plasma levels of corticosterone, oxytocin, and prolactin in rats (ED50s = 2.43, 4.19, and 4.03 mg/kg, respectively), effects that are not inhibited by the 5-HT2C antagonist SB-242084 or the 5-HT2A antagonist MDL 100,907 (volinanserin; ).
Uses
Ro 60-0175 fumarate is a potent and selective SR-2 agonist.
Biological Activity
Potent, selective 5-HT 2 receptor agonist; shows selectivity for the 5-HT 2C subtype (pK i values are 9, 7.5, 5.4, 5.2 and 5.6 for human 5-HT 2C , 2A , 1A , 6 and 7 receptors respectively). Centrally active following oral or systemic administration in vivo .
in vivo
Ro60-0175 (1 mg/kg; s.c.) fumarate preserves the regularity of responding seen in control animals in drug-treated group, but drug-treated animals reach their break-points earlier[1].
Ro60-0175 (0.3, 1, and? 3 mg/kg (Ro60-0175); 1?mg/kg (yohimbine); s.c.; i.p.) fumarate dose dependently attenuates the response increased by the yohimbine treatment alone relative to vehicle injection[1].
Ro60-0175 (0.5 mg/kg (SB242084); 1?mg/kg (Ro60-0175); 1?mg/kg (yohimbine); s.c.; i.p.) fumarate reduces responding and that this effect is prevented by SB242084 pretreatment[1].
Ro60-0175 (0.3, 1, and?3 mg/kg; s.c.) fumarate significantly reduces responding on the active lever in the reinstatement group[1].
Ro60-0175 (0.5?mg/kg SB242084; 1?mg/kg Ro60-0175; s.c.; i.p.) fumarate reduces responding compared to vehicle in the reinstatement group, and that this effect is prevented by pretreatment with SB242084. For responding on the inactive lever, there are no significant main effects or interactions[1].
IC 50
5-HT2C Receptor
storage
Desiccate at RT
References
[1] R H P PORTER. Functional characterization of agonists at recombinant human 5-HT2A, 5-HT2B and 5-HT2C receptors in CHO-K1 cells[J]. British Journal of Pharmacology, 2009, 128 1: 13-20. DOI: 10.1038/sj.bjp.0702751
[2] J R MARTIN. 5-HT2C receptor agonists: pharmacological characteristics and therapeutic potential.[J]. Journal of Pharmacology and Experimental Therapeutics, 1998, 286 2: 913-924.
[3] K J DAMJANOSKA. Neuroendocrine evidence that (S)-2-(chloro-5-fluoro-indol- l-yl)-1-methylethylamine fumarate (Ro 60-0175) is not a selective 5-hydroxytryptamine(2C) receptor agonist.[J]. Journal of Pharmacology and Experimental Therapeutics, 2003, 304 3: 1209-1216. DOI: 10.1124/jpet.102.043489
(AS)-6-CHLORO-5-FLUORO-ALPHA-METHYL-1H-INDOLE-1-ETHANAMINE FUMARATE Preparation Products And Raw materials
Raw materials
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